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采用计算、体外和体内方法评估胡椒(胡椒藤)提取物的抗风湿活性。

Evaluation of anti rheumatic activity of Piper betle L. (Betelvine) extract using in silico, in vitro and in vivo approaches.

机构信息

Department of Biotechnology, Kamaraj College of Engineering and Technology, Virudhunagar, Tamil Nadu, India.

Department of Biotechnology, Bharathidasan University, Tiruchirappalli, Tamil Nadu, India.

出版信息

Bioorg Chem. 2020 Oct;103:104227. doi: 10.1016/j.bioorg.2020.104227. Epub 2020 Aug 26.

DOI:10.1016/j.bioorg.2020.104227
PMID:32891004
Abstract

Rheumatoid Arthritis is a chronic, inflammatory, and systemic autoimmune disease, it affects elders worldwide. Herbal medicines have been used for the treatment of various ailments from ancient times. Betelvine (Piper betle L.) leaves have long been used in Asian countries as a medicine to relieve pain and some metabolic diseases. The present study of methanolic extract of phytochemical analysis confirms the presence of alkaloids, tannins, terpenoids, saponins, steroids, total flavonoids and total phenols. GC-MS analysis of MeOH extract of Piper betle (PBME) revealed the presence of 40 bioactive compounds. In vitro antioxidant and anti-inflammatory assays showed greater inhibitory effect. The anti-arthritic effects of PBME at 250 and 500 mg/kg concentration showed recovery from joint damage in in vivo rat model. Among the 40 GC-MS derived bioactives, 4-Allyl-1,2-Diacetoxybenzene exhibited the higher interactions with minimized binding energy to the RA targets of MMP 1 (-6.4 kcal/mol), TGF-β (-6.9 kcal/mol), IL-1β (-5.9 kcal/mol). Further, the effect of PBME extract against RA molecular disease targets (IL-1β, MMP1 and TGF- β) were studied using Real-time PCR. These results substantiate that P. betle leaves could be a source of therapeutics for the treatment of rheumatoid arthritis.

摘要

类风湿关节炎是一种慢性、炎症性和系统性自身免疫性疾病,它影响着全世界的老年人。草药在古代就被用于治疗各种疾病。胡椒(Piper betle L.)叶在亚洲国家长期以来一直被用作缓解疼痛和一些代谢疾病的药物。本研究对植物化学成分的甲醇提取物进行了分析,证实了生物碱、单宁、萜类、皂苷、甾体、总黄酮和总酚的存在。胡椒甲醇提取物(PBME)的 GC-MS 分析显示存在 40 种生物活性化合物。体外抗氧化和抗炎试验显示出更大的抑制作用。在体内大鼠模型中,PBME 在 250 和 500 mg/kg 浓度下的抗关节炎作用显示出关节损伤的恢复。在 40 种衍生自 GC-MS 的生物活性物质中,4-烯丙基-1,2-二乙酰氧基苯表现出与 MMP1(-6.4 kcal/mol)、TGF-β(-6.9 kcal/mol)、IL-1β(-5.9 kcal/mol)等 RA 靶标更高的相互作用和最小化的结合能。此外,还使用实时 PCR 研究了 PBME 提取物对 RA 分子疾病靶标(IL-1β、MMP1 和 TGF-β)的作用。这些结果证实,胡椒叶可能是治疗类风湿关节炎的一种治疗方法。

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