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Discovery of natural inhibitors for osteoarthritis targeting inflammatory pathway with pharmacoinformatics and molecular docking 基于药物信息学和分子对接的骨关节炎炎症通路天然抑制剂的发现
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-10 DOI: 10.1007/s13596-024-00782-x
Rok Su Shim, Fahad Hassan Shah, Young Seok Eom, Saad Salman, Song Ja Kim

Ziziphus jujuba is a traditional Chinese medicinal plant, whose fruit (Jujubae fructus) has been highly utilized in herbal medicine for decades. The fruit of this plant contains a wide variety of phytochemicals having efficacious biological activity. These phytochemicals have been utilized in this study to discover potential drug candidates in preventing osteoarthritis (OA) progression using network pharmacology and molecular docking method. The phytochemicals information of Jujubae fructus was obtained from the TCMSP database, which were screened for druglikeness and oral bioavailability. Screened compounds were explored for Network pharmacology using BATMAN-TCM database and Molecular Docking with IGEMDOCK 2.1. Obtained compounds from this analysis were used to predict their ADMET properties. Network pharmacology analysis showed that Mairin, Oleanonic acid, Oleanolic acid, and Stigmasterol reduce inflammation and activate Peroxisome Proliferator-Activated Receptors (PPARs) signaling pathway to intervene with OA progression. Molecular docking predicted that Mairin, Oleanonic acid, and Stigmasterol reduce inflammation by targeting Janus-kinase-2 protein. All these compounds have moderate ADMET qualities, which need to be calibrated to counteract their toxic effect and increase the drug effectivity. Mairin, Oleanonic acid, and Stigmasterol are the potential phytochemicals of Jujubae fructus playing a therapeutic role in OA. These compounds can be further explored for invitro and clinical studies.

酸枣是一种传统的药用植物,其果实(Jujubae fructus)几十年来一直被高度利用在草药中。这种植物的果实含有多种具有有效生物活性的植物化学物质。这些植物化学物质已在本研究中利用网络药理学和分子对接方法来发现潜在的候选药物,以防止骨关节炎(OA)的进展。从TCMSP数据库中获取枣子的植物化学物质信息,进行药物相似性和口服生物利用度筛选。通过BATMAN-TCM数据库和IGEMDOCK 2.1分子对接,对筛选出的化合物进行网络药理学研究。从这个分析得到的化合物被用来预测它们的ADMET性质。网络药理学分析显示,Mairin、齐墩果酸、齐墩果酸和豆甾醇可减轻炎症并激活过氧化物酶体增殖物激活受体(PPARs)信号通路,干预OA进展。分子对接预测Mairin、齐墩果酸和豆甾醇通过靶向Janus-kinase-2蛋白来减轻炎症。所有这些化合物都具有中等ADMET质量,需要校准以抵消其毒性作用并提高药物有效性。蜜苷、齐墩果酸和豆甾醇是枣果实中可能具有治疗OA作用的植物化学物质。这些化合物可以进一步用于体外和临床研究。
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引用次数: 0
Anticancer activity of thymoquinone and its combinations with doxorubicin and linseed oil in the treatment of xenograft tumors 百里醌的抗癌活性及其与阿霉素和亚麻籽油联合治疗异种移植肿瘤的研究
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-09 DOI: 10.1007/s13596-024-00785-8
Oleg Shadyro, Anna Sosnovskaya, Irina Edimecheva, Lana Kireicikova, Svetlana Samovich, Boris Dubovik, Sergei Krasny, Dmitry Tzerkovsky

Thymoquinone (TQ), the main bioactive component of Nigella sativa, has shown promising anticarcinogenic activity in extensive preclinical studies. This study aimed to evaluate the antitumor activity of TQ, in a wide range of doses with monotherapy and combined use with known the chemotherapeutic drug doxorubicin (Dox) and linseed oil (LO) in a rat model with Pliss lymphosarcoma (PLS) and a mouse model with Lewis lung adenocarcinoma (LLC). Animals was administered orally of TQ daily for 12 days at doses of 5, 10 and 30 mg/kg of body weight (rats) and 5 mg/kg (mice) from the 7th day after subcutaneous transplantation of tumors, as well as combinations of TQ with Dox (5 mg/kg, once at the start of treatment by i.p.) and LO (3 ml/kg, orally). It was found that TQ in the studied doses significantly suppresses the growth of the PLS and the LLC tumors (p < 0.001) and increases the frequency of complete tumor regression (FCR) (p < 0.001) compared to control. TQ, especially (TQ + LO) were able to effectively potentiates the antitumor effect of Dox when used in combination, reducing the PLS tumor volume at the end of treatment by 1.9–2.7 times (p < 0.009), increasing the FCR tumors 60 days after the start of treatment by 2.7–3.7 times (p < 0.02) (PLS) and by 1.5 times (p ≤ 0.05) (LLC), as well as reducing the LLC frequency of metastasis compared to Dox monotherapy. The results strongly suggest that TQ and its combination with LO have clinical potential as an adjuvant in cancer chemotherapy using Dox.

百里醌(TQ)是黑草(Nigella sativa)的主要生物活性成分,在广泛的临床前研究中显示出良好的抗癌活性。本研究旨在评估TQ在大剂量单药治疗和与已知化疗药物阿霉素(Dox)和亚麻籽油(LO)联合使用下对Pliss淋巴肉瘤(PLS)大鼠模型和Lewis肺腺癌(LLC)小鼠模型的抗肿瘤活性。动物从肿瘤皮下移植后第7天开始,每天口服TQ,剂量分别为5、10和30 mg/kg(大鼠)和5 mg/kg(小鼠),持续12天,以及TQ与Dox (5 mg/kg,在开始ig治疗时1次)和LO (3 ml/kg,口服)联合使用。研究发现,与对照组相比,TQ在研究剂量下显著抑制了PLS和LLC肿瘤的生长(p < 0.001),并增加了肿瘤完全消退(FCR)的频率(p < 0.001)。TQ,特别是(TQ + LO)在联合使用时能够有效增强Dox的抗肿瘤作用,治疗结束时PLS肿瘤体积减少1.9-2.7倍(p < 0.009),治疗开始后60天FCR肿瘤增加2.7-3.7倍(p < 0.02) (PLS)和1.5倍(p≤0.05)(LLC),并且与Dox单药治疗相比,LLC转移频率降低。结果强烈提示,TQ及其联合LO在使用Dox的癌症化疗中具有辅助治疗的临床潜力。
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引用次数: 0
Anti-fatigue effects of low-molecular-weight brewer’s yeast extracts on mice 低分子啤酒酵母提取物对小鼠的抗疲劳作用
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-09 DOI: 10.1007/s13596-024-00786-7
Minsu Pyeon, Jiwon Lee, Myungmi Moon, Jeonghoon Park, Ahyuk Kim, Seonyoung Im, Sooan Kim, Junho H. Lee, Gyung-Hyun Jo

Muscle mass naturally declines with age; however, sudden and significant muscle loss is considered a pathological condition. This decline in physical function increases the risk of falls and fractures; additionally, maintaining daily life activities can become challenging, leading to further complications. The World Health Organization has classified sarcopenia as a disease because affected individuals exhibit a mortality rate up to double that of those without the condition. Brewer’s yeast, a traditional nutritional supplement, has garnered recent attention for its potential role in muscle synthesis. This study focuses on the efficacy of low-molecular-weight yeast extract, specifically that with a molecular weight < 10 kDa, in enhancing muscle growth and regeneration. Yeast extracts are known for their high bioavailability and capacity to facilitate efficient absorption and utilization within the body. Our research involved a series of in vitro and in vivo experiments aimed at elucidating the effects of these extracts on muscle cells. The results demonstrated a significant increase in protein synthesis within muscle cells treated with low-molecular-weight yeast extracts. Additionally, these extracts promoted muscle cell growth and differentiation, further supporting their role in muscle development. Detailed analysis revealed that the yeast extracts enhanced the activation of key signaling pathways involved in muscle protein synthesis and cell differentiation. In the rota-rod test, all yeast extract-treated groups exhibited an increasing trend in exercise performance compared with the control group. These findings underscore the potential of low-molecular-weight yeast extracts as a valuable component in muscle synthesis and regeneration. Furthermore, this study highlights the broader implications of these findings for the growing older population. In addition, it suggests that low-molecular-weight yeast extracts can be incorporated into dietary supplements aimed at addressing sarcopenia and muscle loss in older adults by enhancing muscle growth and recovery.

肌肉质量会随着年龄的增长而自然下降;然而,突然和显著的肌肉损失被认为是一种病理状态。身体机能的下降增加了跌倒和骨折的风险;此外,维持日常生活活动可能变得具有挑战性,导致进一步的并发症。世界卫生组织将肌肉减少症列为一种疾病,因为患有这种疾病的人的死亡率是没有这种疾病的人的两倍。啤酒酵母是一种传统的营养补充剂,最近因其在肌肉合成中的潜在作用而引起了人们的关注。本研究的重点是低分子量酵母提取物,特别是分子量为10 kDa的酵母提取物,在促进肌肉生长和再生方面的功效。酵母提取物以其高生物利用度和促进体内有效吸收和利用的能力而闻名。我们的研究涉及一系列体外和体内实验,旨在阐明这些提取物对肌肉细胞的影响。结果表明,用低分子酵母提取物处理的肌肉细胞内蛋白质合成显著增加。此外,这些提取物促进肌肉细胞生长和分化,进一步支持其在肌肉发育中的作用。详细分析表明,酵母提取物增强了参与肌肉蛋白合成和细胞分化的关键信号通路的激活。在转棒试验中,各酵母提取物处理组的运动性能均较对照组有提高的趋势。这些发现强调了低分子量酵母提取物作为肌肉合成和再生中有价值的成分的潜力。此外,这项研究强调了这些发现对日益增长的老年人口的更广泛的影响。此外,该研究还表明,低分子酵母提取物可以加入膳食补充剂中,通过促进肌肉生长和恢复,解决老年人肌肉减少症和肌肉损失的问题。
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引用次数: 0
Effect of acupressure on migraine: a systematic review and meta-analysis 穴位按压对偏头痛的影响:系统回顾和荟萃分析
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-22 DOI: 10.1007/s13596-024-00780-z
Arya Asadizeidabadi, Seyedmohammadamin Hosseini, Ali Ataei, Hamidreza Amiri, Daniel Shafiei, Mandana Dehghan, Seyede Zakieh Modares Mosalla

Introduction

Migraine, a prevalent neurological disorder, affects about 14.4% of the global population, ranking among the leading causes of disability, especially in young women. Acupressure, a non-invasive therapy akin to acupuncture, has emerged as a potential intervention for migraine management. However, its effectiveness remains inconclusive due to the lack of comprehensive systematic reviews. This study aims to systematic review and meta-analysis existing literature to investigate the effect of acupressure on migraine symptoms. Methods Adhering to PRISMA guidelines, a comprehensive search strategy was employed across multiple databases. Eligible studies included randomized controlled trials (RCTs), cohort studies and case reports involving individuals diagnosed with various migraine types. Data synthesis and analysis were conducted using STATA 14, with meta-analyses performed on available quantitative data. Results From 250 initial records, 12 studies were included, comprising ten RCTs, one cohort study, and one case report, with six RCTs included in the meta-analysis. Results showed mixed findings regarding acupressure’s impact on migraine symptoms, with improvements noted in headache intensity, frequency, duration, and nausea. However, substantial heterogeneity among studies and methodological limitations were identified, limiting the conclusiveness of the evidence. Conclusion Despite promising results, this review underscores the need for further research. Methodologically robust studies with larger sample sizes are warranted to elucidate acupressure’s role in migraine treatment. Nonetheless, continued investigation into complementary therapies like acupressure holds promise for providing non-invasive options for migraine management.

偏头痛是一种普遍存在的神经系统疾病,影响着全球约14.4%的人口,是导致残疾的主要原因之一,尤其是在年轻女性中。穴位按压,一种类似于针灸的非侵入性疗法,已经成为偏头痛治疗的潜在干预手段。然而,由于缺乏全面系统的评价,其有效性仍不确定。本研究旨在系统回顾和荟萃分析现有文献,探讨穴位按压对偏头痛症状的影响。方法遵循PRISMA指南,采用跨多个数据库的综合检索策略。符合条件的研究包括随机对照试验(rct),队列研究和病例报告,涉及诊断为各种偏头痛类型的个体。使用STATA 14进行数据综合和分析,并对可用的定量数据进行荟萃分析。结果从250份初始记录中纳入了12项研究,包括10项随机对照试验、1项队列研究和1份病例报告,其中6项随机对照试验纳入meta分析。结果显示,穴位按压对偏头痛症状的影响好坏参半,在头痛强度、频率、持续时间和恶心方面均有改善。然而,研究之间存在很大的异质性和方法上的局限性,限制了证据的结论性。尽管结果令人鼓舞,但本综述强调了进一步研究的必要性。方法学上稳健的研究与更大的样本量有必要阐明穴位按压在偏头痛治疗中的作用。尽管如此,对穴位按摩等补充疗法的持续研究有望为偏头痛的治疗提供非侵入性的选择。
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引用次数: 0
Ethanol extract of black shallot (Allium ascalonicum Linnaeus) for breast cancer prevention: evidence from a DMBA-induced mouse model 黑葱(Allium ascalonium Linnaeus)乙醇提取物对乳腺癌的预防作用:来自dba诱导的小鼠模型的证据
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-19 DOI: 10.1007/s13596-024-00781-y
Thi Phuong Nhung Tran, Thi Thanh Nha Tran

Breast cancer is the leading cause of cancer-related mortality, posing challenges in treatment due to high costs, numerous side effects, and systemic toxicity. Consequently, many patients seek natural compounds with low toxicity and potential anticancer and pain-relief properties. The ethanol extract of black shallot (EEBS) from Allium ascalonicum Linnaeus has shown promise due to its antioxidant properties and ability to induce apoptosis in various cancer cell lines. This study investigates the effect of EEBS on breast cancer prevention in a DMBA-induced mammary tumor model in mice. EEBS was administered at doses of 300 to 500 mg/kg body weight (BW), with tamoxifen (3.3 mg/kg BW) serving as a standard reference drug. DMBA-treated mice were confirmed to develop mammary tumors (p < 0.05). In contrast, mice dosed with EEBS exhibited slower tumor progression (p < 0.05), indicating the extract’s promising therapeutic potential. EEBS significantly reduced tumor volumes, incidence rates, and TNF-α levels (p < 0.05) in a dose-dependent manner, achieving a maximum reduction in tumor volume of 65.8% and a minimum incidence rate of 24 ± 5.48% at the dose of 500 mg/kg. Treatment with EEBS also considerably improved hematological parameters (WBC, LYM, RBC, HGB, HCT, and PLT) and reduced hepatic and renal function indicators (AST, ALT, ALP, GLU, BIL, URE, CRE, URA) (p < 0.05), reflecting its protective effects on liver and kidney functions. Histopathological examination further confirmed the efficacy of EEBS in inhibiting tumor progression. Importantly, no mortality was observed, highlighting the safety of the experimental treatments. These findings suggest that black shallot extract could be a potential therapeutic agent for breast cancer prevention and for mitigating DMBA-induced toxicity.

乳腺癌是癌症相关死亡的主要原因,由于费用高、副作用多和全身毒性,给治疗带来了挑战。因此,许多患者寻求具有低毒性和潜在抗癌和缓解疼痛特性的天然化合物。黑葱乙醇提取物因其抗氧化特性和诱导多种癌细胞凋亡的能力而具有广阔的应用前景。本研究在dmba诱导的小鼠乳腺肿瘤模型中探讨了EEBS对乳腺癌的预防作用。给药剂量为300 ~ 500 mg/kg体重(BW),他莫昔芬(3.3 mg/kg体重)作为标准参比药物。经dmba处理的小鼠证实发生乳腺肿瘤(p < 0.05)。相比之下,给予EEBS的小鼠肿瘤进展较慢(p < 0.05),表明该提取物具有良好的治疗潜力。ebs显著降低肿瘤体积、发病率和TNF-α水平(p < 0.05),呈剂量依赖性,在500 mg/kg剂量下,肿瘤体积最大减少65.8%,发病率最小减少24±5.48%。应用EEBS治疗也显著改善了血液学指标(WBC、LYM、RBC、HGB、HCT、PLT),降低了肝肾功能指标(AST、ALT、ALP、GLU、BIL、URE、CRE、URA) (p < 0.05),反映了其对肝肾功能的保护作用。组织病理学检查进一步证实了EEBS抑制肿瘤进展的有效性。重要的是,没有观察到死亡,强调了实验治疗的安全性。这些发现表明,黑葱提取物可能是一种潜在的治疗剂,可以预防乳腺癌和减轻dba诱导的毒性。
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引用次数: 0
The biological effects of Rosa rugosa extract on keratinocyte differentiation and enhancement of skin barrier function 玫瑰提取物对角质细胞分化及增强皮肤屏障功能的生物学效应
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-17 DOI: 10.1007/s13596-024-00778-7
Minju Jeong, Jeongmin Cho, Dohyo Lim, Myungsoo Choi, Yukyung Park, Yeonhee Cheong, Youngwoong Kang, Inhee Kang, Sooah Kim, Dongwon Kim

We investigated the biological activity of Rosa rugosa (R. rugosa) extract in human epidermal keratinocytes. To assess the antioxidant capacity of the extract, various concentrations (0.1, 0.5, 1, 5, 10, 50 mg/ml) were tested against DPPH and ABTS free radicals. The results showed antioxidant activities of 45% at 5 mg/ml, 60% at 10 mg/ml, and 82% at 50 mg/ml. Cell toxicity experiments using human keratinocytes revealed no cytotoxicity up to 10 μg/ml, and the cells exhibited a differentiated morphology. We confirmed the efficacy of the extract in keratinocytes, with a significant increase in the expression of keratinocyte differentiation factors Keratin (KRT)1 and KRT10. Moreover, the expression of genes related to skin barrier function, including Filaggrin (FLG), Involucrin (IVL), Loricrin (LOR), and Claudin1 (CLDN1), significantly increased. In an in vitro atopic model experiment treating human keratinocytes with Interleukin (IL)-4/IL-13, the R. rugosa extract maintained the expression of FLG protein. Overall, R. rugosa demonstrated high antioxidant activity and was found to be a safe material for human keratinocytes. Furthermore, it induced keratinocyte differentiation, particularly increasing the expression of FLG, IVL, LOR, and CLDN1, which are components of the skin barrier. While additional research is needed to validate these experimental results, R. rugosa extract holds promise as a novel ingredient for the development of cosmetics or pharmaceuticals that could alleviate inflammatory skin conditions such as atopic dermatitis or psoriasis.

研究了玫瑰提取物在人表皮角质形成细胞中的生物活性。为了评估不同浓度(0.1、0.5、1、5、10、50 mg/ml)的提取物对DPPH和ABTS自由基的抗氧化能力。结果表明,5 mg/ml、10 mg/ml和50 mg/ml的抗氧化活性分别为45%、60%和82%。对人角质形成细胞进行的细胞毒性实验显示,当浓度达到10 μg/ml时,细胞无毒性,细胞形态呈现分化。我们证实了提取物对角质形成细胞的作用,角质形成细胞分化因子Keratin (KRT)1和KRT10的表达显著增加。此外,与皮肤屏障功能相关的聚丝蛋白(FLG)、Involucrin (IVL)、Loricrin (LOR)、cldin1 (CLDN1)等基因的表达也显著升高。在用白细胞介素-4/IL-13处理人角质形成细胞的体外特应性模型实验中,红草提取物维持了FLG蛋白的表达。总的来说,红毛霉具有较高的抗氧化活性,是一种安全的人角质形成细胞材料。此外,它诱导角质细胞分化,特别是增加FLG, IVL, LOR和CLDN1的表达,这些都是皮肤屏障的组成部分。虽然还需要进一步的研究来验证这些实验结果,但红草提取物有望成为开发化妆品或药物的新成分,可以缓解炎症性皮肤疾病,如特应性皮炎或牛皮癣。
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引用次数: 0
Anticancer potential of Calligonum comosum L.’Her. and Calligonum crinitum Boiss plants from United Arab Emirates 芫荽的抗癌潜力。以及产自阿拉伯联合酋长国的沙利贡(caligonum criinitum Boiss)植物
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-01 DOI: 10.1007/s13596-024-00773-y
Wesam Khader, Mohamed K. Kayali, Tawfik M. Taj Eddin, Abdul Hadi S. S. S. Alameri, Mughair Abdul Aziz, Jaleel Kizhakkayil, Annadurai Senthilkumar, Ayesha S. Al Dhaheri, Abdul Jaleel

Indigenous plants from arid regions are known for their diverse applications in traditional medicine. These plants are particularly promising as potential anticancer agents due to their ability to produce a wide range of secondary metabolites. The present study addressed the problem of identifying and evaluating the anticancer properties of crude extracts from indigenous arid-region plants, Calligonum comosum L.’Her. and Calligonum crinitum Boiss., to determine their efficacy against human breast (MCF-7) and human colon adenocarcinoma (Caco-2) cell lines. Through various solvent-treated leaf extracts, including hexane, methanol, acetone, and chloroform, we aimed to determine the antiproliferative activities and identify extracts with promising efficacy in inhibiting cancer cell viability. The morphological changes and anticancer effects induced by these solvent-treated C. comosum and C. crinitum leaf extracts were investigated. Our results indicated that the use of acetone isolated leaf extracts on the MCF-7 cells displayed apoptotic morphological changes. Similarly, the MTT cytotoxicity assay revealed that the acetone-treated extracts of C. comosum and C. crinitum showed a significant inhibitory effect on MCF-7 cell lines, with IC50 values of 24.62 μg/ml and 23.41 μg/ml, respectively. Conversely, the other solvents resulted in higher IC50 values for inhibiting the MCF-7 cell proliferation. While for the Caco-2 cell lines, we observed remarkable antiproliferation activity, with IC50 values of 37.76 µg/ml and 74.88 µg/ml for the C. comosum and C. crinitum chloroform-isolated extracts, respectively, in comparison to the hexane, methanol, and acetone-isolated extracts. These findings suggest that the extracts of C. comosum and C. crinitum possess significant potential for inhibiting the viability of MCF-7 and Caco-2 cancer cell lines, indicating their possible use as anticancer agents.

来自干旱地区的本土植物以其在传统医学中的多种应用而闻名。这些植物特别有希望作为潜在的抗癌药物,因为它们能够产生广泛的次生代谢物。本研究旨在鉴别和评价土着干旱地区植物caligonum comosum L.的抗癌特性。和胭脂草。以确定其对人乳腺(MCF-7)和人结肠腺癌(Caco-2)细胞系的抑制作用。通过己烷、甲醇、丙酮和氯仿等不同溶剂处理的叶提取物,我们旨在确定其抗增殖活性,并鉴定出具有抑制癌细胞活力的有希望的提取物。研究了经溶剂处理的荆芥和荆芥叶提取物的形态变化及其抗癌作用。我们的结果表明,丙酮分离叶提取物对MCF-7细胞产生凋亡形态学改变。同样,MTT细胞毒性实验显示,丙酮处理的金合藤和金合藤提取物对MCF-7细胞株有显著的抑制作用,IC50值分别为24.62 μg/ml和23.41 μg/ml。相反,其他溶剂抑制MCF-7细胞增殖的IC50值较高。而对于Caco-2细胞系,我们观察到显著的抗增殖活性,与己烷、甲醇和丙酮分离的提取物相比,芫花和荆芥氯仿分离提取物的IC50值分别为37.76µg/ml和74.88µg/ml。这些结果表明,荆芥和荆芥提取物对MCF-7和Caco-2癌细胞具有明显的抑制作用,可能作为抗癌药物使用。
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引用次数: 0
Evaluation of the anti-inflammatory potential of zingiber officinale on adjuvant-induced arthritis 药用姜对佐剂性关节炎抗炎作用的评价
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-01 DOI: 10.1007/s13596-024-00779-6
Great Iruoghene Edo, Favour Ogheneoruese Onoharigho, Khawla A. Kasar, Irene Ebosereme Ainyanbhor, Agatha Ngukuran Jikah

Ginger (Zingiber officinale) is an herb utilized all over the world for its extensive phytochemical properties. This study aims to evaluate the anti-inflammatory effects of Zingiber officinale. Arthritis was induced in the rats used in the experiment using Complete Freund’s adjuvant (CFA). Gas chromatography-Mass spectroscopy (GC-MS) was used to screen for bioactive components present in ginger. For ten days, Zingiber officinale ethanolic extract (62.5, 125, and 250 mg/kg/day) was administered orally to the rats. Edema in the paws was measured before and 10 days after Zingiber officinale treatment in order to identify pathological alterations. Additionally, cytokine levels (TNF-α, IL-1β, and IL-6) were assessed in plasma. When compared to the control group, the CFA-arthritis induced group had edema in their paws and knee joints considerably reduced upon treated with Zingiber officinale at days 6, 8, and 10. Rats in the groups given Zingiber officinale also showed a significant decrease in cytokine levels and also recovered from the pathological alterations brought on by CFA. Twenty bioactive metabolites were found when the extracts of the ethanol, hexane, and chloroform was analyzed using GC-MS. There were no carbohydrates or steroids in the chloroform and n-hexane extract. Protein and cardiac glycoside were also missing. In summary, our findings demonstrated that Zingiber officinale treatment was successful in preventing CFA-induced arthritis through its cytokine level regulation anti-inflammatory property.

生姜(Zingiber officinale)是一种因其广泛的植物化学特性而被世界各地使用的草药。本研究旨在评价药用姜的抗炎作用。实验用完全弗氏佐剂(CFA)诱导大鼠关节炎。采用气相色谱-质谱联用技术对生姜中的生物活性成分进行了筛选。大鼠口服生姜乙醇提取物(62.5、125、250 mg/kg/d) 10 d。在给药前和给药后10天测量足部水肿,以确定病理改变。此外,评估血浆中细胞因子水平(TNF-α、IL-1β和IL-6)。与对照组相比,cfa -关节炎诱导组在第6、8和10天服用生姜后,其爪子和膝关节的水肿明显减轻。给药组大鼠的细胞因子水平也明显下降,并从CFA引起的病理改变中恢复过来。对乙醇、己烷和氯仿提取物进行气相色谱-质谱分析,发现20种生物活性代谢物。氯仿和正己烷提取物中不含碳水化合物或类固醇。蛋白质和心糖苷也缺失。综上所述,我们的研究结果表明,生姜通过其调节细胞因子水平的抗炎特性,成功地预防了cfa诱导的关节炎。
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引用次数: 0
Anticancer effect of ethanolic extract of Rheum ribes L. rhizomes: assessment of dose and time-dependent effects in cell-based models 大黄根茎乙醇提取物的抗癌作用:基于细胞模型的剂量和时间依赖性效应评估
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-30 DOI: 10.1007/s13596-024-00772-z
Zeina Nehme, Fatima Ghandour, Akram Hijazi, Mona Diab-Assaf, Racha Karaky

Introduction

Medicinal plants have been traditionally used in the treatment of various diseases including cancer, however, their IC50 determined in vitro are hardly attained in patients. Rheum ribes L. is an indigenous medicinal plant shown to possess anticancer activity due to high polyphenolic compounds abundance. Our objective was to assess if long-term exposure to plant extract concentrations lower than IC50 may still possess an anticancer potential.

Methods

We used the ethanolic extract of rhizomes of Rheum ribes L. (EERR) and assessed its effect on proliferation, clonogenicity, and senescence in cell lines-based models.

Results

Our results showed that EERR has a short-term antiproliferative activity on non-small cell lung carcinoma A549, breast cancer MCF7, and glioblastoma SF268 cell lines with IC50 varying from 100 to 255 µg/mL. Additionally, EERR decreased the population doubling level and the clonogenic ability of the three cancer cell lines at lower concentrations (10 to 100 µg/mL) and with longer treatment protocols. This was accompanied by a significant increase in the senescence-associated β-galactosidase activity, suggesting that EERR induces senescence at these concentrations.

Conclusion

EERR displayed anticancer activity at concentrations 2- to 10-fold lower than the IC50 in three different cancer cell lines and should be further investigated as it may provide novel therapeutic avenues for cancer treatment.

Graphical abstract

传统上,药用植物被用于治疗包括癌症在内的各种疾病,然而,它们在体外测定的IC50在患者体内很难达到。大黄是一种具有抗癌活性的本土药用植物,其多酚类化合物含量较高。我们的目的是评估长期暴露于浓度低于IC50的植物提取物是否仍具有抗癌潜力。方法采用大黄根茎乙醇提取物(EERR)建立细胞系模型,观察其对细胞增殖、克隆原性和衰老的影响。结果EERR对非小细胞肺癌A549、乳腺癌MCF7和胶质母细胞瘤SF268细胞系具有短期的抗增殖活性,IC50在100 ~ 255µg/mL之间。此外,EERR在较低浓度(10 ~ 100µg/mL)和较长的治疗方案下,降低了三种癌细胞的种群倍增水平和克隆生成能力。这伴随着衰老相关β-半乳糖苷酶活性的显著增加,表明EERR在这些浓度下诱导衰老。结论eerr在3种不同的肿瘤细胞系中均表现出低于IC50浓度2 ~ 10倍的抗肿瘤活性,可能为肿瘤治疗提供新的治疗途径,值得进一步研究。图形抽象
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引用次数: 0
Jatropha tanjorensis leaf extracts attenuate adrenaline-induced myocardial cell injury via modulation of cardio-inflammatory biomarkers in Wistar rats 麻风树叶提取物通过调节 Wistar 大鼠心肌炎生物标志物减轻肾上腺素诱导的心肌细胞损伤
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-26 DOI: 10.1007/s13596-024-00776-9
Idara Asuquo Okon, Elizabeth Bassey Umoren, Emmanuel Uchechukwu Modo, Providence Idabie Brown, Joseph Igbo Enya, Daniel Udofia Owu

Myocardial injury (MI) has remain a global concern due to high mortality rate associated with cardiovascular diseases. Jatropha tanjorensis (J. tanjorensis) is a medicinal herb with proven medicinal properties. This study investigated the level of cardio-inflammatory response in adrenaline-induced MI in rats treated with J. tanjorensis. Twenty Wistar rats were randomly divided into four groups (n = 5). Group 1 served as Control. Group 2 was induced with MI using 2 mg/kg bodyweight of adrenaline administered subcutaneously for two days at 24 h interval between the first and second administrations. Group 3 received 200 mg/kg body weight of methanol extract of J. tanjorensis orally for 14days while Group 4 were induced with MI using 2 mg/kg body weight of adrenaline and treated with 200 mg/kg of J. tanjorensis leaf extract for 14 days. Blood was collected via cardiac puncture for biochemical analysis. J. tanjorensis reduced adrenaline-induced MI by lowering serum concentration of ALT, AST and ALP, pro-inflammatory (MDA, CRP and IL-6) and cardiac injury markers (CK-MB, Troponin-I). SOD and NO level were also raised in J. tanjorensis-treated animals. The extract also restored histoarchitectural changes in the cardiac muscle. Jatropha tanjorensis mitigates cardio-inflammatory response and restores cyto-architecture of the cardiac muscle in adrenaline-induced MI rats.

由于与心血管疾病相关的高死亡率,心肌损伤一直是全球关注的问题。麻疯树(jj . tanjorensis)是一种经证实具有药用特性的草药。本研究探讨了肾上腺素诱导的心肌梗死大鼠丹参治疗后的心脏炎症反应水平。Wistar大鼠20只,随机分为4组(n = 5)。第一组为对照组。第2组采用肾上腺素2 mg/kg体重皮下注射,第1、2次给药间隔24 h,连续2天诱导心肌梗死。3组以200 mg/kg体重的丹参甲醇提取物灌胃14d, 4组以2 mg/kg体重的肾上腺素诱导心肌梗死,并用200 mg/kg丹参叶提取物灌胃14d。经心脏穿刺采血进行生化分析。J. tanjorensis通过降低血清ALT、AST和ALP浓度、促炎(MDA、CRP和IL-6)和心脏损伤标志物(CK-MB、Troponin-I)来减轻肾上腺素诱导的心肌梗死。丹参处理动物的SOD和NO水平均升高。该提取物还能恢复心肌的组织结构变化。麻疯树可减轻肾上腺素诱导的心肌梗死大鼠的心脏炎症反应并恢复心肌细胞结构。
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引用次数: 0
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Advances in Traditional Medicine
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