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卡廷加古柯(Erythroxylum caatingae Plowman)茎提取物、馏分及分离化合物的抗菌、抗增殖和促凋亡活性

Antimicrobial, antiproliferative and proapoptotic activities of extract, fractions and isolated compounds from the stem of Erythroxylum caatingae plowman.

作者信息

Aguiar Jaciana S, Araújo Rosilma O, Do Desterro Rodrigues Maria, Sena Kêsia X F R, Batista André M, Guerra Maria M P, Oliveira Steno L, Tavares Josean F, Silva Marcelo S, Nascimento Silene C, Da Silva Teresinha Gonçalves

机构信息

Antibiotics of Departament, Federal University of Pernambuco, 50670-901, Recife, PE, Brasil.

Andrology Laboratory, Veterinary Medicine Department, Rural Federal University of Pernambuco, 52171-900, Recife, PE, Brasil.

出版信息

Int J Mol Sci. 2012;13(4):4124-4140. doi: 10.3390/ijms13044124. Epub 2012 Mar 29.

Abstract

In the study, we have examined the antitumor and antimicrobial activities of the methanol extract, the fractions, a fraction of total alkaloids and two alkaloids isolated from the stem of Erythroxylum caatingae Plowman. All test fractions, except the hexane fractions, showed antimicrobial activity on gram-positive bacteria and fungi. The acetate: methanol (95:5), acetate, chloroform and hexane fractions show the highest cytotoxicity activity against the NCI-H292, HEp-2 and K562 cell lines using MTT. The absence of hemolysis in the erythrocytes of mice was observed in these fractions and 6β-Benzoyloxy-3α-(3,4,5- trimethoxybenzoyloxy) tropane (catuabine B). Staining with Annexin V-FITC and JC-1 was used to verify the mechanism of action of the compounds of E. caatingae that showed cytotoxicity less than 30 μg/mL in leukemic cells. After 48 h of incubation, we observed that the acetate: methanol (95:5), acetate, and chloroform fractions, as well as the catuabine B, increased in the number of cells in early apoptosis, from 53.0 to 74.8%. An analysis of the potential of the mitochondrial membrane by incorporation of JC-1 showed that most cells during incubation of the acetate: methanol (95:5) and acetate fractions (63.85 and 59.2%) were stained, suggesting the involvement of an intrinsic pathway of apoptosis.

摘要

在该研究中,我们检测了从卡廷加古柯(Erythroxylum caatingae Plowman)茎中分离得到的甲醇提取物、各馏分、总生物碱馏分以及两种生物碱的抗肿瘤和抗菌活性。除己烷馏分外,所有测试馏分均对革兰氏阳性菌和真菌显示出抗菌活性。使用MTT法检测发现,乙酸乙酯:甲醇(95:5)、乙酸乙酯、氯仿和己烷馏分对NCI-H292、HEp-2和K562细胞系具有最高的细胞毒性活性。在这些馏分以及6β-苯甲酰氧基-3α-(3,4,5-三甲氧基苯甲酰氧基)托烷(卡图宾B)中,未观察到小鼠红细胞发生溶血现象。采用膜联蛋白V-FITC和JC-1染色来验证卡廷加古柯中细胞毒性小于30μg/mL的化合物在白血病细胞中的作用机制。孵育48小时后,我们观察到乙酸乙酯:甲醇(95:5)、乙酸乙酯和氯仿馏分以及卡图宾B使早期凋亡细胞数量增加,从53.0%增至74.8%。通过掺入JC-1对线粒体膜电位进行分析表明,在乙酸乙酯:甲醇(95:5)和乙酸乙酯馏分孵育期间,大多数细胞(分别为63.85%和59.2%)被染色,这表明凋亡的内在途径参与其中。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e108/3344205/229eecfaf32c/ijms-13-04124f1.jpg

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