{"title":"茜草硫代葡萄糖苷部分体外抗利什曼原虫活性研究。前野生(芸苔科)。","authors":"Fatemeh Mirzaee, Roghiyeh Faridnia, Mahdi Fakhar, Hamed Kalani, Somayeh Shahani","doi":"10.4274/tjps.galenos.2022.78027","DOIUrl":null,"url":null,"abstract":"<p><strong>Objectives: </strong>The intracellular parasitic protozoan, <i>Leishmania</i> spp., causes several forms of diseases in humans. Cytotoxicity and emergence of new strains resistance to the current anti-leishmanial drugs have encouraged researchers to focus on new resources. Glucosinolates (GSL) are found mainly in the Brassicaceae family with potential cytotoxic and anti-parasitic properties. The present study reports <i>in vitro</i> antileishmanial activity of the GSL fraction from <i>Alyssum linifolium</i> seeds against <i>Leishmania major</i>.</p><p><strong>Materials and methods: </strong>The GSL fraction was prepared by ion-exchange and reversed-phase chromatography. For the assessment of antileishmanial activity, the promastigotes and amastigotes of <i>L. major</i> were treated with different concentrations of the fraction (75-625 μg/mL).</p><p><strong>Results: </strong>The IC<sub>50</sub> was 245 µg/mL for anti-promastigote effect of the GSL fraction and 250 µg/mL for its anti-amastigote effect that had a significant difference (<i>p</i><0.05) with both glucantime and amphotericin B. The selectivity index of the GSL fraction (15.8), to glucantime and amphotericin B, was greater than 10, indicating the selective effect of this fraction against <i>L. major</i> amastigotes. Glucoiberverin was the major constituent of the GSL fraction characterized using nuclear magnetic resonance and electron ionization-mass spectrometry spectra. Based on gas chromatography-mass spectrometry data, iberverin and iberverin nitrile, the hydrolysis constituents from glucoiberverin, included 76.91% of the total seed volatiles.</p><p><strong>Conclusion: </strong>The results suggest that GSLs like glucoiberverin could be considered a new promising candidate for further studies on antileishmanial activity.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.8000,"publicationDate":"2023-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9986943/pdf/TJPS-20-16.pdf","citationCount":"0","resultStr":"{\"title\":\"<i>In Vitro</i> Anti-Leishmanial Activity of Glucosinolate Fraction from <i>Alyssum linifolium</i> Steph. ex Willd (Brassicaceae).\",\"authors\":\"Fatemeh Mirzaee, Roghiyeh Faridnia, Mahdi Fakhar, Hamed Kalani, Somayeh Shahani\",\"doi\":\"10.4274/tjps.galenos.2022.78027\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objectives: </strong>The intracellular parasitic protozoan, <i>Leishmania</i> spp., causes several forms of diseases in humans. Cytotoxicity and emergence of new strains resistance to the current anti-leishmanial drugs have encouraged researchers to focus on new resources. Glucosinolates (GSL) are found mainly in the Brassicaceae family with potential cytotoxic and anti-parasitic properties. The present study reports <i>in vitro</i> antileishmanial activity of the GSL fraction from <i>Alyssum linifolium</i> seeds against <i>Leishmania major</i>.</p><p><strong>Materials and methods: </strong>The GSL fraction was prepared by ion-exchange and reversed-phase chromatography. For the assessment of antileishmanial activity, the promastigotes and amastigotes of <i>L. major</i> were treated with different concentrations of the fraction (75-625 μg/mL).</p><p><strong>Results: </strong>The IC<sub>50</sub> was 245 µg/mL for anti-promastigote effect of the GSL fraction and 250 µg/mL for its anti-amastigote effect that had a significant difference (<i>p</i><0.05) with both glucantime and amphotericin B. The selectivity index of the GSL fraction (15.8), to glucantime and amphotericin B, was greater than 10, indicating the selective effect of this fraction against <i>L. major</i> amastigotes. Glucoiberverin was the major constituent of the GSL fraction characterized using nuclear magnetic resonance and electron ionization-mass spectrometry spectra. Based on gas chromatography-mass spectrometry data, iberverin and iberverin nitrile, the hydrolysis constituents from glucoiberverin, included 76.91% of the total seed volatiles.</p><p><strong>Conclusion: </strong>The results suggest that GSLs like glucoiberverin could be considered a new promising candidate for further studies on antileishmanial activity.</p>\",\"PeriodicalId\":23378,\"journal\":{\"name\":\"Turkish Journal of Pharmaceutical Sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2023-03-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9986943/pdf/TJPS-20-16.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Turkish Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4274/tjps.galenos.2022.78027\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Turkish Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4274/tjps.galenos.2022.78027","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
摘要
目的:细胞内寄生原生动物利什曼原虫引起人类多种疾病。细胞毒性和对当前抗利什曼药物产生耐药性的新菌株的出现促使研究人员将重点放在新的资源上。硫代葡萄糖苷(Glucosinolates, GSL)主要存在于十字花科植物中,具有潜在的细胞毒和抗寄生特性。本研究报道了Alyssum linifolium种子GSL部分对利什曼原虫的体外抗利什曼原虫活性。材料和方法:采用离子交换-反相色谱法制备GSL馏分。采用不同浓度的提取物(75 ~ 625 μg/mL)处理大黄乳杆菌原毛菌和无尾毛菌,考察其抗利什曼原虫活性。结果:GSL部位抗promastigote作用的IC50为245µg/mL,其抗amastigote作用的IC50为250µg/mL,两者具有显著性差异(pL. major amastigotes)。利用核磁共振和电子电离质谱分析对GSL部分的主要成分进行了表征。气相色谱-质谱分析结果表明,从葡萄籽中提取的水解成分——鸢尾素和鸢尾素腈占总挥发物的76.91%。结论:GSLs类糖维苷可作为抗利什曼原虫活性进一步研究的新候选物。
In Vitro Anti-Leishmanial Activity of Glucosinolate Fraction from Alyssum linifolium Steph. ex Willd (Brassicaceae).
Objectives: The intracellular parasitic protozoan, Leishmania spp., causes several forms of diseases in humans. Cytotoxicity and emergence of new strains resistance to the current anti-leishmanial drugs have encouraged researchers to focus on new resources. Glucosinolates (GSL) are found mainly in the Brassicaceae family with potential cytotoxic and anti-parasitic properties. The present study reports in vitro antileishmanial activity of the GSL fraction from Alyssum linifolium seeds against Leishmania major.
Materials and methods: The GSL fraction was prepared by ion-exchange and reversed-phase chromatography. For the assessment of antileishmanial activity, the promastigotes and amastigotes of L. major were treated with different concentrations of the fraction (75-625 μg/mL).
Results: The IC50 was 245 µg/mL for anti-promastigote effect of the GSL fraction and 250 µg/mL for its anti-amastigote effect that had a significant difference (p<0.05) with both glucantime and amphotericin B. The selectivity index of the GSL fraction (15.8), to glucantime and amphotericin B, was greater than 10, indicating the selective effect of this fraction against L. major amastigotes. Glucoiberverin was the major constituent of the GSL fraction characterized using nuclear magnetic resonance and electron ionization-mass spectrometry spectra. Based on gas chromatography-mass spectrometry data, iberverin and iberverin nitrile, the hydrolysis constituents from glucoiberverin, included 76.91% of the total seed volatiles.
Conclusion: The results suggest that GSLs like glucoiberverin could be considered a new promising candidate for further studies on antileishmanial activity.