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The Influence of Portulaca Oleracea L. Leaves Extracts on the Histoarchitecture of Culex Quinquefasciatus and Anopheles Stephensi Larvae 马齿苋叶提取物对致倦库蚊和史蒂芬按蚊幼虫组织结构的影响
Pub Date : 2022-09-01 DOI: 10.1016/j.ccmp.2022.100053
Parthasarathy Sudharsan , Durairaj Siva , Kamaraj Prabhu , Chandran Janani

Background

Mosquito is a big threat to the human health. Mosquito-borne diseases cause millions of death to the human beings. Hence, a permanent solution is eagerly to be established to control its excessive growth in stagnant water. Portulaca oleracea Linn is a natural larvicidal agent, which contains active ingredients such as linolenic acid, linoleic acid (omega-3 fatty acids). These bioactive compounds may be responsible for its larvicidal properties on mosquito.

Objective

The present study is focussed on identifying the bioactive compounds, such as linolenic acid, through GC–MS, and analyzing the larvicidal efficacy of Portulaca oleracea L. against Culex quinquefasciatus and Anopheles stephensi larvae.

Methods

Preliminary phytochemical analysis, total protein content, total carbohydrate content, total phenol content, total flavonoid content and GC–MS analysis exhibited the presence of rich phytoconstituents in Portulaca oleracea. DPPH analysis was carried out to analyze the antioxidant potential of plant extract. Larvicidal activity and histological change were detected to evaluate the efficacy of Portulaca oleracea L. on the Culex quinquefasciatus and Anopheles stephensi larvae.

Results

Aqueous and ethanol leaf extracts of Portulaca oleracea L. against both Culex quinquefasciatus and Anopheles stephensi larvae, showed a very good larvicidal activity at 500 µg/mL among the various concentrations. Histological damages of mosquito larvae were observed when treated with the Portulaca oleracea L. extract, and provided further evidence for its larvicidal activity.

Conclusion

This study concluded that the plant Portulaca oleracea L. contained many useful bioactive compounds, can be a strong larvicidal agent against both Culex quinquefasciatus and Anopheles stephensi larvae. The molecular mechanism for the larvicidal activity will be identified in future studies.

蚊子是人类健康的一大威胁。蚊子传播的疾病导致数百万人死亡。因此,迫切需要建立一个永久的解决方案,以控制其在死水中的过度生长。马齿苋亚麻是一种天然的杀幼虫剂,含有亚麻酸、亚油酸(omega-3脂肪酸)等活性成分。这些生物活性化合物可能是其对蚊子具有杀幼虫作用的原因。目的通过气相色谱-质谱联用技术鉴定马蹄莲中亚麻酸等生物活性成分,并分析马蹄莲对致倦库蚊和斯氏按蚊幼虫的杀灭效果。方法初步植物化学分析、总蛋白含量、总碳水化合物含量、总酚含量、总黄酮含量及GC-MS分析显示马马苋中存在丰富的植物成分。采用DPPH法分析植物提取物的抗氧化能力。通过测定马齿苋对致倦库蚊和斯氏按蚊幼虫的杀幼虫活性和组织学变化,评价马齿苋对致倦库蚊和斯氏按蚊幼虫的杀幼虫效果。结果马齿苋叶片水提液和乙醇提液在500µg/mL浓度下对致倦库蚊和斯氏按蚊幼虫均有较好的杀灭活性。观察了马齿苋提取物对蚊子幼虫的组织学损伤,为马齿苋提取物的杀幼虫活性提供了进一步的证据。结论马齿苋含有多种有益的生物活性成分,可作为致倦库蚊和斯氏按蚊的强杀幼虫剂。其杀虫活性的分子机制有待进一步研究。
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引用次数: 2
A Review of the Effects of Policosanol on Metabolic Syndrome 多酚醇对代谢综合征作用的研究进展
Pub Date : 2022-09-01 DOI: 10.1016/j.ccmp.2022.100058
Lawal Kayode Olatunji , Abdulgafar O. Jimoh , Umar Muhammad Tukur , Mustapha Umar Imam

Background

Cardiovascular disease is the world's number one killer disease and the leading non-communicable disease in terms of causing premature deaths. Overwhelming evidence suggest that effective management of metabolic syndrome will markedly reduce morbidity and premature deaths from cardiovascular disease. Although many therapies exist, most of them are ineffective due to decreased effectiveness and/or side effects following prolonged usage. Policosanol, a well-tolerated long-chain aliphatic alcohol has been proven to be effective against the components of metabolic syndrome (namely dyslipidemia, diabetes, hypertension, and obesity) even when used for a long period with minimal or no adverse effects.

Objective

This study intends to explore the potential benefits of Policosanol in the management of metabolic syndrome.

Methods

PubMed, Google Scholar, and Science Direct were used as the search engines to retrieve articles related to Policosanol and metabolic syndrome from 2010 to 2021.

Results

The results from the three search engines were scrutinized and merged. Duplicate publications were excluded. Similarly, four articles from the WHO website (www.who.int/publications) were included making a total of 63 articles used in this review. Most of the reviewed articles show Policosanol to be effective in reducing systolic and diastolic blood pressure, blood glucose level, body weight, total cholesterol level, triglyceride level, low density lipoprotein and increasing high density lipoprotein levels. There are few conflicting articles that reported Policosanol to have no effect on lipid parameters.

Conclusion

Policosanol was shown to be a safe and well-tolerated natural product that is effective against all the components of metabolic syndrome. Thus, using this natural product will go a long way in reducing the burden and economic consequences of the syndrome.

背景心血管疾病是世界头号杀手疾病,也是导致过早死亡的头号非传染性疾病。大量证据表明,代谢综合征的有效管理将显著降低心血管疾病的发病率和过早死亡。虽然存在许多治疗方法,但由于长期使用后效果下降和/或副作用,大多数都无效。甘草糖醇是一种耐受性良好的长链脂肪醇,已被证明对代谢综合征(即血脂异常、糖尿病、高血压和肥胖)的成分有效,即使长期使用也几乎没有副作用。目的探讨多酚在代谢综合征治疗中的潜在益处。方法采用spubmed、Google Scholar和Science Direct作为搜索引擎,检索2010 - 2021年与糖醇与代谢综合征相关的文章。结果三个搜索引擎的结果被仔细审查和合并。重复出版物被排除在外。同样,世卫组织网站(www.who.int/publications)上的四篇文章也被纳入,使得本综述共使用了63篇文章。大多数综述文章表明,多酚能有效降低收缩压和舒张压、血糖水平、体重、总胆固醇水平、甘油三酯水平、低密度脂蛋白水平和增加高密度脂蛋白水平。很少有相互矛盾的文章报道壬二醇对脂质参数没有影响。结论甘草皂醇是一种安全、耐受性良好的天然产物,对代谢综合征各组分均有疗效。因此,使用这种天然产品将大大有助于减轻该综合征的负担和经济后果。
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引用次数: 0
The Influence of Age on Blood Flow and Temperature of Acupuncture Points: A Study based on Laser Doppler Flowmetry and Infrared Thermography 年龄对穴位血流和温度的影响:基于激光多普勒血流仪和红外热像仪的研究
Pub Date : 2022-09-01 DOI: 10.1016/j.ccmp.2021.100018
Yajun Zhang , Xiaoyu Li , Xiaofen He , Yongliang Jiang , Hantong Hu , Jiali Lou , Ruijie Ma , Yi Liang , Xiaomei Shao , Jianqiao Fang

Background

To date, there has been a great lack of investigation on the influence of age on blood flow and temperature of acupoints in specific regions.

Objective

This study aimed to determine the association between different age categories and acupoint blood flow/temperature on the forearm.

Methods

Acupoint blood flow and temperature were measured in healthy adults of different age categories using laser doppler flowmetry (LDF) and infrared thermography (IRT), respectively. A total of 60 eligible healthy volunteers were divided into the young group, mid age group and old age group. All groups received LDF and IRT examination. Shenmen (HT7), Shaohai (HT3), Taiyuan (LU9) and Chize (LU5) of the Heart and Lung meridians on the forearm were selected as 4 test acupoints.

Results

Regarding blood flow of the 4 test acupoints, the PU of Taiyuan (LU9) in the old age group was significantly different compared with that of the young age group (P < 0.05) and the mid age group (P < 0.05), while there was no significant difference in PU of the other acupoints between 3 groups (all P > 0.05). Similarly, regarding acupoint temperature of the 4 test sites, the temperature of Shaohai (HT3) in the old age group was significantly different compared with that of the mid age group (P < 0.05), while there was no significant difference in the temperature of the other 3 acupoints between 3 age groups (all P > 0.05).

Conclusion

Age category tends to have notable influence on the blood flow and temperature in specific acupoints in the forearm. Therefore, particular concerns should be taken into consideration regarding the effect of age differences for future studies in this field. Nevertheless, further studies with a large sample size and more test acupoints are needed to further verify current findings.

迄今为止,关于年龄对特定区域血流量和穴位温度影响的研究非常缺乏。目的探讨不同年龄与前臂穴位血流量/温度的关系。方法采用激光多普勒血流仪(LDF)和红外热像仪(IRT)分别测量不同年龄段健康成人穴位血流和体温。将60名符合条件的健康志愿者分为青年组、中年组和老年组。各组均行LDF和IRT检查。选取前臂心肺经的申门穴(HT7)、少海穴(HT3)、太原穴(LU9)、赤泽穴(LU5)作为4个试验穴位。结果老年组太原穴(LU9)血流量与青年组比较差异有统计学意义(P <0.05)和中年组(P <0.05),其他穴位PU值3组间比较差异无统计学意义(P >0.05)。同样,在4个试验点的穴位温度上,老年组少海穴(HT3)温度与中老年组比较差异有统计学意义(P <0.05),其余3个穴位温度在3个年龄组间差异无统计学意义(P >0.05)。结论年龄类别对前臂特定穴位的血流量和体温有显著影响。因此,在这一领域的未来研究中,应该特别关注年龄差异的影响。然而,需要进一步的大样本研究和更多的测试穴位来进一步验证目前的发现。
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引用次数: 2
Ayurvedic and Other Herbal Remedies for Dengue: An Update 阿育吠陀和其他草药治疗登革热:最新进展
Pub Date : 2022-09-01 DOI: 10.1016/j.ccmp.2022.100024
Vivek P. Chavda , Anup Kumar , Rittwika Banerjee , Nayan Das

Dengue fever is a flu-like ailment propagated by female mosquitos of the Aedes aegypti species. It is also known as dandaka jwara in Ayurveda. It is most common in the world's subtropical and tropical climate zones. Vomiting, severe headache, nausea, rashes, joint pain, pain behind the eyes, muscle pain, and swollen glands are all common dengue symptoms. If not handled promptly, these symptoms can lead to more severe issues such as exhaustion, blood in the vomit, continuous vomiting, bleeding gums, restlessness, severe abdominal pain, and rapid bleeding. Because there is no specific medication for dengue fever, the disease is treated by eliminating and managing the symptoms. Fortunately, there are a variety of ayurvedic remedies (like Carica papaya L., Cissampelos pareira L., etc.) that can help to tackle the same by strengthening the immune system and controlling hyperthermia. This review article provides a comprehensive overview of dengue virus infections, clinical symptoms, diagnosis, mitigation, and treatments, focusing on ayurvedic and herbal remedies.

登革热是一种类似流感的疾病,由埃及伊蚊的雌性蚊子传播。它在阿育吠陀中也被称为dandaka jwara。它在世界上的亚热带和热带气候区最常见。呕吐、严重头痛、恶心、皮疹、关节痛、眼后痛、肌肉痛和腺体肿胀都是登革热的常见症状。如果不及时处理,这些症状会导致更严重的问题,如疲惫、呕吐物中带血、持续呕吐、牙龈出血、烦躁不安、严重腹痛和快速出血。由于没有针对登革热的特异性药物,所以这种疾病的治疗方法是消除和控制症状。幸运的是,有各种各样的印度草药疗法(如番木瓜、西葫芦等)可以通过加强免疫系统和控制体温过高来帮助解决这个问题。这篇综述文章提供了登革热病毒感染、临床症状、诊断、缓解和治疗的全面概述,重点是印度草药和草药疗法。
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引用次数: 8
A Prospective, Observational Study of Use Combination Silodosin 8 mg Plus Serenoa Repens, Urtica Dioica, Cucurbita Pepo (Rotaprost) Compared With Silodosin 8 mg Alone in Treatment Patients with Benign Prostate Hyperplasia 西洛多辛8 mg联合西洛多辛8 mg治疗良性前列腺增生与单独西洛多辛8 mg联合西洛多辛8 mg治疗良性前列腺增生的前瞻性观察研究
Pub Date : 2022-09-01 DOI: 10.1016/j.ccmp.2022.100043
Denis V. Krakhotkin , Volodymyr A. Chernylovskyi , Ruslan A. Bugaev , Dmitry N. Pikhovkin

Background

Benign prostatic hyperplasia (BPH) is one of the most common causes of lower urinary tract symptoms (LUTS) in older men. Nowadays, there are several plant extracts used for the treatment of LUTS due to BPH.

Objective

The aim of this study is to compare the effect of combining silodosin 8 mg with Serenoa repens, Urtica dioica, Cucurbita pepo (Rotaprost 530 mg) compared to silodosin 8 mg and Rotaprost 530 mg alone in patients with LUTS/BPH.

Methods

Four hundred five men with symptomatic BPH were recruited for the study from June 2020 to January 2021. Three hundred eighty-nine patients were followed up for 6 months. All participants provided written informed consent. This prospective study included analysis of three treatment groups: Group I patients (n = 130) received a combination of silodosin 8 mg and Rotaprost 530 mg (containing a dry extract of Serenoa repens 80 mg, a dry extract of Urtica dioica 150 mg, a dry extract of Cucurbita pepo seeds 200 mg, zinc (in the form of zinc picolinate) 0.105 mg, and selenium (as sodium selenite) 22.5 µg); the group II (n = 129) received silodosin 8 mg alone, and the group III (n = 130) received Rotaprost 530 mg alone. Outcomes were measured by changes from baseline in International Prostate Symptom Score (IPPS) total score, PSA value, prostate volume, residual urine after urination, and maximum flow rate. Statistical significance was set at P < 0.05.

Results

In group I, IPSS, prostate volume, and maximum urinary flow rate (Qmax) improved significantly (P < 0.05) compared with groups II and III during follow-up. Prostate volume in group I showed a significant decrease only during 6 months of therapy (P < 0.05). No serious adverse effects were registered in the three groups.

Conclusion

Combination therapy with silodosin 8 mg significantly reduced LUTS/BPH, Qmax, and prostate volume compared with silodosin 8 mg alone. Rotaprost 530 mg can also reduce PSA by at least 20.6−25.7% after 6-months of treatment.

背景:良性前列腺增生(BPH)是老年男性下尿路症状(LUTS)最常见的原因之一。目前,有几种植物提取物用于治疗由BPH引起的LUTS。目的:比较西洛多辛8mg联合罗塔前列素530mg治疗LUTS/BPH患者的疗效,比较西洛多辛8mg联合罗塔前列素530mg治疗LUTS/BPH的疗效。方法从2020年6月至2021年1月招募了450名有症状性前列腺增生的男性进行研究。389例患者随访6个月。所有参与者均提供书面知情同意书。这项前瞻性研究包括三个治疗组的分析:第一组患者(n = 130)接受西洛多辛8 mg和罗他前列素530 mg的联合治疗(其中含有雪蕊花的干提取物80 mg,荨麻疹的干提取物150 mg,瓜籽的干提取物200 mg,锌(以吡啶甲酸锌的形式)0.105 mg,硒(以亚硒酸钠的形式)22.5µg);II组(n = 129)单用西洛多辛8 mg, III组(n = 130)单用罗他前列素530 mg。结果通过国际前列腺症状评分(IPPS)总分、PSA值、前列腺体积、排尿后残余尿和最大尿流量的基线变化来衡量。P <有统计学意义;0.05.结果I组患者IPSS、前列腺体积、最大尿流率(Qmax)明显改善(P <随访时,与II组和III组比较,p < 0.05)。第一组前列腺体积仅在治疗6个月期间出现显著下降(P <0.05)。三组均未见严重不良反应。结论与单用西洛多辛8 mg相比,西洛多辛8 mg联合治疗可显著降低LUTS/BPH、Qmax和前列腺体积。治疗6个月后,罗他前列素530 mg也能使PSA降低至少20.6 - 25.7%。
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引用次数: 0
Jieduquyuziyin Prescription Suppresses the Inflammatory Activity of Macrophages via NOTCH1/NF-κB Pathway 解毒祛瘀子饮方通过NOTCH1/NF-κB通路抑制巨噬细胞炎症活性
Pub Date : 2022-09-01 DOI: 10.1016/j.ccmp.2022.100039
Sijia Fang , Lina Ji , Shan Wu , Xiaoxuan Yang , Kepeng Yang , Yongsheng Fan

Background

Jieduquyuziyin prescription (JP) is a traditional Chinese medicine (TCM) formula, which has been applied to the treatment of systemic lupus erythematosus (SLE) for decades, and its efficacy and safety have been confirmed in clinical practice. However, little is known about its molecular mechanism.

Objective

To explore the effects of JP on macrophages' inflammatory activity and NOTCH1/NF-κB pathway.

Methods

The JP-treated serum was prepared to determine its optimal concentration. Given the fact that active components in rats' serum might affect the results, control serum without JP components was prepared simultaneously. Lipopolysaccharide (LPS) was used to activate RAW264.7, and the cells were interfered with DAPT (NOTCH1 blocker), control serum, and JP-treated serum, respectively. After the above intervention, the expression of NOTCH1 and RBPJ, the nuclear translocation of NF-κB, and the extracellular release of IL6, TNFα, and NO, was evaluated by real-time reverse transcription-polymerase chain reaction (RT-PCR), western blotting (WB), enzyme-linked immunosorbent assay (ELISA), and Griess method.

Results

Both DAPT and JP-treated serum could significantly suppress the expression of NOTCH1 and RBPJ induced by LPS, as well as the nuclear translocation of NF-κB, leading to the decreased release of IL6, TNFα, and NO, while control serum had little effect on macrophage activity and NOTCH1/NF-κB pathway.

Conclusion

These results demonstrated the effects of JP on macrophage activation and pro-inflammatory response and suggested that the molecular mechanism of JP might attribute to the inhibition of the NOTCH1/NF-κB pathway. Besides, previous studies suggested that paeoniflorin and ferulic acid are two major effective components in JP. In subsequent experiments, we would further explore the effects of these two components on MRL/lpr mice and macrophage activity.

解毒祛瘀子饮方(JP)是一种中药方剂,用于治疗系统性红斑狼疮(SLE)已有几十年的历史,其有效性和安全性已在临床实践中得到证实。然而,人们对其分子机制知之甚少。目的探讨JP对巨噬细胞炎症活性及NOTCH1/NF-κB通路的影响。方法制备jp处理血清,确定其最佳浓度。考虑到大鼠血清中活性成分可能影响结果,同时制备不含JP成分的对照血清。用脂多糖(LPS)激活RAW264.7,并分别用DAPT (NOTCH1阻滞剂)、对照血清和jp处理血清干扰细胞。采用实时逆转录聚合酶链式反应(RT-PCR)、western blotting (WB)、酶联免疫吸附试验(ELISA)和Griess法检测干预后NOTCH1和RBPJ的表达、NF-κB的核易位以及细胞外il - 6、TNFα和NO的释放情况。结果DAPT和jp处理血清均能显著抑制LPS诱导的NOTCH1和RBPJ的表达以及NF-κB的核易位,导致il - 6、TNFα和NO的释放减少,而对照血清对巨噬细胞活性和NOTCH1/NF-κB通路影响不大。结论JP对巨噬细胞活化和促炎反应的影响,提示JP的分子机制可能与抑制NOTCH1/NF-κB通路有关。此外,已有研究表明,芍药苷和阿魏酸是JP的主要有效成分。在后续实验中,我们将进一步探讨这两种成分对MRL/lpr小鼠及巨噬细胞活性的影响。
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引用次数: 0
Effect of Ningxin-Yishen Formula on D-galactose-induced Premature Ovarian Insufficiency Mice by Inhibiting p53 宁心益肾方通过抑制p53对d -半乳糖诱导的小鼠卵巢早衰的影响
Pub Date : 2022-08-27 DOI: 10.1016/j.ccmp.2022.100068
Jiawen Ma , Zaiyang Zhang , Xin Yan , Cenglin Xu , Yizhou Zhang

Background

The prevalence of premature ovarian insufficiency (POI) is gradually increasing, safer and more effective treatments are urgently needed.

Objective

The aim of this study was to evaluate the effects of Ningxin-Yishen formula (NXYSF) on D-galactose-induced POI mice as well as to shed a light on its potential mechanisms.

Methods

Six to eight weeks old female C57BL/6 mice were used in this study and randomly divided into six groups: control group; model group; estradiol valerate (EV) treatment group and NXYSF treatment group with graded doses (9.5, 19, and 38 g·kg−1/d). Both EV and NXYSF treatments were initiated at the 15th day of modeling and lasted for 28 days. Afterwards, the ovarian function was evaluated in each group by analyzing the proportion of primordial follicles as well as the serum sex hormone levels. Furthermore, network pharmacology approach was performed to elucidate the potential targets of NXYSF, which was verified through western blotting experiments finally.

Results

NXYSF could significantly reverse the inefficiency of weight gain caused by POI, and promote the development of primordial follicles. In addition, it could restore the abnormal serum anti-Müllerian hormone (AMH), estradiol (E2), luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Moreover, some crucial key gene targets including TP53 were as propose to be relate with the effect of NXYSF through network pharmacology analysis. Last but importantly, western blotting experiments confirmed that NXYSF could inhibit the expression of p53 protein in mouse ovaries.

Conclusion

Our findings proposed that NXYSF might be an effective alternative treatment for POI.

背景卵巢功能不全(POI)的发病率正在逐渐上升,迫切需要更安全、更有效的治疗方法。目的观察宁心益肾方对d -半乳糖诱导的POI小鼠的影响,并探讨其作用机制。方法选用6 ~ 8周龄雌性C57BL/6小鼠,随机分为6组:对照组;模型组;戊酸雌二醇(EV)治疗组和NXYSF治疗组按剂量分级(9.5、19和38 g·kg−1/d)。EV和NXYSF均于造模第15天开始处理,持续28 d。然后,通过分析各组原始卵泡比例和血清性激素水平来评估卵巢功能。此外,采用网络药理学方法阐明NXYSF的潜在靶点,最后通过western blotting实验进行验证。结果snxysf能明显扭转POI引起的增重效率低下,促进原始卵泡发育。此外,它还能恢复异常的血清抗勒氏激素(AMH)、雌二醇(E2)、促黄体生成素(LH)和促卵泡激素(FSH)。此外,通过网络药理学分析,提出了包括TP53在内的一些关键基因靶点与NXYSF的作用有关。最后,western blotting实验证实NXYSF可以抑制小鼠卵巢中p53蛋白的表达。结论NXYSF可能是治疗POI的有效替代方法。
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引用次数: 0
Polyphenol-rich Fraction of Terminalia catappa Prevents Chronic Lead Acetate Induced Oxidative Stress and Cardiorenal Toxicities in Rats 蛇麻多酚提取物对大鼠慢性醋酸铅氧化应激及心肾毒性的预防作用
Pub Date : 2022-06-01 DOI: 10.1016/j.ccmp.2022.100032
Temitayo Ajibade , Adedeji Adebayo , Ademola Oyagbemi , Temidayo Omobowale

Background

Lead (Pb), a naturally occurring environmental contaminant, has been implicated in several pathological conditions of the cardiovascular and renal systems.

Objective

The study was designed to evaluate the modulatory roles of the polyphenol-rich fraction of Terminalia catappa on chronic lead acetate-induced cardiovascular and renal toxicities in rats.

Methods

Thirty-six rats were randomly selected and divided into six groups of six rats each. Pb toxicity was induced by the administration of 100 mg/L Pb in drinking water for 12 weeks in groups B-F. Groups A and B were left untreated; groups C and D were treated with polyphenol-rich fraction of Terminalia catappa [PRFTC (100 and 200 mg/kg b.w.)]; vitamin E (50 mg/kg b.w.) and lisinopril (10 mg/kg b.w.) were administered to groups E and F, respectively.

Results

Exposure of rats to Pb induced significantly elevated (P < 0.05) primary haemodynamic parameters, severe disseminated congestion of blood vessels and haemorrhages in the cardiac and renal tissues, significantly elevated (P < 0.05) markers of oxidative stress markers of inflammation and myocardial infarction, but significantly decreased serum nitric oxide and the systemic antioxidants. Furthermore, rats exposed to Pb showed heightened immune-positive reactions to Caspase-3, a marker of apoptosis, in both renal and cardiac tissues. All manifestations of Pb-associated toxicities in the cardiovascular and renal systems were alleviated by the PRFTC treatment in rats.

Conclusion

The polyphenol-rich fraction of T. catappa proved effective in the reduction of oxidative stress-mediated derangements of the physiological homeostasis and decreased apoptosis in the cardiovascular and renal systems of rats chronically exposed to lead acetate toxicities and may therefore have therapeutic potential as a supplement that can be applied in chronic lead poisoning.

背景:铅(Pb)是一种天然存在的环境污染物,与心血管和肾脏系统的几种病理状况有关。目的探讨富多酚部位对醋酸铅致大鼠慢性心血管和肾毒性的调节作用。方法随机选取36只大鼠分为6组,每组6只。B-F组小鼠饮水中Pb浓度为100 mg/L,连续12周诱导铅中毒。A、B组不进行治疗;C组和D组分别用富多酚部位[PRFTC(100和200 mg/kg b.w.)]处理;E组和F组分别给予维生素E (50 mg/kg b.w)和赖诺普利(10 mg/kg b.w)。结果大鼠暴露于Pb后显著升高(P <0.05)原发性血流动力学参数,严重弥散性血管充血,心脏和肾脏组织出血,显著升高(P <血清一氧化氮和全身抗氧化剂水平均显著降低(0.05)。此外,暴露于Pb的大鼠对肾脏和心脏组织中凋亡标志物Caspase-3的免疫阳性反应增强。经PRFTC处理后,大鼠心血管和肾脏系统中铅相关毒性的所有表现均得到缓解。结论富多酚部位能有效降低醋酸铅慢性中毒大鼠氧化应激引起的生理稳态紊乱,减少心血管和肾脏系统的细胞凋亡,具有治疗慢性铅中毒的潜力。
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引用次数: 1
QSAR Applied to 4-Chloro-3-formylcoumarin Derivatives Targeting Human Thymidine Phosphorylase 靶向人胸苷磷酸化酶的4-氯-3-甲酰基香豆素衍生物的QSAR研究
Pub Date : 2022-06-01 DOI: 10.1016/j.ccmp.2022.100031
Thomas Scior , Juan Carlos Garcia-Hernandez , Hassan H. Abdallah , Christian Alexander

Background

Coumarins are secondary metabolites from the phenylpropanoid-type biosynthesis in higher plants. A plethora of potential phytopharmacological activities have been described for derivatives of the coumarin scaffold: hepatoprotective, antineoplastic, antimicrobial, antituberculosis, antiviral, anti-inflammatory anticoagulant, or antithrombotic effects.

Objective

A computer-based quantitative structure – activity relationships (QSAR) study for a series of 4‑chloro-3-formylcoumarins was carried out.

Methods

To this end we generated the 3D models of 17 published coumarin structures, calculated their physicochemical properties (descriptors) to correlate them to their experimentally known biological activities measured as inhibition concentrations to block the target enzyme activity. Our proposed approach used free molecular modeling software and applies our scripts written in the programming language R.

Results

The final multiple regression models achieved satisfactory results with a small number of descriptors – all of which were statistically significant and meaningful in the field of pharmacodynamics to develop new 3-formylcoumarins with enhanced activities targeting the human thymidine phosphorylase enzyme.

Conclusion

On theoretical grounds, our in silico research contributes in a crucial step in the field of complementary phyto-medicine. This step is located between in vivo pharmacological observations of plant extracts on ethnopharmacological, preclinical or controlled clinical levels and the need to identify – at an atomic scale – all those plant ingredients responsible for the biological actions under scrutiny. Our simulations shed light on the modification of phyto-medicine’s physicochemical properties to enhance the interaction with their biomolecular target in the patient's body.

香豆素是高等植物苯丙类生物合成的次生代谢产物。香豆素支架衍生物具有多种潜在的植物药理学活性:保肝、抗肿瘤、抗菌、抗结核、抗病毒、抗炎、抗凝或抗血栓作用。目的对一系列4 -氯-3-甲酰基香豆素进行定量构效关系(QSAR)研究。为此,我们生成了17种已发表香豆素结构的三维模型,计算了它们的物理化学性质(描述符),将它们与实验已知的生物活性(抑制浓度)相关联,以阻断目标酶的活性。我们的方法使用了免费的分子建模软件,并应用了我们用编程语言r编写的脚本。结果最终的多元回归模型在少量描述符的情况下获得了令人满意的结果,这些描述符在药效学领域都具有统计学意义,对于开发出针对人胸腺嘧啶磷酸化酶活性增强的新型3-甲酰基香豆素具有重要意义。结论从理论上讲,我们的硅片研究为植物互补医学领域迈出了关键的一步。这一步骤位于对植物提取物在民族药理学、临床前或临床控制水平上的体内药理学观察和需要在原子尺度上识别所有负责被审查的生物作用的植物成分之间。我们的模拟揭示了植物药的物理化学性质的修改,以加强与患者体内的生物分子靶点的相互作用。
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引用次数: 1
Chemosensitizer Effect of Violacein on Cisplatin-treated Bladder Cancer Cells 紫堇素对顺铂治疗的膀胱癌细胞的化学增敏作用
Pub Date : 2022-06-01 DOI: 10.1016/j.ccmp.2022.100036
Diego Alem , Lucía Canclini , Susana Castro-Sowinski , Wilner Martínez-López

Background

Bladder cancer is the tenth most common cancer worldwide. Considering its high prevalence (vulnerability to multiple recurrences and progression despite local therapy), which leads to a substantial health service burden, it becomes necessary to develop new strategies to increase the effectiveness of bladder tumor therapy. Natural compounds with antiproliferative effect on cancer cells could be a good choice for co-adjuvant chemotherapy. Microorganisms are one of the main sources for natural compounds. Pigments extracted from the cold-adapted microorganisms can contribute to the development of a broader range of applications in biotechnology. Violacein is a purple pigment commonly produced by many bacterial strains. We have previously shown that very low concentrations of violacein extracted from Janthinobacterium sp. produced an antiproliferative effect on HeLa cells.

Objective

With the aim to determine if violacein has an antiproliferative activity on bladder cancer cells, as well as to test if it has synergistic effects on cisplatin treated cells in vitro, T24 and 253J cell lines (derived bladder cancer cells from carcinoma in situ and retroperitoneal metastasis, respectively) were exposed to different concentrations of violacein in the presence or absence of cisplatin.

Methods

i) Resazurin assay and flow cytometry were performed in two bladder cancer-derived cell lines, namely T24 and 253J, to see if violacein affects cell viability and induce cell death. ii) To find out whether violacein sensitizes bladder cancer cells to cisplatin, the drug interaction among different doses of cisplatin and violacein was analyzed, as well their combination index was determined. iii) The effect of violacein to induce primary genetic damage was determined through the analysis of induced micronuclei frequency and γH2AX foci, as well as performing the comet assay.

Results

The half-maximal inhibitory concentration of violacein at 24 h for both cell lines were around 500 nM, and decreased below 400 nM in combination with 10 µM of cisplatin, indicating antiproliferative and sensitizing effects of violacein to cisplatin in both cell lines tested. A clear cell cycle delay, as well as an increase in the percentage of cell death was observed by flow cytometry at 300 nM of violacein, either alone or in combination with cisplatin. On the other hand, the analysis of the micronucleus frequency did not evidence an increase in genetic damage. Moreover, in combined treatments with cisplatin there was a slight decrease on micronucleus induction. Besides, the induction of genetic damage was not observed through comet assay when cells were treated with violacein alone, however, when cells were treated with violacein in the presence of cisplatin (10 µM). The production of genetic damage was diminished in T24 or 253J cells. By the same token, increase in

背景:膀胱癌是全球第十大常见癌症。考虑到其高患病率(尽管局部治疗,但容易多次复发和进展),这导致了巨大的卫生服务负担,有必要制定新的策略来提高膀胱肿瘤治疗的有效性。对癌细胞具有抗增殖作用的天然化合物可能是辅助化疗的良好选择。微生物是天然化合物的主要来源之一。从冷适应微生物中提取的色素在生物技术中具有广泛的应用前景。紫紫素是一种紫色色素,通常由许多菌株产生。我们之前已经证明,从Janthinobacterium sp.中提取的极低浓度的violacein对HeLa细胞具有抗增殖作用。目的探讨紫紫素对膀胱癌细胞是否具有抗增殖作用,并对体外顺铂处理的膀胱癌细胞T24和253J细胞系(来源于原位癌和腹膜后转移的膀胱癌细胞)是否具有协同作用。方法采用reazurin法和流式细胞术对2株膀胱癌源性细胞株T24和253J进行检测,观察violacein是否影响细胞活力和诱导细胞死亡。ii)分析不同剂量的顺铂与紫堇素的药物相互作用,并测定其联合指数,以确定紫堇素是否使膀胱癌细胞对顺铂致敏。iii)通过诱导微核频率和γ - h2ax焦点分析,以及彗星实验,确定violacein诱导原发性遗传损伤的效果。结果violacein在24 h对两种细胞系的半最大抑制浓度均在500 nM左右,在400 nM以下,与10µM顺铂联合作用时,violacein对两种细胞系均有抗增殖和增敏作用。通过流式细胞术观察到,在300 nM紫紫素浓度下,无论是单独使用还是与顺铂联合使用,细胞周期明显延迟,细胞死亡百分比增加。另一方面,对微核频率的分析没有证据表明遗传损伤增加。此外,与顺铂联合治疗微核诱导略有下降。此外,通过彗星实验,当细胞单独用violacein处理时,没有观察到诱导遗传损伤,而当细胞在顺铂(10µM)存在的情况下用violacein处理时,则没有观察到诱导遗传损伤。在T24和253J细胞中,基因损伤的产生减少。同样,在两种细胞系中,在任何测试剂量下,均未观察到紫罗兰素对γ - h2ax聚焦频率的增加。结论堇菜素对膀胱癌细胞株具有体外抗增殖作用,使其对顺铂敏感。有趣的是,在测试剂量下,紫罗兰碱不会诱导遗传毒性并降低顺铂产生的遗传毒性作用。
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引用次数: 3
期刊
Clinical complementary medicine and pharmacology
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