鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动...鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动了负载鱼藤素的新制剂和鱼藤素结构修饰类似物的不断发展。本文通过检索SciFinder、Web of science、PubMed、CNKI等数据库中已发表的关于鱼藤素及其衍生物的相关文献资料,对鱼藤素的来源、生物活性、毒性、及其衍生物的研究进展,特别是针对其抗肿瘤活性的结构修饰与优化研究进行了综述,经分析和归纳总结发现针对鱼藤素的结构修饰主要集中于B、C、E环骨架和A环上的取代基,其目的主要是提高抗肿瘤活性并降低毒性,所得衍生物多数是作为Hsp90 C端抑制剂而表现出优良的抗肿瘤活性。本综述研究将为后续基于鱼藤素的生物活性研究和新药研发,特别是关于鱼藤素及其衍生物在抗肿瘤领域的深入研究和探索提供一定的借鉴和参考。展开更多
The current single-atom catalysts(SACs)for medicine still suffer from the limited active site density.Here,we develop a synthetic method capable of increasing both the metal loading and mass-specific activity of SACs ...The current single-atom catalysts(SACs)for medicine still suffer from the limited active site density.Here,we develop a synthetic method capable of increasing both the metal loading and mass-specific activity of SACs by exchanging zinc with iron.The constructed iron SACs(h^(3)-FNC)with a high metal loading of 6.27 wt%and an optimized adjacent Fe distance of~4 A exhibit excellent oxidase-like catalytic performance without significant activity decay after being stored for six months and promising antibacterial effects.Attractively,a“density effect”has been found at a high-enough metal doping amount,at which individual active sites become close enough to interact with each other and alter the electronic structure,resulting in significantly boosted intrinsic activity of single-atomic iron sites in h^(3)-FNCs by 2.3 times compared to low-and medium-loading SACs.Consequently,the overall catalytic activity of h^(3)-FNC is highly improved,with mass activity and metal mass-specific activity that are,respectively,66 and 315 times higher than those of commercial Pt/C.In addition,h^(3)-FNCs demonstrate efficiently enhanced capability in catalyzing oxygen reduction into superoxide anion(O_(2)·^(−))and glutathione(GSH)depletion.Both in vitro and in vivo assays demonstrate the superior antibacterial efficacy of h^(3)-FNCs in promoting wound healing.This work presents an intriguing activity-enhancement effect in catalysts and exhibits impressive therapeutic efficacy in combating bacterial infections.展开更多
目的对肾茶(Clerodendranthus spicatus(Thunb)C Y Wu ex H.W.Li)地上部分的化学成分进行研究,进一步丰富其物质基础。方法采用加热回流提取法对肾茶的干燥地上部分进行提取,联合应用硅胶、ODS及高效液相色谱等多种色谱法对肾茶地上部...目的对肾茶(Clerodendranthus spicatus(Thunb)C Y Wu ex H.W.Li)地上部分的化学成分进行研究,进一步丰富其物质基础。方法采用加热回流提取法对肾茶的干燥地上部分进行提取,联合应用硅胶、ODS及高效液相色谱等多种色谱法对肾茶地上部分提取物的化学成分进行分离纯化,结合圆二色光谱、核磁、质谱等波谱技术以及化学反应的方法,鉴定化合物的结构,确定其绝对构型。结果从肾茶地上部分分离鉴定了7个丹参素衍生物,分别为(R)-迷迭香酸(1)、(R)-迷迭香酸甲酯(2)、(R)-迷迭香酸乙酯(3)、2R-羟基-3-(4-羟基苯基)丙酸甲酯(4)、2R-羟基-3-(3,4-二羟基苯基)丙酸(5)、2R-羟基-3-(3,4-二羟基苯基)丙酸甲酯(6)和2R-羟基-3-(3,4-二羟基苯基)丙酸乙酯(7)。结论化合物4为首次从肾茶属植物中分离得到。此外,发现对于α-羟基羧酸类化合物,即使是只有一个手性中心,也不能仅仅通过旋光值的比对确定其绝对构型。本文所提供的方法为该类成分构型的研究提供了借鉴。展开更多
文摘鱼藤素是大量存在于豆科植物中的一种鱼藤酮类化合物,具有多种生物学活性,如杀虫、抗肿瘤、抗炎、抗病毒、抗糖尿病神经病变以及抗骨质疏松等。然而,高剂量的鱼藤素可导致呼吸抑制、心脏毒性和神经传导阻断等剂量相关的不良影响,这推动了负载鱼藤素的新制剂和鱼藤素结构修饰类似物的不断发展。本文通过检索SciFinder、Web of science、PubMed、CNKI等数据库中已发表的关于鱼藤素及其衍生物的相关文献资料,对鱼藤素的来源、生物活性、毒性、及其衍生物的研究进展,特别是针对其抗肿瘤活性的结构修饰与优化研究进行了综述,经分析和归纳总结发现针对鱼藤素的结构修饰主要集中于B、C、E环骨架和A环上的取代基,其目的主要是提高抗肿瘤活性并降低毒性,所得衍生物多数是作为Hsp90 C端抑制剂而表现出优良的抗肿瘤活性。本综述研究将为后续基于鱼藤素的生物活性研究和新药研发,特别是关于鱼藤素及其衍生物在抗肿瘤领域的深入研究和探索提供一定的借鉴和参考。
基金supported by the National Key Research and Development Program of China(Grant No.2022YFB3804500)the National Natural Science Foundation of China(Grant No.52202352,22335006)+4 种基金the Shanghai Municipal Health Commission(Grant No.20224Y0010)the CAMS Innovation Fund for Medical Sciences(Grant No.2021-I2M-5-012)the Basic Research Program of Shanghai Municipal Government(Grant No.21JC1406000)the Fundamental Research Funds for the Central Universities(Grant No.22120230237,2023-3-YB-11,22120220618)the Basic Research Program of Shanghai Municipal Government(23DX1900200).
文摘The current single-atom catalysts(SACs)for medicine still suffer from the limited active site density.Here,we develop a synthetic method capable of increasing both the metal loading and mass-specific activity of SACs by exchanging zinc with iron.The constructed iron SACs(h^(3)-FNC)with a high metal loading of 6.27 wt%and an optimized adjacent Fe distance of~4 A exhibit excellent oxidase-like catalytic performance without significant activity decay after being stored for six months and promising antibacterial effects.Attractively,a“density effect”has been found at a high-enough metal doping amount,at which individual active sites become close enough to interact with each other and alter the electronic structure,resulting in significantly boosted intrinsic activity of single-atomic iron sites in h^(3)-FNCs by 2.3 times compared to low-and medium-loading SACs.Consequently,the overall catalytic activity of h^(3)-FNC is highly improved,with mass activity and metal mass-specific activity that are,respectively,66 and 315 times higher than those of commercial Pt/C.In addition,h^(3)-FNCs demonstrate efficiently enhanced capability in catalyzing oxygen reduction into superoxide anion(O_(2)·^(−))and glutathione(GSH)depletion.Both in vitro and in vivo assays demonstrate the superior antibacterial efficacy of h^(3)-FNCs in promoting wound healing.This work presents an intriguing activity-enhancement effect in catalysts and exhibits impressive therapeutic efficacy in combating bacterial infections.
文摘目的对肾茶(Clerodendranthus spicatus(Thunb)C Y Wu ex H.W.Li)地上部分的化学成分进行研究,进一步丰富其物质基础。方法采用加热回流提取法对肾茶的干燥地上部分进行提取,联合应用硅胶、ODS及高效液相色谱等多种色谱法对肾茶地上部分提取物的化学成分进行分离纯化,结合圆二色光谱、核磁、质谱等波谱技术以及化学反应的方法,鉴定化合物的结构,确定其绝对构型。结果从肾茶地上部分分离鉴定了7个丹参素衍生物,分别为(R)-迷迭香酸(1)、(R)-迷迭香酸甲酯(2)、(R)-迷迭香酸乙酯(3)、2R-羟基-3-(4-羟基苯基)丙酸甲酯(4)、2R-羟基-3-(3,4-二羟基苯基)丙酸(5)、2R-羟基-3-(3,4-二羟基苯基)丙酸甲酯(6)和2R-羟基-3-(3,4-二羟基苯基)丙酸乙酯(7)。结论化合物4为首次从肾茶属植物中分离得到。此外,发现对于α-羟基羧酸类化合物,即使是只有一个手性中心,也不能仅仅通过旋光值的比对确定其绝对构型。本文所提供的方法为该类成分构型的研究提供了借鉴。
