Alkadi Khalid A A, Ashraf Kamran, Adam Aishah, Shah Syed Adnan Ali, Taha Muhammad, Hasan Mizaton Hazizul, John Cinimathew, Salleh Razali Mohamed, Ahmad Wasim
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.
Atta-ur-Rahman Institute for Natural Product Discovery, UniversitiTeknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia.
J Pharm Bioallied Sci. 2021 Jan-Mar;13(1):116-122. doi: 10.4103/jpbs.JPBS_279_19. Epub 2020 Dec 21.
The aim of the present study was to isolate and evaluate cytotoxicity and anti-inflammatory activities of new novel compounds isolated from .
Dried root of was extracted under reflux with methyl alcohol, fractionated through the vacuum liquid chromatography technique, and evaporated and then purified the compounds using column chromatography and preparative thin-layer chromatography. THP-1 cells were treated with amentoflavone, 5,7,4'-hydroxyflavonoid, and stigmasterol with various concentrations (0-30 µg/mL) and then incubated with MTS reagent for 2h. Treatment was done for 24, 48, and 72h. Then, effects of these compounds were also tested on PGE TNF-, and IL-6 expression in human THP-1-derived macrophage cells for 24h.
Three new compounds such as amentoflavone, 5,7,4'-hydroxyflavonoid, and stigmasterol were isolated. After 24h of incubation, a significant decrease in cell viability was reported with IC values of amentoflavone, 5,7,4'- hydroxyflavonoid, and stigmasterol (21 µg/mL ≡ 38 M), (18 µg/mL ≡ 66 M) and (20 µg/mL ≡ 48.5 M), respectively. Whereas for 48 and 72h treatment showed a less decreased cell viability compared with 24h treatment. These compounds also showed a significant reduction in the production of TNF-, IL-6, and PGE in a dose-dependent manner.
The isolated new compounds showed significant cytotoxicity and anti-inflammatory effects.
本研究的目的是分离并评估从……中分离出的新型化合物的细胞毒性和抗炎活性。
……的干燥根用甲醇回流提取，通过真空液相色谱技术进行分离，蒸发后再用柱色谱和制备薄层色谱法纯化化合物。用不同浓度（0 - 30 µg/mL）的穗花杉双黄酮、5,7,4'-羟基黄酮和豆甾醇处理THP - 1细胞，然后与MTS试剂孵育2小时。处理时间为24、48和72小时。然后，还检测了这些化合物对人THP - 1衍生巨噬细胞中PGE、TNF - 和IL - 6表达的影响，处理时间为24小时。
分离出了三种新化合物，即穗花杉双黄酮、5,7,4'-羟基黄酮和豆甾醇。孵育24小时后，据报道穗花杉双黄酮、5,7,4'-羟基黄酮和豆甾醇的IC值分别为（21 µg/mL ≡ 38 M）、（18 µg/mL ≡ 66 M）和（20 µg/mL ≡ 48.5 M），细胞活力显著下降。而在48和72小时处理时，与24小时处理相比，细胞活力下降较少。这些化合物还以剂量依赖性方式显著降低了TNF - 、IL - 6和PGE的产生。
分离出的新化合物显示出显著的细胞毒性和抗炎作用。
