Adedokun Oluwasegun, Gbolade Adebayo, Ayinde Bunyaminu
Igbinedion University, College of Pharmacy, Department of Pharmacognosy, Okada, Nigeria.
University of Benin, Faculty of Pharmacy, Department of Pharmacognosy, Benin City, Nigeria.
Turk J Pharm Sci. 2022 Apr 29;19(2):180-186. doi: 10.4274/tjps.galenos.2021.48264.
Male infertility has been associated with oxidative stress-induced and/or microbial induced in some men. The use of medicinal plants to overcome oxidative stress-induced infertility cannot be over emphasized. Hence, the aim of this research was to isolate the antilipid peroxidation (an index of usage for treating oxidative stress-induced male infertility) bioactive principle from using bioactivity-guided isolation.
-Hexane fraction from the crude ethanol extract obtained by Soxhlet extraction of aerial parts (without fruit) of bitter melon, , was assessed for lipid peroxidation, followed by bioactivity-guided isolation of bioactive principles using lipid peroxidation as an index of aphrodisiac and male fertility enhancer.
Fractionation of the active -hexane fraction using vacuum liquid chromatography (VLC) gave five pooled fractions on the basis of their thin layer chromatography (TLC) characteristics (-hexane: EtOAc, 2:3, sulphuric acid spray). activity of the most active VLC fraction C was less than that of the positive control, vitamin E. Further fractionation of VLC-C by open column chromatography on silica gel led to the isolation of a compound which was purified by preparative-TLC. The purified compound, 10 mg/mL (R 0.54, TLC silica gel, -hexane: ethyl acetate; 2:3) was equipotent with vitamin E (25 mg/mL) in reducing peroxidation of polyunsaturated fatty acids . Structural elucidation by NMR (H, C) and mean mass spectroscopy confirmed the identity of the new bioactive compound as 13, 14-epoxyoleanan-3-ol-acetate.
This study scientifically validates the traditional claim of as an aphrodisiac or male fertility enhancer and suggests that 13, 14-epoxyoleanan-3-ol-acetate might be responsible for the observed activity.
在一些男性中,男性不育与氧化应激诱导和/或微生物诱导有关。使用药用植物来克服氧化应激诱导的不育再怎么强调都不为过。因此,本研究的目的是通过生物活性导向分离从[苦瓜]中分离出抗脂质过氧化(治疗氧化应激诱导的男性不育的一个指标)生物活性成分。
对通过索氏提取苦瓜地上部分(无果实)得到的粗乙醇提取物的正己烷馏分进行脂质过氧化评估,然后以脂质过氧化作为壮阳和增强男性生育能力的指标,通过生物活性导向分离生物活性成分。
使用真空液相色谱(VLC)对活性正己烷馏分进行分馏,根据其薄层色谱(TLC)特征(正己烷:乙酸乙酯,2:3,硫酸喷雾)得到五个合并馏分。活性最强的VLC馏分C的活性低于阳性对照维生素E。通过硅胶柱色谱对VLC-C进一步分馏,得到一种通过制备型TLC纯化的化合物。纯化后的化合物10 mg/mL(Rf 0.54,硅胶TLC,正己烷:乙酸乙酯;2:3)在降低多不饱和脂肪酸的过氧化方面与维生素E(25 mg/mL)等效。通过核磁共振(氢谱、碳谱)和质谱对其结构进行解析,证实新的生物活性化合物为13,14-环氧齐墩果-3-醇乙酸酯。
本研究科学地验证了[苦瓜]作为壮阳药或男性生育增强剂的传统说法,并表明13,14-环氧齐墩果-3-醇乙酸酯可能是观察到的活性的原因。