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Isolation of diverse bioactive compounds from Euphorbia balsamifera: Cytotoxicity and antibacterial activity studies

机译:从大戟属Balsamifera中分离各种生物活性化合物:细胞毒性和抗菌活性研究

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Antibacterial and cytotoxic activities of Euphorbia balsamifera , fractions and pure compounds were evaluated.?The cytotoxic assays for?HCT116, HePG2 and MCF7 showed a significant IC 50 : 54.7 and 76.2?μg/mL of non-polar fraction “ n -hexane” against HCT116 and HePG2, respectively. Antibacterial results revealed that plant fractions exhibited significant potential against the tested pathogens than the total extract where n -butanol and ethyl acetate fractions showed significant antibacterial activity ( P ?0.05) against tested bacterial strains. Isolation and structure determination of compounds from n -hexane and n -butanol fractions were performed. From n -hexane fraction, 29-nor-cycloartanol ( 1), lanost-8-en-3-ol (2a ) , cycloartanol (2b) and kampferol-3,4'-dimethyl ether ( 3 ) were isolated and structurally identified, along with 24 compounds were tentatively identified by GC–MS. From the polar n -butanol fraction, 4- O -β-D-glucopyranosyl-2-hydroxy-6-methoxyacetophenone ( 4), 4- O -α-L-rhamnosyl-(1?→?6)-β-D-glucopyranosyl-2-hydroxy-6methoxy-acetophenone ( 5) , quercetin-3- O -glucopyranoside ( 6) and isoorientin ( 7) were assigned. Structures of the obtained compounds were determined by nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry. Except compounds 1 and 5, all reported compounds announced antibacterial efficiency. Compound 2 showed selectively the highest activity against Enterococcus faecalis (22?±?0.13?mm), meanwhile 4- O -β-D-glucopyranosyl-2-hydroxy-6-methoxyacetophenone ( 4) showed broadly the highest antibacterial activity with MIC of 1.15–1.88?mg/mL against the test Gram-positive and Gram-negative bacteria. Cytotoxic assays indicated that kampferol-3,4'-dimethyl ether ( 3) exhibited the highest activity with matching IC 50 values to doxorubicin; 111.46, 42.67 and 44.90?μM against HCT116, HePG2 and MCF7, respectively, however, it is toxic on retina normal cell line RPE1.
机译:评价抗菌和细胞毒性和细胞毒活性,级分和纯化合物进行了β-HCT116,HEPG2和MCF7的细胞毒性测定显示出显着的IC 50:54.7和76.2≤μg/ mL非极性级分“n-己烷” HCT116和HepG2分别。抗菌结果表明,植物级分表现出对测试病原体的显着潜力,而不是N-丁醇和乙酸乙酯级分的总提取物,其针对测试的细菌菌株显示出显着的抗菌活性(P <β.05)。进行N-己烷和N-丁醇级分的分离和结构测定。从N-己烷级分,分离和结构识别,将29-己烷醇(1),Lanost-8-ZEN-3-OL(2a),环丙醇(2b)和kampferolol-3,4'-二甲醚(3)分离和GC-MS一起暂时鉴定24种化合物。从极性N-丁醇级分,4-O-β-D-吡喃葡萄糖酰基-2-羟基-6-甲氧基乙酮(4),4-O-α-L- rhamnosyl-(1?→→6)-β-D - 分配 - 甘氨基吡喃糖基-2-羟基-6甲氧基 - 乙酮(5),分配槲皮素-3-O--葡糖胺(6)和等管素(7)。通过核磁共振(NMR)光谱和质谱法测定所得化合物的结构。除了化合物1和5,所有报道的化合物都宣布抗菌效率。化合物2选择性地显示出对肠球菌的最高活性(22?±0.13mm),同时4-O-β-D-吡喃葡萄糖烯基-2-羟基-6-甲氧基乙酮(4)均具有宽度最高的抗菌活性1.15-1.88?mg / ml对抗测试革兰氏阳性和革兰氏阴性细菌。细胞毒性测定表明,Kampferolol-3,4'-二甲醚(3)表现出具有匹配IC 50值至多柔比星的最高活性;然而,对于HCT116,HepG2和MCF7,111.46,42.67和44.90?μm,然而,它在视网膜正常细胞系RPE1上有毒。

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