Objective:To investigate the leishmanicidal effect of the Bixa orellana crude seed extract and its fractions against Leishmania amazonensis.Methods:Four main fractions(BO-A,BO-B,BO-C and BO-D)were obtained by exhausti...Objective:To investigate the leishmanicidal effect of the Bixa orellana crude seed extract and its fractions against Leishmania amazonensis.Methods:Four main fractions(BO-A,BO-B,BO-C and BO-D)were obtained by exhaustion with solvent with increased polarity from the Bixa orellana crude seed extract and 28 sub-fractions.The antileishmanial activity was evaluated in intracellular amastigotes and the cytotoxicity was assessed in murine intraperitoneal macrophages.Results:The BO-A and BO-B fractions showed a good antileishmanial activity with IC50 values of(12.9±4.1)and(12.4±0.3)μg/mL,respectively.The sub-fractions BO-B1(IC_(50)=(11.8±3.8)μg/mL)and BO-B3[IC_(50)=(13.6±4.7)μg/mL]also proved to have a good leishmanicidal effect.In general,the sub-fractions showed a lower toxicity than the crude extract.A selectivity index of 9 indicated a moderate selectivity of the BO-A,BO-B and BO-C fractions and BO-B1 sub-fraction.Conclusions:Potential of this plant against cutaneous leishmaniasis should be further investigated.展开更多
The present work studies the chemical constituents from marine-derived streptomyces 3320^# and their antitumor activities. The n-BuOH extract of the ferment broth of 3320^# was chromatographed on silica gel, Sephadex ...The present work studies the chemical constituents from marine-derived streptomyces 3320^# and their antitumor activities. The n-BuOH extract of the ferment broth of 3320^# was chromatographed on silica gel, Sephadex LH-20, ODS columns and HPLC to separate the compounds with antitoumor activities. Their structures were identified using IR, UV, NMR, MS spectroscopic techniques and compared with published data. The antitumor activities of the isolates were assayed using SRB method and flow cytometry assay, accompanied with the morphological observation of the cells under light micro- scope against mammalian tsFT210 cells. Ten compounds, cyclo-(Ala-Leu) 1, cyclo-(Ala-Ile) 2, cyclo-(Ala-Val) 3, cyclo- (Phe-Pro) 4, cyclo-(Phe-Gly)5, cyclo-(Leu-Pro)6, 1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid 7, N-(4- hydroxyphenethyl) acetamide 8, 4-methyoxy-l-(2-hydroxy) ethylbenzene 9 and uridine 10, were isolated from the ferment broth of streptomyces 3320^# . Among them, compounds 6, 7, 8 and 10 showed potent cytotoxicity against the tsFT210 cell with the IC50 values of 3.6, 7.2, 5.2 and 1.6 mmol L-1, respectively. Compounds 8, 10 also exhibited apoptosis inducing activity under 2.0 mmol L-1. Compounds 6, 7, 8 and 10 are the principle bioactive constituents responsible for the antitumor activities of marine streptomyces 3320^#. Compound 7 was isolated from this species for the first time.展开更多
Three new compounds, namely siderochelins D (2), E (3), and F (4), together with one known siderochelin A (1), were isolated from Amycolatopsis sp. LZ149 and elucidated by spectroscopic analyses includinglD- a...Three new compounds, namely siderochelins D (2), E (3), and F (4), together with one known siderochelin A (1), were isolated from Amycolatopsis sp. LZ149 and elucidated by spectroscopic analyses includinglD- and 2D-NMR and X-ray single crystal diffraction. Compounds 1-3 showed antibacterial activity against Mycobacterium smegmatis.展开更多
基金Supported by the Ministry of Public Health and Ministry of Science,Technology and Enviroment of Cuba(Grant No.1003021/2010).
文摘Objective:To investigate the leishmanicidal effect of the Bixa orellana crude seed extract and its fractions against Leishmania amazonensis.Methods:Four main fractions(BO-A,BO-B,BO-C and BO-D)were obtained by exhaustion with solvent with increased polarity from the Bixa orellana crude seed extract and 28 sub-fractions.The antileishmanial activity was evaluated in intracellular amastigotes and the cytotoxicity was assessed in murine intraperitoneal macrophages.Results:The BO-A and BO-B fractions showed a good antileishmanial activity with IC50 values of(12.9±4.1)and(12.4±0.3)μg/mL,respectively.The sub-fractions BO-B1(IC_(50)=(11.8±3.8)μg/mL)and BO-B3[IC_(50)=(13.6±4.7)μg/mL]also proved to have a good leishmanicidal effect.In general,the sub-fractions showed a lower toxicity than the crude extract.A selectivity index of 9 indicated a moderate selectivity of the BO-A,BO-B and BO-C fractions and BO-B1 sub-fraction.Conclusions:Potential of this plant against cutaneous leishmaniasis should be further investigated.
基金supported by the Project of Chinese National Programs for High Technology Research and Development(No.2003AA624020)the National Natural Science Foundation of China(Nos.30472136 and 30470196)Shandong Province and Qingdao Natural Science Foundation(Nos.Z2001C01 and 04-2-JZ-81).
文摘The present work studies the chemical constituents from marine-derived streptomyces 3320^# and their antitumor activities. The n-BuOH extract of the ferment broth of 3320^# was chromatographed on silica gel, Sephadex LH-20, ODS columns and HPLC to separate the compounds with antitoumor activities. Their structures were identified using IR, UV, NMR, MS spectroscopic techniques and compared with published data. The antitumor activities of the isolates were assayed using SRB method and flow cytometry assay, accompanied with the morphological observation of the cells under light micro- scope against mammalian tsFT210 cells. Ten compounds, cyclo-(Ala-Leu) 1, cyclo-(Ala-Ile) 2, cyclo-(Ala-Val) 3, cyclo- (Phe-Pro) 4, cyclo-(Phe-Gly)5, cyclo-(Leu-Pro)6, 1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid 7, N-(4- hydroxyphenethyl) acetamide 8, 4-methyoxy-l-(2-hydroxy) ethylbenzene 9 and uridine 10, were isolated from the ferment broth of streptomyces 3320^# . Among them, compounds 6, 7, 8 and 10 showed potent cytotoxicity against the tsFT210 cell with the IC50 values of 3.6, 7.2, 5.2 and 1.6 mmol L-1, respectively. Compounds 8, 10 also exhibited apoptosis inducing activity under 2.0 mmol L-1. Compounds 6, 7, 8 and 10 are the principle bioactive constituents responsible for the antitumor activities of marine streptomyces 3320^#. Compound 7 was isolated from this species for the first time.
基金supported by the 973 Program(Nos.2010CB833802 and 2012CB721005)the National Science Fund for Distinguished Young Scholars(No.30325044)the Natural Science Foundation of China(No.81373304)
文摘Three new compounds, namely siderochelins D (2), E (3), and F (4), together with one known siderochelin A (1), were isolated from Amycolatopsis sp. LZ149 and elucidated by spectroscopic analyses includinglD- and 2D-NMR and X-ray single crystal diffraction. Compounds 1-3 showed antibacterial activity against Mycobacterium smegmatis.