El-Shiekh Riham A, Shalabi Akram A, Al-Hawshabi Othman S S, Ayman Salkini Mohamad, Abdel-Sattar Essam
Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
Department of Biology, Faculty of Science, University of Aden, Aden, Yemen.
Steroids. 2023 May;193:109198. doi: 10.1016/j.steroids.2023.109198. Epub 2023 Feb 11.
From the dichloromethane (DCM) fraction of the crude ethanolic extract of Caralluma awdeliana, four pregnane glycosides and a flavone glycoside were isolated using a bio-guided isolation approach. The different extracts of C. awdeliana were subjected to in vitro enzyme inhibitory assays of anticholinesterases (AChE and BChE) and anti-inflammatory (COXs and 5-LOX). The highest inhibitory activity was exhibited by DCM fraction against COX-1, COX-2, and 5-LOX with IC of 4.8 ± 0.5 μg/mL, 0.68 ± 0.2 μg/mL, and 39.5 ± 3.0 μg/mL, respectively. The DCM showed also a moderate activity against AChE (IC 384.72 ± 3.6 μg/mL), and BChE (IC 384.72 ± 3.6 μg/mL). The repeated chromatography of DCM fraction resulted in the isolation of two new pregnane glycosides, namely awdeliosides A (1) and B (4), two known ones, namely caratuberosides B and D, along with the known flavone glycoside identified as luteolin 4 -O-neohesperidoside. All the isolated compounds were tested for their in vitro enzyme inhibitory assays. Among the isolated compounds, awdelioside B (4) showed the most potent effect against COX-1 with IC value of 10.99 ± 0.35 μM, compared to standard celecoxib (IC 230.74 ± 2.62 μM). All the isolated compounds showed weak anticholinesterase, except a moderate activity observed for awdelioside B (4) against BChE with IC value of 15.63 ± 3.5 μM, compared to standard donepezil (IC 0.77 ± 0.0088 μM).
从牛角瓜乙醇粗提物的二氯甲烷（DCM）部分，采用生物导向分离方法分离得到了4种孕甾烷糖苷和1种黄酮糖苷。对牛角瓜的不同提取物进行了体外抗胆碱酯酶（乙酰胆碱酯酶和丁酰胆碱酯酶）和抗炎（环氧化酶和5-脂氧合酶）的酶抑制试验。DCM部分对COX-1、COX-2和5-脂氧合酶表现出最高的抑制活性，IC50分别为4.8±0.5μg/mL、0.68±0.2μg/mL和39.5±3.0μg/mL。DCM对乙酰胆碱酯酶（IC50为384.72±3.6μg/mL）和丁酰胆碱酯酶（IC50为384.72±3.6μg/mL）也表现出中等活性。DCM部分经反复柱色谱分离得到2种新的孕甾烷糖苷，即牛角瓜苷A（1）和B（4），2种已知的孕甾烷糖苷，即卡拉图贝苷B和D，以及鉴定为木犀草素4'-O-新橙皮糖苷的已知黄酮糖苷。对所有分离得到的化合物进行了体外酶抑制试验。在分离得到的化合物中，牛角瓜苷B（4）对COX-1表现出最显著的抑制作用，IC50值为10.99±0.35μM，而标准塞来昔布的IC50值为230.74±2.62μM。所有分离得到的化合物均表现出较弱的抗胆碱酯酶活性，除了牛角瓜苷B（4）对丁酰胆碱酯酶表现出中等活性，IC50值为15.63±3.5μM，而标准多奈哌齐的IC50值为0.77±0.0088μM。
