首页 > 最新文献

Recent patents on inflammation & allergy drug discovery最新文献

英文 中文
Effects of Flavonoids and Its Derivatives on Immune Cell Responses. 黄酮类化合物及其衍生物对免疫细胞应答的影响。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-09-30 DOI: 10.2174/1872213X13666190426164124
G. Martínez, M. Mijares, J. D. de Sanctis
BACKGROUNDVarious pieces of evidence have shown that people who consume foods rich in polyphenolic and flavonoids compounds have a lower incidence of inflammatory, autoimmune diseases and cancer.OBJECTIVEThe study aimed to review the most potent compounds that affect the immune response and diseases associated with it.METHODSPublications in PubMed and EmBase, from 1974-2018, and patents form Free patents online, Scifinder, Espacenet and Mendeley in which flavonoids, their semi-synthetic and synthetic derivatives are involved in immunosuppressive or immunostimulatory responses in vitro and in vivo.RESULTSIn vitro, flavonoids and their derivatives inhibit various transcriptional factors, which modulate differentiation, proliferation, activation of immune cells and enhance regulatory T cell generation. Some flavonoids exert anti-inflammatory effects through: Blockade of NF-κB, and NLRP3 inflammasome, inhibition of pro-inflammatory cytokine production, IL-1β, IL-2, IL-6, TNF-α, IL-17A, down regulation of chemokines, and reduction of reactive oxygen and nitrogen species. Nevertheless, several reports have shown that some flavonoids enhance immune response by enhancing: oxygen and nitrogen radicals, antibody production, cytotoxic activity against tumours by increasing activating receptors and down regulating inhibitory receptors. In consequence, flavonoids may be potentially useful for treatment of infectious diseases and cancer.CONCLUSIONThe most potent flavonoids in inflammation that modify immune responses are apigenin, quercetin and Epigallocatechin-3-Gallate (EGCG) although, other compounds are still under study and cannot be excluded. The most relevant patents concerning the use of flavones and other polyphenols were revised. A promising future of these compounds in different therapies is discussed.
背景多种证据表明,食用富含多酚和黄酮类化合物的食物的人炎症、自身免疫性疾病和癌症的发病率较低。目的本研究旨在综述影响免疫反应及其相关疾病的最有效的化合物。1974年至2018年,在PubMed和EmBase上发表的文献,以及在线自由专利、Scifinder、Espacenet和Mendeley的专利,它们的半合成和合成衍生物在体外和体内参与免疫抑制或免疫刺激反应。结果在体外,黄酮类化合物及其衍生物抑制多种转录因子,这些转录因子调节免疫细胞的分化、增殖和活化,并增强调节性T细胞的生成。一些黄酮类化合物通过以下途径发挥抗炎作用:阻断NF-κB和NLRP3炎症小体,抑制促炎细胞因子的产生,IL-1β、IL-2、IL-6、TNF-α、IL-17A,下调趋化因子,减少活性氧和活性氮。然而,一些报道表明,一些黄酮类化合物通过增强氧和氮自由基、抗体产生、通过增加激活受体和下调抑制性受体对肿瘤的细胞毒性活性来增强免疫反应。因此,黄酮类化合物可能潜在地用于治疗传染病和癌症。结论在炎症中最有效的改变免疫反应的黄酮类化合物是芹菜素、槲皮素和表没食子儿茶素-3-没食子酸盐(EGCG),尽管其他化合物仍在研究中,不能排除。修订了有关黄酮和其他多酚使用的最相关专利。讨论了这些化合物在不同治疗中的前景。
{"title":"Effects of Flavonoids and Its Derivatives on Immune Cell Responses.","authors":"G. Martínez, M. Mijares, J. D. de Sanctis","doi":"10.2174/1872213X13666190426164124","DOIUrl":"https://doi.org/10.2174/1872213X13666190426164124","url":null,"abstract":"BACKGROUND\u0000Various pieces of evidence have shown that people who consume foods rich in polyphenolic and flavonoids compounds have a lower incidence of inflammatory, autoimmune diseases and cancer.\u0000\u0000\u0000OBJECTIVE\u0000The study aimed to review the most potent compounds that affect the immune response and diseases associated with it.\u0000\u0000\u0000METHODS\u0000Publications in PubMed and EmBase, from 1974-2018, and patents form Free patents online, Scifinder, Espacenet and Mendeley in which flavonoids, their semi-synthetic and synthetic derivatives are involved in immunosuppressive or immunostimulatory responses in vitro and in vivo.\u0000\u0000\u0000RESULTS\u0000In vitro, flavonoids and their derivatives inhibit various transcriptional factors, which modulate differentiation, proliferation, activation of immune cells and enhance regulatory T cell generation. Some flavonoids exert anti-inflammatory effects through: Blockade of NF-κB, and NLRP3 inflammasome, inhibition of pro-inflammatory cytokine production, IL-1β, IL-2, IL-6, TNF-α, IL-17A, down regulation of chemokines, and reduction of reactive oxygen and nitrogen species. Nevertheless, several reports have shown that some flavonoids enhance immune response by enhancing: oxygen and nitrogen radicals, antibody production, cytotoxic activity against tumours by increasing activating receptors and down regulating inhibitory receptors. In consequence, flavonoids may be potentially useful for treatment of infectious diseases and cancer.\u0000\u0000\u0000CONCLUSION\u0000The most potent flavonoids in inflammation that modify immune responses are apigenin, quercetin and Epigallocatechin-3-Gallate (EGCG) although, other compounds are still under study and cannot be excluded. The most relevant patents concerning the use of flavones and other polyphenols were revised. A promising future of these compounds in different therapies is discussed.","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":"13 2 1","pages":"84-104"},"PeriodicalIF":4.2,"publicationDate":"2019-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X13666190426164124","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48443044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 59
Meet Our Editorial Board Member 见见我们的编辑委员会成员
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-08-05 DOI: 10.2174/1872213x1301190626095210
P. Barnes
{"title":"Meet Our Editorial Board Member","authors":"P. Barnes","doi":"10.2174/1872213x1301190626095210","DOIUrl":"https://doi.org/10.2174/1872213x1301190626095210","url":null,"abstract":"","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":""},"PeriodicalIF":4.2,"publicationDate":"2019-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213x1301190626095210","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46619817","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Anti-Arthritic Effect of Garcinol Enriched Fraction Against Adjuvant Induced Arthritis. Garcinol富集部位对佐剂性关节炎的抗关节炎作用。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X12666181120091528
Purnima Warriar, Kalyani Barve, Bala Prabhakar

Background: Garcinia indica also known as kokum is used in traditional system of medicine for relieving inflammation and rheumatic pain. Garcinol, a benzophenone obtained from its fruit rind is reported to have anti-inflammatory effect via modulating arachidonic acid metabolism, suppressing iNOS expression, NF-κB activation and COX-2 expression. It has also been studied for antioxidant and anticancer activity. Apart from these, few patents claim that garcinol also has anti-obesity and hepatoprotective effect and has a potential to be used for the treatment of renal disorders, endometriosis and cardiac dysfunction.

Objective: Garcinol Enriched Fraction (GEF) from the fruit rind of Garcinia indica should be effective in the treatment of arthritis, one of the chronic inflammatory disorder owing to its anti-inflammatory property as indicated by earlier experiments.

Methods: GEF was prepared from the fruit rind of Garcinia indica and quantified using LC-MS/MS. It was found to contain 89.4% w/w of garcinol. GEF was evaluated at the dose of 10mg/kg for its efficacy against Complete Freund's Adjuvant (CFA) induced arthritis in Wistar albino rats. Paw volumes of both sides were measured by Plethysmometer and body weight was recorded on 0, 1, 5, 12 and 21st day. The hyperalgesic response was also measured by motility test and stair climbing test.

Results: GEF showed a significant reduction in paw swelling (p < 0.0001) and arthritis index (p < 0.0001) exhibiting anti-inflammatory potential. It also improves the motility and stair climbing ability of experimental animals (p < 0.05), thus reducing hyperalgesia.

Conclusion: Garcinol enriched fraction shows anti-arthritic activity in experimental animals.

背景:藤黄在传统医学系统中用于缓解炎症和风湿痛。Garcinol是一种从其果皮中提取的二苯甲酮,据报道通过调节花生四烯酸代谢、抑制iNOS表达、NF-κB活化和COX-2表达而具有抗炎作用。还研究了它的抗氧化和抗癌活性。除此之外,很少有专利声称garcinol还具有抗肥胖和保护肝脏的作用,并有可能用于治疗肾脏疾病、子宫内膜异位症和心功能障碍。目的:前期实验表明,从黄藤果皮提取的Garcinol富集部位(GEF)具有抗炎作用,可有效治疗慢性炎症性疾病之一的关节炎。方法:以藤黄果皮为原料制备GEF,采用LC-MS/MS进行定量分析。结果发现,它含有89.4% w/w的garcinol。以10mg/kg剂量评价GEF对Wistar白化大鼠完全弗氏佐剂(CFA)诱导的关节炎的疗效。分别于第0、1、5、12、21天用体积计测量双侧爪体积,并记录体重。用运动试验和爬楼梯试验测定痛觉过敏反应。结果:GEF显著降低足跖肿胀(p < 0.0001)和关节炎指数(p < 0.0001),具有抗炎作用。提高了实验动物的运动能力和爬楼梯能力(p < 0.05),减轻了痛觉过敏。结论:Garcinol富集部位对实验动物具有抗关节炎作用。
{"title":"Anti-Arthritic Effect of Garcinol Enriched Fraction Against Adjuvant Induced Arthritis.","authors":"Purnima Warriar,&nbsp;Kalyani Barve,&nbsp;Bala Prabhakar","doi":"10.2174/1872213X12666181120091528","DOIUrl":"https://doi.org/10.2174/1872213X12666181120091528","url":null,"abstract":"<p><strong>Background: </strong>Garcinia indica also known as kokum is used in traditional system of medicine for relieving inflammation and rheumatic pain. Garcinol, a benzophenone obtained from its fruit rind is reported to have anti-inflammatory effect via modulating arachidonic acid metabolism, suppressing iNOS expression, NF-κB activation and COX-2 expression. It has also been studied for antioxidant and anticancer activity. Apart from these, few patents claim that garcinol also has anti-obesity and hepatoprotective effect and has a potential to be used for the treatment of renal disorders, endometriosis and cardiac dysfunction.</p><p><strong>Objective: </strong>Garcinol Enriched Fraction (GEF) from the fruit rind of Garcinia indica should be effective in the treatment of arthritis, one of the chronic inflammatory disorder owing to its anti-inflammatory property as indicated by earlier experiments.</p><p><strong>Methods: </strong>GEF was prepared from the fruit rind of Garcinia indica and quantified using LC-MS/MS. It was found to contain 89.4% w/w of garcinol. GEF was evaluated at the dose of 10mg/kg for its efficacy against Complete Freund's Adjuvant (CFA) induced arthritis in Wistar albino rats. Paw volumes of both sides were measured by Plethysmometer and body weight was recorded on 0, 1, 5, 12 and 21st day. The hyperalgesic response was also measured by motility test and stair climbing test.</p><p><strong>Results: </strong>GEF showed a significant reduction in paw swelling (p < 0.0001) and arthritis index (p < 0.0001) exhibiting anti-inflammatory potential. It also improves the motility and stair climbing ability of experimental animals (p < 0.05), thus reducing hyperalgesia.</p><p><strong>Conclusion: </strong>Garcinol enriched fraction shows anti-arthritic activity in experimental animals.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":"49-56"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X12666181120091528","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36689487","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 13
Allergic Contact Dermatitis to Fentanyl TTS with Good Tolerance to Systemic Fentanyl. 芬太尼TTS过敏性接触性皮炎,对全身芬太尼有良好的耐受性。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X13666190527105718
Patricia Rojas-Pérez-Ezquerra, Sarah Micozzi, Ines Torrado-Español, Ana Rodríguez-Fernández, Vicente Albéndiz-Gutiérrez, Blanca Noguerado-Mellado

Background: Fentanyl is primarily an opioid agonist. It is frequently used in general anesthesia as a potent analgesic. It can be administered either orally, transdermally or systemically. Adverse effects due to opium alkaloids are usually because of a non-specific histamine release. Only in a few cases, a true allergy mechanism could be involved. Immediate reactions to opioids are most frequent than delayed reactions. In the past years, delayed reactions have increased in frequency because of the wide use of Transdermal Therapeutic System (TTS) with several opioids for its potent analgesic properties.

Objective: The objective was to study delayed reaction to fentanyl TTS and cross-reactivity with other opioids.

Methods: A 52-year-old man with a diagnosis of pancreatic cancer who began treatment for a bone metastases pain with fentanyl TTS, at a dose of 50 micrograms per hour (mcg/h) is the subject of the study. After 10-15 days of treatment, he developed an itchy papulovesicular rash in the application site of the fentanyl TTS. Afterward, eczema and superficial desquamation just on the application site of the patch were observed. He changed several times the site of application, but always developing the same symptoms in every single application. Later on, he tolerated other opioids such as oral morphine or tramadol. An allergy workout was performed. We performed Patch Tests (PT) with fentanyl at a concentration of 10% in aqua (aq) and with buprenorphine 10% aq., in order to investigate probable crossreactivity among other topical opioids.

Results: Readings were recorded at day 2 (D2) and day 4 (D4), with positive PT only with fentanyl at D2 (+++) and D4 (+++). We decided to perform a single-blind challenge test with buprenorphine 35 mcg/h in TTS, with a negative result. At this moment, fentanyl TTS was replaced by buprenorphine TTS, with good tolerance.

Conclusion: We present the case of Allergic Contact Dermatitis (ACD) due to hypersensitivity to fentanyl with good tolerance to buprenorphine. Positive PT in this patient suggests a type IV hypersensitivity mechanism. Allergic reactions to opioids are frequently immediate, but delayed reactions could appear, especially when the drug is administered topically.

背景:芬太尼主要是一种阿片类激动剂。它经常作为一种有效的止痛药用于全身麻醉。它可以口服、经皮或全身给药。由于鸦片生物碱的不良反应通常是由于非特异性组胺释放。只有在少数情况下,可能涉及真正的过敏机制。对阿片类药物的即时反应比延迟反应更常见。在过去的几年里,由于广泛使用透皮治疗系统(TTS)和几种阿片类药物的有效镇痛特性,延迟反应的频率增加。目的:研究芬太尼TTS的延迟反应及与其他阿片类药物的交叉反应性。方法:一名诊断为胰腺癌的52岁男性患者开始使用芬太尼TTS治疗骨转移性疼痛,剂量为50微克/小时(mcg/h)。治疗10-15天后,芬太尼TTS应用部位出现瘙痒丘疹。随后,仅在贴敷部位观察到湿疹和浅表脱屑。他多次更换涂抹部位,但每次涂抹都出现同样的症状。后来,他耐受了其他阿片类药物,如口服吗啡或曲马多。进行过敏训练。我们用浓度为10%的芬太尼和浓度为10%的丁丙诺啡进行了斑贴试验(PT),以调查其他局部阿片类药物可能的交叉反应性。结果:在第2天(D2)和第4天(D4)记录读数,仅芬太尼在D2(+++)和D4(+++)时呈阳性。我们决定在TTS中使用丁丙诺啡35 mcg/h进行单盲激发试验,结果为阴性。此时,芬太尼TTS被丁丙诺啡TTS取代,耐受性良好。结论:我们报告一例因芬太尼过敏引起的过敏性接触性皮炎(ACD),对丁丙诺啡耐受性良好。该患者PT阳性提示IV型超敏反应机制。对阿片类药物的过敏反应通常是立即的,但可能出现延迟反应,特别是当药物局部施用时。
{"title":"Allergic Contact Dermatitis to Fentanyl TTS with Good Tolerance to Systemic Fentanyl.","authors":"Patricia Rojas-Pérez-Ezquerra,&nbsp;Sarah Micozzi,&nbsp;Ines Torrado-Español,&nbsp;Ana Rodríguez-Fernández,&nbsp;Vicente Albéndiz-Gutiérrez,&nbsp;Blanca Noguerado-Mellado","doi":"10.2174/1872213X13666190527105718","DOIUrl":"https://doi.org/10.2174/1872213X13666190527105718","url":null,"abstract":"<p><strong>Background: </strong>Fentanyl is primarily an opioid agonist. It is frequently used in general anesthesia as a potent analgesic. It can be administered either orally, transdermally or systemically. Adverse effects due to opium alkaloids are usually because of a non-specific histamine release. Only in a few cases, a true allergy mechanism could be involved. Immediate reactions to opioids are most frequent than delayed reactions. In the past years, delayed reactions have increased in frequency because of the wide use of Transdermal Therapeutic System (TTS) with several opioids for its potent analgesic properties.</p><p><strong>Objective: </strong>The objective was to study delayed reaction to fentanyl TTS and cross-reactivity with other opioids.</p><p><strong>Methods: </strong>A 52-year-old man with a diagnosis of pancreatic cancer who began treatment for a bone metastases pain with fentanyl TTS, at a dose of 50 micrograms per hour (mcg/h) is the subject of the study. After 10-15 days of treatment, he developed an itchy papulovesicular rash in the application site of the fentanyl TTS. Afterward, eczema and superficial desquamation just on the application site of the patch were observed. He changed several times the site of application, but always developing the same symptoms in every single application. Later on, he tolerated other opioids such as oral morphine or tramadol. An allergy workout was performed. We performed Patch Tests (PT) with fentanyl at a concentration of 10% in aqua (aq) and with buprenorphine 10% aq., in order to investigate probable crossreactivity among other topical opioids.</p><p><strong>Results: </strong>Readings were recorded at day 2 (D2) and day 4 (D4), with positive PT only with fentanyl at D2 (+++) and D4 (+++). We decided to perform a single-blind challenge test with buprenorphine 35 mcg/h in TTS, with a negative result. At this moment, fentanyl TTS was replaced by buprenorphine TTS, with good tolerance.</p><p><strong>Conclusion: </strong>We present the case of Allergic Contact Dermatitis (ACD) due to hypersensitivity to fentanyl with good tolerance to buprenorphine. Positive PT in this patient suggests a type IV hypersensitivity mechanism. Allergic reactions to opioids are frequently immediate, but delayed reactions could appear, especially when the drug is administered topically.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":"66-68"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X13666190527105718","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37279580","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Probing into Therapeutic Anti-cancer Potential of Apigenin: Recent Trends and Future Directions. 芹菜素抗癌治疗潜力的研究进展及展望。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X13666190816160240
Ajay Sharma, Abdul Ghani, K. Sak, H. Tuli, A. Sharma, W. Setzer, Sanjeev Sharma, A. Das
BACKGROUND Natural products represent a therapeutic charm for the treatment of inflammation-associated diseases. Flavonoids which are one of the special categories of such natural products, have previously shown promising therapeutic potential. OBJECTIVES The current review discusses about the synthetic preview and anti-inflammatory potential of apigenin along with the underlying molecular mechanism in chronic human diseases especially cancer. In addition, the relevant patents on therapeutic potential of apigenin have also been mentioned. METHODS Literature search was carried out using PubMed/Science, Google Scholar etc. which was further expended by the different combination of keywords: apigenin, inflammation, mechanism,therapeutic potential, cancer etc. Patent information was retrieved by searching the key terms: apigenin, inflammation, therapeutic potential from various databanks including Espacenet, Google patents, freepatent online and mendeley of WIPO, USPTO, SIPO, JPO, KIPO and EPO databases. CONCLUSION Studies related to the anti-inflammatory and anticancer potential of apigenin have been explored through this review article. Moreover, the patent analysis of apigenin has further strengthened its therapeutic role. Probing into the therapeutic properties of apigenin, further add value to this molecule in terms of its down regulation of major inflammatory and cancer associated signaling pathways. The article simultaneously would assist the scientific community to precisely understand the role of apigenin and design novel anti-cancer therapies.
背景:天然产品代表了治疗炎症相关疾病的治疗魅力。黄酮类化合物是这类天然产物的特殊类别之一,此前已显示出良好的治疗潜力。目的综述芹菜素的合成前景、抗炎作用及其在人类慢性疾病特别是癌症中的分子机制。此外,还介绍了芹菜素治疗潜力的相关专利。方法通过PubMed/Science、谷歌Scholar等进行文献检索,并以芹菜素、炎症、机制、治疗潜力、肿瘤等关键词的不同组合进行扩展。通过检索WIPO、USPTO、SIPO、JPO、KIPO和EPO数据库的Espacenet、谷歌专利、freepent online和mendeley等数据库的关键词:芹菜素、炎症、治疗潜力等专利信息。结论本文对芹菜素抗炎和抗癌作用的相关研究进行了综述。此外,芹菜素的专利分析进一步加强了其治疗作用。探索芹菜素的治疗特性,进一步增加该分子在下调主要炎症和癌症相关信号通路方面的价值。同时,这篇文章将帮助科学界准确理解芹菜素的作用,并设计新的抗癌疗法。
{"title":"Probing into Therapeutic Anti-cancer Potential of Apigenin: Recent Trends and Future Directions.","authors":"Ajay Sharma, Abdul Ghani, K. Sak, H. Tuli, A. Sharma, W. Setzer, Sanjeev Sharma, A. Das","doi":"10.2174/1872213X13666190816160240","DOIUrl":"https://doi.org/10.2174/1872213X13666190816160240","url":null,"abstract":"BACKGROUND Natural products represent a therapeutic charm for the treatment of inflammation-associated diseases. Flavonoids which are one of the special categories of such natural products, have previously shown promising therapeutic potential. OBJECTIVES The current review discusses about the synthetic preview and anti-inflammatory potential of apigenin along with the underlying molecular mechanism in chronic human diseases especially cancer. In addition, the relevant patents on therapeutic potential of apigenin have also been mentioned. METHODS Literature search was carried out using PubMed/Science, Google Scholar etc. which was further expended by the different combination of keywords: apigenin, inflammation, mechanism,therapeutic potential, cancer etc. Patent information was retrieved by searching the key terms: apigenin, inflammation, therapeutic potential from various databanks including Espacenet, Google patents, freepatent online and mendeley of WIPO, USPTO, SIPO, JPO, KIPO and EPO databases. CONCLUSION Studies related to the anti-inflammatory and anticancer potential of apigenin have been explored through this review article. Moreover, the patent analysis of apigenin has further strengthened its therapeutic role. Probing into the therapeutic properties of apigenin, further add value to this molecule in terms of its down regulation of major inflammatory and cancer associated signaling pathways. The article simultaneously would assist the scientific community to precisely understand the role of apigenin and design novel anti-cancer therapies.","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":"1 1","pages":""},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X13666190816160240","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68048644","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 25
Molecular Allergy Diagnostics as an Adjunct to Conventional Diagnostics in a Secondary Pediatric Referral Center. 分子过敏诊断作为辅助常规诊断在二级儿科转诊中心。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X13666190610143439
Ole D Wolthers

Background: Several compositions for determination of specific molecular components in allergens have recently been patented. The role of Molecular Allergy (MA) diagnostics in suspected IgE mediated allergic conditions is currently debated. Guideline reports have concluded that population- based studies involving evaluation of the usefulness of MA diagnostics are needed.

Objective: To evaluate the usefulness of MA diagnostics in a secondary pediatric referral center.

Methods: A total of 961 children and adolescents aged 0.2-18.8 (mean 7.0) years was included in a prospective observational survey. Inclusion criterion was a suspected diagnosis of an IgE mediated condition based on history and clinical symptoms and signs. If a specific diagnosis could not be reached from conventional investigations suspected peanut allergy, birch pollen allergy and associated crossreactivity, insect allergy and triggering allergens for specific immunotherapy were assessed by MA diagnostics.

Results: Based on conventional work-up a diagnostic conclusion was established in 946 patients (98.4%). MA diagnostics were performed in 15 individuals (1.6%), 7 girls and 8 boys aged 3.2 to 17.8 (mean 10.6) years. In 8 cases a specific diagnosis was established based on MA diagnostics; in 7 cases MA diagnostics could not improve diagnosis. MA were most frequently (N = 7 (14%)) used in children with peanut allergy (N = 50).

Conclusion: Most patients in a secondary pediatric referral center with suspected IgE mediated allergy can be managed by conventional diagnostic methods. MA diagnostics may be useful in small and selected subgroups as in patients with suspected peanut allergy, however, may not be helpful in all cases.

背景:几种用于测定过敏原中特定分子成分的组合物最近获得了专利。分子过敏(MA)诊断在疑似IgE介导的过敏条件中的作用目前存在争议。指南报告的结论是,有必要开展以人群为基础的研究,评估MA诊断的有效性。目的:评价二级儿科转诊中心MA诊断的有效性。方法:对961名年龄在0.2-18.8岁(平均7.0岁)的儿童和青少年进行前瞻性观察性调查。纳入标准是基于病史和临床症状和体征的疑似IgE介导疾病的诊断。如果常规调查无法得出特异性诊断,则采用MA诊断评估特异性免疫治疗的疑似花生过敏、桦木花粉过敏及相关交叉反应、昆虫过敏和触发过敏原。结果:946例患者(98.4%)在常规检查的基础上得出诊断结论。15人(1.6%)进行了MA诊断,7名女孩和8名男孩,年龄为3.2至17.8岁(平均10.6岁)。在8例中,基于MA诊断建立了特定的诊断;7例MA诊断不能提高诊断。花生过敏儿童(N = 50)最常使用MA (N = 7(14%))。结论:在二级儿科转诊中心,大多数疑似IgE介导的过敏患者可以通过常规诊断方法进行治疗。MA诊断可能对小的和选定的亚组有用,如疑似花生过敏的患者,然而,可能不是对所有病例都有帮助。
{"title":"Molecular Allergy Diagnostics as an Adjunct to Conventional Diagnostics in a Secondary Pediatric Referral Center.","authors":"Ole D Wolthers","doi":"10.2174/1872213X13666190610143439","DOIUrl":"https://doi.org/10.2174/1872213X13666190610143439","url":null,"abstract":"<p><strong>Background: </strong>Several compositions for determination of specific molecular components in allergens have recently been patented. The role of Molecular Allergy (MA) diagnostics in suspected IgE mediated allergic conditions is currently debated. Guideline reports have concluded that population- based studies involving evaluation of the usefulness of MA diagnostics are needed.</p><p><strong>Objective: </strong>To evaluate the usefulness of MA diagnostics in a secondary pediatric referral center.</p><p><strong>Methods: </strong>A total of 961 children and adolescents aged 0.2-18.8 (mean 7.0) years was included in a prospective observational survey. Inclusion criterion was a suspected diagnosis of an IgE mediated condition based on history and clinical symptoms and signs. If a specific diagnosis could not be reached from conventional investigations suspected peanut allergy, birch pollen allergy and associated crossreactivity, insect allergy and triggering allergens for specific immunotherapy were assessed by MA diagnostics.</p><p><strong>Results: </strong>Based on conventional work-up a diagnostic conclusion was established in 946 patients (98.4%). MA diagnostics were performed in 15 individuals (1.6%), 7 girls and 8 boys aged 3.2 to 17.8 (mean 10.6) years. In 8 cases a specific diagnosis was established based on MA diagnostics; in 7 cases MA diagnostics could not improve diagnosis. MA were most frequently (N = 7 (14%)) used in children with peanut allergy (N = 50).</p><p><strong>Conclusion: </strong>Most patients in a secondary pediatric referral center with suspected IgE mediated allergy can be managed by conventional diagnostic methods. MA diagnostics may be useful in small and selected subgroups as in patients with suspected peanut allergy, however, may not be helpful in all cases.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":"73-76"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X13666190610143439","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37059515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Urinary Tract Infection in Children. 儿童尿路感染
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X13666181228154940
Alexander K C Leung, Alex H C Wong, Amy A M Leung, Kam L Hon

Background: Urinary Tract Infection (UTI) is a common infection in children. Prompt diagnosis and appropriate treatment are very important to reduce the morbidity associated with this condition.

Objective: To provide an update on the evaluation, diagnosis, and treatment of urinary tract infection in children.

Methods: A PubMed search was completed in clinical queries using the key terms "urinary tract infection", "pyelonephritis" OR "cystitis". The search strategy included meta-analyses, randomized controlled trials, clinical trials, observational studies, and reviews. The search was restricted to English literature and the pediatric age group. Patents were searched using the key terms "urinary tract infection" "pyelonephritis" OR "cystitis" from www.google.com/patents, http://espacenet.com, and www.freepatentsonline.com.

Results: Escherichia coli accounts for 80 to 90% of UTI in children. The symptoms and signs are nonspecific throughout infancy. Unexplained fever is the most common symptom of UTI during the first two years of life. After the second year of life, symptoms and signs of pyelonephritis include fever, chills, rigor, flank pain, and costovertebral angle tenderness. Lower tract symptoms and signs include suprapubic pain, dysuria, urinary frequency, urgency, cloudy urine, malodorous urine, and suprapubic tenderness. A urinalysis and urine culture should be performed when UTI is suspected. In the work-up of children with UTI, physicians must judiciously utilize imaging studies to minimize exposure of children to radiation. While waiting for the culture results, prompt antibiotic therapy is indicated for symptomatic UTI based on clinical findings and positive urinalysis to eradicate the infection and improve clinical outcome. The choice of antibiotics should take into consideration local data on antibiotic resistance patterns. Recent patents related to the management of UTI are discussed.

Conclusion: Currently, a second or third generation cephalosporin and amoxicillin-clavulanate are drugs of choice in the treatment of acute uncomplicated UTI. Parenteral antibiotic therapy is recommended for infants ≤ 2 months and any child who is toxic-looking, hemodynamically unstable, immunocompromised, unable to tolerate oral medication, or not responding to oral medication. A combination of intravenous ampicillin and intravenous/intramuscular gentamycin or a third-generation cephalosporin can be used in those situations. Routine antimicrobial prophylaxis is rarely justified, but continuous antimicrobial prophylaxis should be considered for children with frequent febrile UTI.

背景:尿路感染(UTI)是一种常见的儿童感染。及时诊断和适当治疗对降低该病的发病率非常重要:提供有关儿童尿路感染的评估、诊断和治疗的最新信息:方法:使用关键词 "尿路感染"、"肾盂肾炎 "或 "膀胱炎 "在PubMed上进行临床检索。搜索策略包括荟萃分析、随机对照试验、临床试验、观察性研究和综述。检索仅限于英文文献和儿科年龄组。在 www.google.com/patents、http://espacenet.com 和 www.freepatentsonline.com.Results 中使用关键词 "尿路感染"、"肾盂肾炎 "或 "膀胱炎 "检索专利:大肠杆菌占儿童尿路感染的 80% 至 90%。整个婴儿期的症状和体征都是非特异性的。不明原因的发烧是出生后头两年尿毒症最常见的症状。出生后第二年,肾盂肾炎的症状和体征包括发热、寒战、僵硬、侧腹疼痛和肋脊角压痛。下尿路症状和体征包括耻骨上疼痛、排尿困难、尿频、尿急、尿液混浊、尿液恶臭和耻骨上压痛。怀疑患上尿道炎时,应进行尿液分析和尿液培养。在对患有尿道炎的儿童进行检查时,医生必须明智地使用影像学检查,以尽量减少儿童受到的辐射。在等待培养结果期间,应根据临床发现和阳性尿液分析结果对有症状的 UTI 患者及时使用抗生素治疗,以根除感染并改善临床疗效。选择抗生素时应考虑当地的抗生素耐药性模式数据。本文讨论了与UTI治疗相关的最新专利:目前,第二代或第三代头孢菌素和阿莫西林-克拉维酸是治疗急性无并发症UTI的首选药物。对于≤2 个月的婴儿和任何面色发黄、血流动力学不稳定、免疫力低下、不能耐受口服药物或对口服药物无反应的患儿,建议使用肠外抗生素治疗。在这些情况下,可联合使用静脉注射氨苄西林和静脉注射/肌肉注射庆大霉素或第三代头孢菌素。常规的抗菌药物预防很少是合理的,但对于频繁发生发热性尿毒症的儿童,应考虑持续使用抗菌药物预防。
{"title":"Urinary Tract Infection in Children.","authors":"Alexander K C Leung, Alex H C Wong, Amy A M Leung, Kam L Hon","doi":"10.2174/1872213X13666181228154940","DOIUrl":"10.2174/1872213X13666181228154940","url":null,"abstract":"<p><strong>Background: </strong>Urinary Tract Infection (UTI) is a common infection in children. Prompt diagnosis and appropriate treatment are very important to reduce the morbidity associated with this condition.</p><p><strong>Objective: </strong>To provide an update on the evaluation, diagnosis, and treatment of urinary tract infection in children.</p><p><strong>Methods: </strong>A PubMed search was completed in clinical queries using the key terms \"urinary tract infection\", \"pyelonephritis\" OR \"cystitis\". The search strategy included meta-analyses, randomized controlled trials, clinical trials, observational studies, and reviews. The search was restricted to English literature and the pediatric age group. Patents were searched using the key terms \"urinary tract infection\" \"pyelonephritis\" OR \"cystitis\" from www.google.com/patents, http://espacenet.com, and www.freepatentsonline.com.</p><p><strong>Results: </strong>Escherichia coli accounts for 80 to 90% of UTI in children. The symptoms and signs are nonspecific throughout infancy. Unexplained fever is the most common symptom of UTI during the first two years of life. After the second year of life, symptoms and signs of pyelonephritis include fever, chills, rigor, flank pain, and costovertebral angle tenderness. Lower tract symptoms and signs include suprapubic pain, dysuria, urinary frequency, urgency, cloudy urine, malodorous urine, and suprapubic tenderness. A urinalysis and urine culture should be performed when UTI is suspected. In the work-up of children with UTI, physicians must judiciously utilize imaging studies to minimize exposure of children to radiation. While waiting for the culture results, prompt antibiotic therapy is indicated for symptomatic UTI based on clinical findings and positive urinalysis to eradicate the infection and improve clinical outcome. The choice of antibiotics should take into consideration local data on antibiotic resistance patterns. Recent patents related to the management of UTI are discussed.</p><p><strong>Conclusion: </strong>Currently, a second or third generation cephalosporin and amoxicillin-clavulanate are drugs of choice in the treatment of acute uncomplicated UTI. Parenteral antibiotic therapy is recommended for infants ≤ 2 months and any child who is toxic-looking, hemodynamically unstable, immunocompromised, unable to tolerate oral medication, or not responding to oral medication. A combination of intravenous ampicillin and intravenous/intramuscular gentamycin or a third-generation cephalosporin can be used in those situations. Routine antimicrobial prophylaxis is rarely justified, but continuous antimicrobial prophylaxis should be considered for children with frequent febrile UTI.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":"2-18"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/03/2a/RPIAD-13-2.PMC6751349.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36819348","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ferulic Acid: A Promising Therapeutic Phytochemical and Recent Patents Advances. 阿魏酸:一种很有前途的治疗植物化学物质及最新专利进展。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X13666190621125048
Ashun Chaudhary, Vivek S Jaswal, Sonika Choudhary, Sonika, Ajay Sharma, Vikas Beniwal, Hardeep S Tuli, Sanjeev Sharma

Background: Among the various phenolics metabolites, ferulic acid is considered as the promising mitigating, restorative and antioxidant agent. Ferulic acid is one of the most commonly found natural products in vegetables, for example, tomatoes, sweet corn, and in rice grain. Phytochemicals are utilized in the treatment of human ailments and these are derived from the dietary compounds.

Objective: The present review widely argued the calming restorative capability of ferulic acid alongside the scientific evidences and its proposed mechanism for activity. Furthermore, we provided the main practical points for the use of ferulic acid in oxidative damages during various diseases. Additionally, the relevant patents on ferulic acid with various therapeutic potential has been discussed.

Methods: The approach consisted of searching several resources, including theses, technical reports, web-based scientific databases such as publications on PubMed, ScienceDirect, Springer, PROTA, Google Scholar, and other allied databases. Thus, recent patent regarding the role of ferulic acid therapeutic potenitial has been discussed.

Results: One hundred and twenty references have been cited in the present review article. The cited references were found to be suitable and described the therapeutic application of ferulic acid thoroughly.

Conclusion: Ferulic acids are known to contrarily down-manage an assortment of extracellular and intrcelullular molecular targets related to infection movement. Various patents on ferulic acid based moieties have been accounted for from 2018. The ferulic acids have a wide scope of impacts against different infections like malignant growth, diabetes, cardiovascular and neurodegenerative diseases. The current review deals with the antioxidant property of ferulic acid and the recent patent describes the role of ferulic acid against human diseases.

背景:在各种酚类代谢产物中,阿魏酸被认为是一种很有前途的缓解、恢复和抗氧化剂。阿魏酸是蔬菜中最常见的天然产物之一,例如西红柿、甜玉米和稻谷。植物化学物质用于治疗人类疾病,这些物质来源于膳食化合物。目的:综述阿魏酸的镇静恢复作用及其作用机制。此外,我们还提供了阿魏酸在各种疾病中氧化损伤的应用的主要实用要点。此外,还讨论了具有各种治疗潜力的阿魏酸的相关专利。方法:该方法包括搜索多种资源,包括论文、技术报告、基于网络的科学数据库,如PubMed、ScienceDirect、Springer、PROTA、Google Scholar和其他相关数据库。因此,最近的专利关于阿魏酸的治疗潜力的作用进行了讨论。结果:共引用文献120篇。发现所引用的文献均属合适,并对阿魏酸的治疗应用作了较为全面的描述。结论:阿魏酸与感染运动相关的细胞外和细胞内分子靶标具有相反的抑制作用。从2018年起,阿魏酸基部分的各种专利已被计算在内。阿魏酸对不同的感染有广泛的影响,如恶性生长、糖尿病、心血管和神经退行性疾病。本文综述了阿魏酸的抗氧化性能,最近的专利描述了阿魏酸对人类疾病的作用。
{"title":"Ferulic Acid: A Promising Therapeutic Phytochemical and Recent Patents Advances.","authors":"Ashun Chaudhary,&nbsp;Vivek S Jaswal,&nbsp;Sonika Choudhary,&nbsp;Sonika,&nbsp;Ajay Sharma,&nbsp;Vikas Beniwal,&nbsp;Hardeep S Tuli,&nbsp;Sanjeev Sharma","doi":"10.2174/1872213X13666190621125048","DOIUrl":"https://doi.org/10.2174/1872213X13666190621125048","url":null,"abstract":"<p><strong>Background: </strong>Among the various phenolics metabolites, ferulic acid is considered as the promising mitigating, restorative and antioxidant agent. Ferulic acid is one of the most commonly found natural products in vegetables, for example, tomatoes, sweet corn, and in rice grain. Phytochemicals are utilized in the treatment of human ailments and these are derived from the dietary compounds.</p><p><strong>Objective: </strong>The present review widely argued the calming restorative capability of ferulic acid alongside the scientific evidences and its proposed mechanism for activity. Furthermore, we provided the main practical points for the use of ferulic acid in oxidative damages during various diseases. Additionally, the relevant patents on ferulic acid with various therapeutic potential has been discussed.</p><p><strong>Methods: </strong>The approach consisted of searching several resources, including theses, technical reports, web-based scientific databases such as publications on PubMed, ScienceDirect, Springer, PROTA, Google Scholar, and other allied databases. Thus, recent patent regarding the role of ferulic acid therapeutic potenitial has been discussed.</p><p><strong>Results: </strong>One hundred and twenty references have been cited in the present review article. The cited references were found to be suitable and described the therapeutic application of ferulic acid thoroughly.</p><p><strong>Conclusion: </strong>Ferulic acids are known to contrarily down-manage an assortment of extracellular and intrcelullular molecular targets related to infection movement. Various patents on ferulic acid based moieties have been accounted for from 2018. The ferulic acids have a wide scope of impacts against different infections like malignant growth, diabetes, cardiovascular and neurodegenerative diseases. The current review deals with the antioxidant property of ferulic acid and the recent patent describes the role of ferulic acid against human diseases.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":"13 2","pages":"115-123"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X13666190621125048","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37354386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 73
The Inhibitory Role of M2000 (β-D-Mannuronic Acid) on Expression of Toll-like Receptor 2 and 4 in HT29 Cell Line. M2000对HT29细胞Toll样受体2和4表达的抑制作用。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X13666181211160238
Laleh Sharifi, Mona Moshiri, Mohammad M S Dallal, Mohammad H Asgardoon, Maryam Nourizadeh, Saied Bokaie, Abbas Mirshafiey

Background/objectives: Anti-inflammatory agents play a crucial role in controlling inflammatory diseases such as Inflammatory Bowel Disease (IBD) but their use is restricted due to their vast side effects. M2000 (β-D-mannuronic acid) is a new immunomodulatory drug. According to the capacity of M2000 in suppressing some molecules involved in Toll Like Receptors (TLRs) signaling and reducing oxidative stress we hypothesize that, this molecule may have a potential role in decreasing inflammatory responses in IBD. The aim of this study was to evaluate the cytotoxicity of M2000 and its effect on the gene expression of TLR2 and TLR4.

Methods: HEK293 cell line was grown and divided into 96-well cell plate and MTT assay was performed. HT29 cells were cultured and treated with low and high doses of M2000. Total RNA was extracted and cDNA synthesized and quantitative real-time PCR was done to quantify the TLR2 and TLR4 mRNA expression.

Results: We found that M2000 at the concentration of ≤ 1000µg/ml had no obvious cytotoxicity effect on the HEK293 cells. Also, low and high doses of M2000 could significantly down-regulate both TLR2 and TLR4 mRNA expression. Moreover, a significant reduction in gene expression of TLR2 and TLR4 in an inflammatory condition resulted in high doses of M2000 in the presence of LPS.

Conclusion: Our study which was conducted in colonic epithelial cell model, shows that M2000 can be considered as a new anti-inflammatory agent in IBD. However, more comprehensive experimental and clinical studies are required to recognize the molecular mechanism of M2000 and also its safety and efficacy.

背景/目的:抗炎药在控制炎症性肠病(IBD)等炎症性疾病方面发挥着至关重要的作用,但由于其巨大的副作用,其使用受到限制。M2000(β-D-甘露糖醛酸)是一种新型的免疫调节药物。根据M2000在抑制Toll样受体(TLRs)信号传导和减少氧化应激中的一些分子方面的能力,我们假设该分子可能在减少IBD的炎症反应中发挥潜在作用。本研究旨在评价M2000的细胞毒性及其对TLR2和TLR4基因表达的影响。培养HT29细胞并用低剂量和高剂量的M2000处理。提取总RNA并合成cDNA,并进行定量实时PCR以定量TLR2和TLR4的mRNA表达。结果:M2000在≤1000µg/ml浓度下对HEK293细胞无明显的细胞毒性作用。此外,低剂量和高剂量的M2000可以显著下调TLR2和TLR4 mRNA的表达。此外,炎症条件下TLR2和TLR4基因表达的显著降低导致在LPS存在下高剂量的M2000。结论:我们在结肠上皮细胞模型中进行的研究表明,M2000可以被认为是一种新的IBD抗炎剂。然而,需要更全面的实验和临床研究来认识M2000的分子机制及其安全性和有效性。
{"title":"The Inhibitory Role of M2000 (β-D-Mannuronic Acid) on Expression of Toll-like Receptor 2 and 4 in HT29 Cell Line.","authors":"Laleh Sharifi,&nbsp;Mona Moshiri,&nbsp;Mohammad M S Dallal,&nbsp;Mohammad H Asgardoon,&nbsp;Maryam Nourizadeh,&nbsp;Saied Bokaie,&nbsp;Abbas Mirshafiey","doi":"10.2174/1872213X13666181211160238","DOIUrl":"10.2174/1872213X13666181211160238","url":null,"abstract":"<p><strong>Background/objectives: </strong>Anti-inflammatory agents play a crucial role in controlling inflammatory diseases such as Inflammatory Bowel Disease (IBD) but their use is restricted due to their vast side effects. M2000 (β-D-mannuronic acid) is a new immunomodulatory drug. According to the capacity of M2000 in suppressing some molecules involved in Toll Like Receptors (TLRs) signaling and reducing oxidative stress we hypothesize that, this molecule may have a potential role in decreasing inflammatory responses in IBD. The aim of this study was to evaluate the cytotoxicity of M2000 and its effect on the gene expression of TLR2 and TLR4.</p><p><strong>Methods: </strong>HEK293 cell line was grown and divided into 96-well cell plate and MTT assay was performed. HT29 cells were cultured and treated with low and high doses of M2000. Total RNA was extracted and cDNA synthesized and quantitative real-time PCR was done to quantify the TLR2 and TLR4 mRNA expression.</p><p><strong>Results: </strong>We found that M2000 at the concentration of ≤ 1000µg/ml had no obvious cytotoxicity effect on the HEK293 cells. Also, low and high doses of M2000 could significantly down-regulate both TLR2 and TLR4 mRNA expression. Moreover, a significant reduction in gene expression of TLR2 and TLR4 in an inflammatory condition resulted in high doses of M2000 in the presence of LPS.</p><p><strong>Conclusion: </strong>Our study which was conducted in colonic epithelial cell model, shows that M2000 can be considered as a new anti-inflammatory agent in IBD. However, more comprehensive experimental and clinical studies are required to recognize the molecular mechanism of M2000 and also its safety and efficacy.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":"57-65"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X13666181211160238","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36773612","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Inhaled Biologicals for the Treatment of Cystic Fibrosis. 治疗囊性纤维化的吸入生物制剂。
IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2019-01-01 DOI: 10.2174/1872213X12666181012101444
Valentina Sala, Alessandra Murabito, Alessandra Ghigo

Background: Cystic Fibrosis (CF), one of the most frequent genetic diseases, is characterized by the production of viscous mucus in several organs. In the lungs, mucus clogs the airways and traps bacteria, leading to recurrent/resistant infections and lung damage. For cystic fibrosis patients, respiratory failure is still lethal in early adulthood since available treatments display incomplete efficacy.

Objective: The objective of this review is to extend the current knowledge in the field of available treatments for cystic fibrosis. A special focus has been given to inhaled peptide-based drugs.

Methods: The current review is based on recent and/or relevant literature and patents already available in various scientific databases, which include PubMed, PubMed Central, Patentscope and Science Direct. The information obtained through these diverse databases is compiled, critically interpreted and presented in the current study. An in-depth but not systematic approach to the specific research question has been adopted.

Results: Recently, peptides have been proposed as possible pharmacologic agents for the treatment of respiratory diseases. Of note, peptides are suitable to be administered by inhalation to maximize efficacy and reduce systemic side effects. Moreover, innovative delivery carriers have been developed for drug administration through inhalation, allowing not only protection against proteolysis, but also a prolonged and controlled release.

Conclusion: Here, we summarize newly patented peptides that have been developed in the last few years and advanced technologies for inhaled drug delivery to treat cystic fibrosis.

背景:囊性纤维化(CF)是最常见的遗传性疾病之一,其特征是在几个器官中产生粘稠的粘液。在肺部,黏液堵塞气道并捕获细菌,导致复发性/耐药性感染和肺部损伤。对于囊性纤维化患者,呼吸衰竭在成年早期仍然是致命的,因为现有的治疗方法显示不完全有效。目的:本综述的目的是扩展目前在囊性纤维化可用治疗领域的知识。特别关注的是吸入肽类药物。方法:本综述基于各种科学数据库中已经存在的最新和/或相关文献和专利,包括PubMed、PubMed Central、Patentscope和Science Direct。通过这些不同的数据库获得的信息被编译,批判性地解释并呈现在当前的研究中。对具体的研究问题采用了深入但不系统的方法。结果:近年来,多肽被认为是治疗呼吸系统疾病的潜在药物。值得注意的是,多肽适合通过吸入给药,以最大限度地提高疗效并减少全身副作用。此外,通过吸入给药的创新递送载体已经开发出来,不仅可以防止蛋白质水解,还可以延长和控制释放。结论:在这里,我们总结了近年来开发的新专利肽和吸入给药治疗囊性纤维化的先进技术。
{"title":"Inhaled Biologicals for the Treatment of Cystic Fibrosis.","authors":"Valentina Sala,&nbsp;Alessandra Murabito,&nbsp;Alessandra Ghigo","doi":"10.2174/1872213X12666181012101444","DOIUrl":"https://doi.org/10.2174/1872213X12666181012101444","url":null,"abstract":"<p><strong>Background: </strong>Cystic Fibrosis (CF), one of the most frequent genetic diseases, is characterized by the production of viscous mucus in several organs. In the lungs, mucus clogs the airways and traps bacteria, leading to recurrent/resistant infections and lung damage. For cystic fibrosis patients, respiratory failure is still lethal in early adulthood since available treatments display incomplete efficacy.</p><p><strong>Objective: </strong>The objective of this review is to extend the current knowledge in the field of available treatments for cystic fibrosis. A special focus has been given to inhaled peptide-based drugs.</p><p><strong>Methods: </strong>The current review is based on recent and/or relevant literature and patents already available in various scientific databases, which include PubMed, PubMed Central, Patentscope and Science Direct. The information obtained through these diverse databases is compiled, critically interpreted and presented in the current study. An in-depth but not systematic approach to the specific research question has been adopted.</p><p><strong>Results: </strong>Recently, peptides have been proposed as possible pharmacologic agents for the treatment of respiratory diseases. Of note, peptides are suitable to be administered by inhalation to maximize efficacy and reduce systemic side effects. Moreover, innovative delivery carriers have been developed for drug administration through inhalation, allowing not only protection against proteolysis, but also a prolonged and controlled release.</p><p><strong>Conclusion: </strong>Here, we summarize newly patented peptides that have been developed in the last few years and advanced technologies for inhaled drug delivery to treat cystic fibrosis.</p>","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":" ","pages":"19-26"},"PeriodicalIF":4.2,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1872213X12666181012101444","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36583072","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 9
期刊
Recent patents on inflammation & allergy drug discovery
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1