Muyenga Tumelo Akapelwa, Bamitale Samuel K Dominion, Kibuule Dan, Sithole Simbarashe, Mukanganyama Stanley, Rudolph Carlen, Venables Luanne, Hattingh Anna C, van de Venter Maryna, Ezeala Christian Chinyere
Department of Physiological Sciences, School of Medicine and Health Sciences, Mulungushi University, P.O. Box 60009, Livingstone, Zambia.
Department of Pharmacology and Therapeutics, Faculty of Health and Veterinary Sciences, University of Namibia, Windhoek, Namibia.
BMC Complement Med Ther. 2024 Jun 12;24(1):230. doi: 10.1186/s12906-024-04510-5.
Diabetes affects 75% of people in low-income countries, where conventional drugs like metformin are available, but newer drugs like alpha-glucosidase inhibitors are not accessible to most Southern African patients.
To evaluate the α-glucosidase and α-amylase inhibitory activities of fractionated aqueous extracts of Kigelia africana fruit (KAFE) and their phytochemical fingerprints using gas chromatography-mass spectrometry (GC-MS).
We studied K. africana fruit fractions' inhibitory effects on alpha-glucosidase and alpha-amylase using bioassay-guided fractionation, and analyzed their phytochemical profiles with GC-MS.
Both the aqueous extract and ethyl acetate fraction of the aqueous extract exhibited a low dose-dependent inhibition of alpha-amylase activity (p < 0.0001). At a concentration of 500 μg/mL, the aqueous extract caused an alpha-glucosidase inhibition of 64.10 ± 2.7%, with an estimated IC50 of 193.7 μg/mL, while the ethyl acetate fraction had an inhibition of 89.82 ± 0.8% and an estimated IC50 of 10.41 μg/mL. The subfraction G, which had the highest alpha-glucosidase inhibitory activity at 85.10 ± 0.7%, had significantly lower activity than the ethyl acetate fraction. The most bioactive fraction was found to contain 11"(2-cyclopenten-1-yl) undecanoic acid, ( +)- and cyclopentane undecanoic acid as well as the indole alkaloids Akuammilan-17-ol-10-methoxy, N-nitroso-2-methyl-oxazolidine and epoxide Oxirane2.2″ -(1.4-butanediyl) bis-.
The K. africana fruit fraction demonstrated significant alpha-glucosidase inhibitory activity, while its alpha-amylase inhibitory activity was limited. This study suggests a potential natural alpha-glucosidase inhibitor and phytocompounds that could serve as leads for developing antidiabetic agents.
糖尿病影响着低收入国家75%的人口,在这些国家,像二甲双胍这样的传统药物是可以获得的,但大多数南部非洲患者无法获得像α-葡萄糖苷酶抑制剂这样的新型药物。
利用气相色谱-质谱联用仪(GC-MS)评估非洲吊灯树果实分级水提取物(KAFE)的α-葡萄糖苷酶和α-淀粉酶抑制活性及其植物化学指纹图谱。
我们采用生物测定导向分级法研究了非洲吊灯树果实各组分对α-葡萄糖苷酶和α-淀粉酶的抑制作用,并利用GC-MS分析了它们的植物化学特征。
水提取物及其乙酸乙酯级分均表现出低剂量依赖性的α-淀粉酶活性抑制作用(p < 0.0001)。在500μg/mL的浓度下,水提取物对α-葡萄糖苷酶的抑制率为64.10 ± 2.7%,估计IC50为193.7μg/mL,而乙酸乙酯级分的抑制率为89.82 ± 0.8%,估计IC50为10.41μg/mL。亚组分G的α-葡萄糖苷酶抑制活性最高,为85.10 ± 0.7%,但其活性显著低于乙酸乙酯级分。发现生物活性最高的级分含有11"(2-环戊烯-1-基)十一烷酸、(+)-环戊烷十一烷酸以及吲哚生物碱 Akuammilan-17-ol-10-methoxy、N-亚硝基-2-甲基-恶唑烷和环氧化物环氧乙烷2.2″ -(1.4-丁二醇)双-。
非洲吊灯树果实级分表现出显著的α-葡萄糖苷酶抑制活性,而其α-淀粉酶抑制活性有限。本研究表明一种潜在的天然α-葡萄糖苷酶抑制剂和植物化合物,可作为开发抗糖尿病药物的先导物。