Alpha-glucosidase inhibitory and antiplasmodial properties of terpenoids from the leaves of Buddleja saligna Willd

Alpha-glucosidase inhibitory and antiplasmodial properties of terpenoids from the leaves of Buddleja saligna Willd
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DOI:
10.3109/14756366.2014.1003927
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发表时间:
2016-01-02
影响因子:
5.6
通讯作者:
van Staden, Johannes
van Staden, Johannes
中科院分区:
医学2区
文献类型:
--
作者:
Chukwujekwu, Jude C.;Rengasamy, Kannan R. R.;van Staden, Johannes

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在我们继续寻找具有生物活性的植物来源的天然产物(S)的过程中,南非药用植物醉鱼草被筛选出与其传统用途一致,具有抗糖尿病(酵母菌α-葡萄糖苷酶抑制)和抗疟原虫(针对恶性疟原虫氯喹敏感株(NF54))的活性。正己烷组分具有最好的抗糖尿病活性(IC_(50)=260+/-0.112µg/ml)和抗疟原虫活性(IC_(50)=8.5+/-1.6µg/ml)。采用活性导向分级法,首次从该种植物中分离得到3个已知的萜类化合物(白桦酸、桦木酮和菠萝醇)。这些化合物表现出不同程度的生物活性(抗糖尿病:27.31mUg/ml;=C-50>=5.6mU/ml;抗疟原虫:14mUg/ml;=C-50>=2mUg/ml),毒性非常小。
In our continuing search for biologically active natural product(s) of plant origin, Buddleja saligna, a South African medicinal plant, was screened in line with its traditional use for antidiabetic (yeast alpha glucosidase inhibitory) and antiplasmodial (against a chloroquine sensitive strain of Plasmodium falciparum (NF54)) activities. The hexane fraction showed the most promising activity with regards to its antidiabetic (IC50=260 +/- 0.112 mu g/ml) and antiplasmodial (IC50=8.5 +/- 1.6 mu g/ml) activities. Using activity guided fractionation three known terpenoids (betulonic acid, betulone and spinasterol) were isolated from this species for the first time. The compounds displayed varying levels of biological activities (antidiabetic: 27.31 mu g/ml >= C-50 >= 5.6 mu g/ml; antiplasmodial: 14 mu g/ml >= C-50 >= 2 mu g/ml) with very minimal toxicity.