Lee Seoung Rak, Lee Bum Soo, Yu Jae Sik, Kang Heesun, Yoo Min Jeong, Yi Sang Ah, Han Jeung-Whan, Kim Sil, Kim Jung Kyu, Kim Jin-Chul, Kim Ki Hyun
School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea.
Department of Chemistry, Princeton University, NJ, United States.
J Ginseng Res. 2022 May;46(3):357-366. doi: 10.1016/j.jgr.2021.09.004. Epub 2021 Oct 6.
(Solanaceae), generally known as Indian ginseng, is a medicinal plant that is used in Ayurvedic practice for promoting health and longevity. This study aims to identify the bioactive metabolites from Indian ginseng and elucidate their structures.
Withanolides were purified by chromatographic techniques, including HPLC coupled with LC/MS. Chemical structures of isolated withanolides were clarified by analyzing the spectroscopic data from 1D and 2D NMR, and HR-ESIMS experiment. Absolute configurations of the withanolides were established by the application of NMR chemical shifts and ECD calculations. Anti-adipogenic activities of isolates were evaluated using 3T3-L1 preadipocytes with Oil Red O staining and quantitative real-time PCR (qPCR).
Phytochemical examination of the roots of Indian ginseng afforded to the isolation of six withanolides (-), including three novel withanolides, withasilolides G-I (-). All the six compounds inhibited adipogenesis and suppressed the enlargement of lipid droplets, compared to those of the control. Additionally, the mRNA expression levels of and , the adipocyte markers decreased noticeably following treatment with 25 μM of -. The active compounds (-) also promoted lipid metabolism by upregulating the expression of the lipolytic genes and and downregulating the expression of the lipogenic gene
The results of our experimental studies suggest that the withasilolides identified herein have anti-adipogenic potential and can be considered for the development of therapeutic strategies against adipogenesis in obesity. Our study also provides a mechanistic rationale for using Indian ginseng as a potential therapeutic agent against obesity and related metabolic diseases.
刺蒺藜(茄科),通常被称为印度人参,是一种药用植物,在阿育吠陀医学实践中用于促进健康和长寿。本研究旨在鉴定印度人参中的生物活性代谢物并阐明其结构。
通过色谱技术纯化睡茄内酯,包括高效液相色谱与液相色谱/质谱联用。通过分析一维和二维核磁共振光谱数据以及高分辨电喷雾电离质谱实验来阐明分离得到的睡茄内酯的化学结构。通过应用核磁共振化学位移和电子圆二色光谱计算来确定睡茄内酯的绝对构型。使用3T3-L1前脂肪细胞,通过油红O染色和定量实时聚合酶链反应(qPCR)评估分离物的抗脂肪生成活性。
对印度人参根进行植物化学研究,分离得到六种睡茄内酯(-),包括三种新型睡茄内酯,即睡茄西洛内酯G-I(-)。与对照组相比,所有六种化合物均抑制脂肪生成并抑制脂滴增大。此外,在用25μM的-处理后,脂肪细胞标志物和的mRNA表达水平显著下降。活性化合物(-)还通过上调脂肪分解基因和的表达以及下调脂肪生成基因的表达来促进脂质代谢。
我们的实验研究结果表明,本文鉴定的睡茄西洛内酯具有抗脂肪生成潜力,可考虑用于开发针对肥胖症中脂肪生成的治疗策略。我们的研究还为将印度人参用作抗肥胖及相关代谢疾病的潜在治疗剂提供了机制依据。