Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, ...Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, Leishmania infantum, the multidrug-resistant K1 and chloroquine-sensitive NF54 strains of Plasmodium falciparum indicated that all samples from the leaves extract presented interesting antiparasitaire activity at different extents. The 80% methanol extract, its chloroform acid, petroleum ether and 80% methanol soluble fractions and the aqueous extract exhibited strong activity against Trypanosoma b. brucei, T. cruzi, L. infantum and the multidrug-resistant K1 strain of P. falciparum with IC<sub>50</sub> values from <0.25 to 4.35 μg/ml as well as against chloroquine-sensitive NF54 strain of P. falciparum with IC<sub>50</sub> values ranging from <0.02 to 2.0.4 μg/ml. Most samples were cytotoxic against MRC-5 cell lines (0.2 <sub>50</sub>) < 34.24 μg/ml) and showed good selective effect against all tested parasites. In acute toxicity, the aqueous extract was found to be non-toxic and its LD<sub>50 </sub>was estimated to be greater than 5 g/kg. In addition, it did not significantly modify the concentration levels of some evaluated biochemical and hematological parameters in treated rats. These results constitute a scientific validation supporting and justifying the traditional use of the leaves of B. sumatrana for the treatment of malaria, sleeping sickness and at some extent Chagas disease.展开更多
为探究宁夏大籽蒿(Artemisia sieversiana Ehrhart ex Willd.)精油成分、抑菌功能及安全性,采用水蒸气蒸馏法进行精油提取,通过气相色谱-质谱连用法(GC-MS)进行成分分析,采用滤纸片法测定其对3种菌的抑菌圈直径,测定最低抑菌浓度(MIC)...为探究宁夏大籽蒿(Artemisia sieversiana Ehrhart ex Willd.)精油成分、抑菌功能及安全性,采用水蒸气蒸馏法进行精油提取,通过气相色谱-质谱连用法(GC-MS)进行成分分析,采用滤纸片法测定其对3种菌的抑菌圈直径,测定最低抑菌浓度(MIC)、最低杀菌浓度(MBC),并通过cck-8法检测大籽蒿精油对于2种皮肤细胞的毒性作用。结果表明,宁夏大籽蒿精油的主要成分为母菊薁(29.61%),樟脑(4.80%)、桉叶油醇(4.32%)、异木香酸甲酯(4.02%);精油对铜绿假单胞菌和大肠杆菌的最低抑菌浓度为0.0781µg/mL,最低杀菌浓度为0.3125µg/mL;金黄色葡萄球菌MIC为0.0195µg/mL,MBC为0.078125µg/mL;当精油浓度小于100µg/mL时对角质细胞(HaCaT)和皮肤成纤维细胞(NHSF)均无毒性。综上,宁夏地区大籽蒿精油具有较强的抑菌活性且安全性较高,以上结果为宁夏大籽蒿精油开发提供理论依据,以期为当地脱贫致富提供科技支撑。展开更多
One new diarylheptanoid, namely （4E,6E）-7-（3,4-dihydroxy-5-methoxyphenyl）-1-（4-hydroxy-3-methoxyphenyl）- hepta-4,6-dien-3-one （1）, was isolated from the rhizomes of Zingiber officinale, along with ten known on...One new diarylheptanoid, namely （4E,6E）-7-（3,4-dihydroxy-5-methoxyphenyl）-1-（4-hydroxy-3-methoxyphenyl）- hepta-4,6-dien-3-one （1）, was isolated from the rhizomes of Zingiber officinale, along with ten known ones, tetra- hydrocurcumin （2）, curcumin （3）, 5-hydroxy-1,7-bis（4-hydroxy-3-methoxyphenyl）heptan-3-one （4）, gingerenone A （5）, 7-（3,4-dihydroxyphenyl）-5-hydroxy-1-（4-hydroxy-3-methoxyphenyl）heptan-3-one （6）, （E）-1,7-bis（4-hydroxy- 3-methoxyphenyl）hept-1-ene-3,5-dione （7）, （E）-7-（4-hydroxy-3-methoxyphenyl）-1-（4-hydroxyphenyl）-hept-l-ene- 3,5-dione （8）, shogasulfonic acid A （9）, 1,5-epoxy-3-hydroxy-1-（3,4-dihydroxy-5-methoxyphenyl）-7-（4-hydroxy-3- methoxyphenyl）heptane （10）, and （3S, SS）-3,5-diacetoxy-1,7-bis（3,4-dihydroxyphenyl）heptane （11）. Their structures were elucidated on the basis of spectral evidence and comparisons with literature data. The free radical scavenging activity of 1--11 was evaluated by the 1,l-diphenyl-2-picrylhydrazyl （DPPH） assay. Most of the isolated com- pounds were found to be better antioxidants than the positive control ascorbic acid. These compounds were also evaluated for their cytotoxicity against HeLa and MNK-45 cells using the MTT assay. Our results suggest that com- pounds 3 and 5-8 inhibited HeLa cells, and 3, 5, 7 and 8 inhibited MNK-45 cells. It was found that compound 5 was markedly cytotoxic against HeLa and MNK-45 cell lines with ICs0 values of 6.4 and 7.8 μmol/L, respectively.展开更多
文摘Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, Leishmania infantum, the multidrug-resistant K1 and chloroquine-sensitive NF54 strains of Plasmodium falciparum indicated that all samples from the leaves extract presented interesting antiparasitaire activity at different extents. The 80% methanol extract, its chloroform acid, petroleum ether and 80% methanol soluble fractions and the aqueous extract exhibited strong activity against Trypanosoma b. brucei, T. cruzi, L. infantum and the multidrug-resistant K1 strain of P. falciparum with IC<sub>50</sub> values from <0.25 to 4.35 μg/ml as well as against chloroquine-sensitive NF54 strain of P. falciparum with IC<sub>50</sub> values ranging from <0.02 to 2.0.4 μg/ml. Most samples were cytotoxic against MRC-5 cell lines (0.2 <sub>50</sub>) < 34.24 μg/ml) and showed good selective effect against all tested parasites. In acute toxicity, the aqueous extract was found to be non-toxic and its LD<sub>50 </sub>was estimated to be greater than 5 g/kg. In addition, it did not significantly modify the concentration levels of some evaluated biochemical and hematological parameters in treated rats. These results constitute a scientific validation supporting and justifying the traditional use of the leaves of B. sumatrana for the treatment of malaria, sleeping sickness and at some extent Chagas disease.
文摘为探究宁夏大籽蒿(Artemisia sieversiana Ehrhart ex Willd.)精油成分、抑菌功能及安全性,采用水蒸气蒸馏法进行精油提取,通过气相色谱-质谱连用法(GC-MS)进行成分分析,采用滤纸片法测定其对3种菌的抑菌圈直径,测定最低抑菌浓度(MIC)、最低杀菌浓度(MBC),并通过cck-8法检测大籽蒿精油对于2种皮肤细胞的毒性作用。结果表明,宁夏大籽蒿精油的主要成分为母菊薁(29.61%),樟脑(4.80%)、桉叶油醇(4.32%)、异木香酸甲酯(4.02%);精油对铜绿假单胞菌和大肠杆菌的最低抑菌浓度为0.0781µg/mL,最低杀菌浓度为0.3125µg/mL;金黄色葡萄球菌MIC为0.0195µg/mL,MBC为0.078125µg/mL;当精油浓度小于100µg/mL时对角质细胞(HaCaT)和皮肤成纤维细胞(NHSF)均无毒性。综上,宁夏地区大籽蒿精油具有较强的抑菌活性且安全性较高,以上结果为宁夏大籽蒿精油开发提供理论依据,以期为当地脱贫致富提供科技支撑。
文摘One new diarylheptanoid, namely （4E,6E）-7-（3,4-dihydroxy-5-methoxyphenyl）-1-（4-hydroxy-3-methoxyphenyl）- hepta-4,6-dien-3-one （1）, was isolated from the rhizomes of Zingiber officinale, along with ten known ones, tetra- hydrocurcumin （2）, curcumin （3）, 5-hydroxy-1,7-bis（4-hydroxy-3-methoxyphenyl）heptan-3-one （4）, gingerenone A （5）, 7-（3,4-dihydroxyphenyl）-5-hydroxy-1-（4-hydroxy-3-methoxyphenyl）heptan-3-one （6）, （E）-1,7-bis（4-hydroxy- 3-methoxyphenyl）hept-1-ene-3,5-dione （7）, （E）-7-（4-hydroxy-3-methoxyphenyl）-1-（4-hydroxyphenyl）-hept-l-ene- 3,5-dione （8）, shogasulfonic acid A （9）, 1,5-epoxy-3-hydroxy-1-（3,4-dihydroxy-5-methoxyphenyl）-7-（4-hydroxy-3- methoxyphenyl）heptane （10）, and （3S, SS）-3,5-diacetoxy-1,7-bis（3,4-dihydroxyphenyl）heptane （11）. Their structures were elucidated on the basis of spectral evidence and comparisons with literature data. The free radical scavenging activity of 1--11 was evaluated by the 1,l-diphenyl-2-picrylhydrazyl （DPPH） assay. Most of the isolated com- pounds were found to be better antioxidants than the positive control ascorbic acid. These compounds were also evaluated for their cytotoxicity against HeLa and MNK-45 cells using the MTT assay. Our results suggest that com- pounds 3 and 5-8 inhibited HeLa cells, and 3, 5, 7 and 8 inhibited MNK-45 cells. It was found that compound 5 was markedly cytotoxic against HeLa and MNK-45 cell lines with ICs0 values of 6.4 and 7.8 μmol/L, respectively.
