Antiparasitic and antimicrobial indolizidines from the leaves of Prosopis glandulosa var. glandulosa.
Antiparasitic and antimicrobial indolizidines from the leaves of Prosopis glandulosa var. glandulosa.
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DOI：
10.1055/s-0030-1270906
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发表时间：
2011-09
期刊：
影响因子：
2.7
通讯作者：
Muhammad I
中科院分区：
文献类型：
--
作者：
Rahman AA;Samoylenko V;Jacob MR;Sahu R;Jain SK;Khan SI;Tekwani BL;Muhammad I
从腺牧豆（Prosopis glandulosa var.）从美国内华达州采集的P. glandulosa;而另外两种已知的吲哚嗪类化合物juliprosopine（6）和juliprosine（7）分离自美国德克萨斯州采集的P. glandulosa叶。使用NMR和MS技术的组合确定化合物1和7的结构。化合物7对恶性疟原虫D 6和W2株表现出有效的抗疟原虫活性，IC 50值分别为170和150 ng/mL，而发现1活性较低（IC 50值为560和600 ng/mL）。两种化合物在高达23800 ng/mL的浓度下均无VERO细胞毒性。在THP 1巨噬细胞培养物中评价了吲哚嗪类药物对杜氏利什曼原虫前鞭毛体、无鞭毛体和无鞭毛体的抗利什曼原虫活性。当针对巨噬细胞培养物进行测试时，发现叔碱（1、3、6）比季盐（2、5、7）更有效，分别显示出0.8-1.7 μg/mL和3.1-6.0 μg/mL的IC 50值。此外，化合物7对新生隐球菌有较强的抗真菌活性，对胞内分枝杆菌有较强的抗菌活性，而化合物1仅对隐球菌有较强的抗菌活性。对其他生物的活性较弱。
A new indolizidine alkaloid, named Δ1,6-juliprosopine (1), together with previously known indolizidine analogs (2–6), was isolated from the leaves of Prosopis glandulosa var. glandulosa, collected from Nevada, USA; while two other known indolizidines juliprosopine (6) and juliprosine (7) were isolated from P. glandulosa leaves collected in Texas, USA. The structures of compound 1 and 7 were determined using a combination of NMR and MS techniques. Compound 7 exhibited potent antiplasmodial activity against Plasmodium falciparum D6 and W2 strains with IC50 values of 170 and 150 ng/mL, respectively, while 1 was found to be less active (IC50 values 560 and 600 ng/mL). Both the compounds were devoid of VERO cells toxicity up to a concentration of 23800 ng/mL. The antileishmanial activity of indolizidines was evaluated against Leishmania donovani promastigotes, axenic amastigotes and amastigotes in THP1 macrophage cultures. When tested against macrophage cultures, the tertiary bases (1, 3, 6) were found to be more potent than quaternary salts (2, 5, 7), displayed IC50 values between 0.8–1.7 μg/mL and 3.1–6.0 μg/mL, respectively. In addition, compound 7 showed potent antifungal activity against Cryptococcus neoformans and antibacterial activity against Mycobacterium intracellulare, while 1 was potent only against C. neoformans and weakly active against other organisms.
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影响因子：
1.8
作者：
DATWYLER, P;OTTLONGONI, R;HESSE, M
通讯作者：
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影响因子：
1.9
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影响因子：
5.1
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影响因子：
1.8
作者：
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通讯作者：
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影响因子：
5.2
作者：
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通讯作者：
Neubert, BJ