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从 中分离得到的红药醇-3-乙酸酯和 2,4-二叔丁基苯酚的抗炎和抗癌活性。

Anti-inflammatory and anticancer activities of erythrodiol-3-acetate and 2,4-di-tert-butylphenol isolated from .

机构信息

Phytochemistry and Phytopharmacology Division, Jawaharlal Nehru Tropical Botanic Garden and Research Institute, Thiruvananthapuram, Kerala, India.

University of Kerala, Thiruvananthapuram, Kerala, India.

出版信息

Nat Prod Res. 2020 Aug;34(16):2319-2322. doi: 10.1080/14786419.2018.1531406. Epub 2018 Nov 26.

DOI:10.1080/14786419.2018.1531406
PMID:30475646
Abstract

Bedd., endemic to Agasthyamala in Western Ghats in India, is traditionally used by local Kani tribes for chicken pox, head ache and snake bite. This study reports the isolation of erythrodiol-3-acetate (HU-1) and 2,4-di-tert-butylphenol (HU-2) from roots and their anti-inflammatory and anticancer activities in macrophage, skin and breast cancer cell lines. Effects of HU-1 and HU-2 treatments (50, 100 µg/mL) on gene expression profiles of pro-inflammatory cytokines TNFα, IL-6 and IL-1β, and apoptosis genes p53 and caspase 7 were studied. HU-2 exerted a significantly superior anti-inflammatory effect compared to HU-1 in all three pro-inflammatory genes. HU-2 showed a superior dose dependent anticancer effect through activation of p53 gene over HU-1 in MCF-7 cells. HU-1 exhibited a dose dependent effect on caspase 7 gene in both cell lines while HU-2 was more effective in A431. HU-2 has potential for development as a novel anti-inflammatory and anticancer agent.

摘要

贝迪(Bedd.),印度西高止山脉阿加西马拉的特有种,传统上被当地卡尼部落用于治疗水痘、头痛和蛇咬伤。本研究从根部分离出了赤酮醇-3-乙酸酯(HU-1)和 2,4-二叔丁基苯酚(HU-2),并研究了它们在巨噬细胞、皮肤和乳腺癌细胞系中的抗炎和抗癌活性。研究了 HU-1 和 HU-2 处理(50、100μg/mL)对促炎细胞因子 TNFα、IL-6 和 IL-1β以及凋亡基因 p53 和 caspase 7 的基因表达谱的影响。与 HU-1 相比,HU-2 在所有三种促炎基因中均表现出显著更强的抗炎作用。与 HU-1 相比,HU-2 通过激活 MCF-7 细胞中的 p53 基因,表现出更好的剂量依赖性抗癌作用。HU-1 在两种细胞系中均表现出剂量依赖性的 caspase 7 基因效应,而 HU-2 在 A431 中更有效。HU-2 有作为新型抗炎和抗癌药物开发的潜力。

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