Biologically Active Withanolides from Withania coagulans

详细信息    查看全文

• 作者：Ihsan-ul-Haq ; Ui Joung Youn ; Xingyun Chai ; Eun-Jung Park ; Tamara P. Kondratyuk ; Charles J. Simmons ; Robert P. Borris ; Bushra Mirza ; John M. Pezzuto ; Leng Chee Chang
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：January 25, 2013
• 年：2013
• 卷：76
• 期：1
• 页码：22-28
• 全文大小：302K
• 年卷期：v.76,no.1(January 25, 2013)
• ISSN：1520-6025

文摘

Bioassay-directed isolation and purification of the crude extract of Withania coagulans, using two assays for cancer chemopreventive mechanisms, led to the isolation of three new steroidal lactones, withacoagulin G (1), withacoagulin H (2), and withacoagulin I (3), along with six known derivatives (4鈥?/i>9). The structures and absolute stereochemistry of these compounds were determined on the basis of spectroscopic analyses, including 1D and 2D NMR, mass spectrometry, and CD analyses. The structure of 1 was confirmed using X-ray diffraction methods. Compounds 1鈥?b>9 inhibited nitric oxide production in lipopolysaccharide-activated murine macrophage RAW 264.7 cells with IC₅₀ values in the range of 1.9鈥?8.2 渭M. Compounds 1 and 2 were the most active (IC₅₀ 3.1 and 1.9 渭M, respectively). Withanolides 1鈥?b>9 exhibited inhibition of tumor necrosis factor-伪 (TNF-伪)-induced nuclear factor-kappa B (NF-魏B) activation with IC₅₀ values in the range of 1.60鈥?2.4 渭M.