Sixteen novel and four known（4a, 4d, 4e, 4h） amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five comp...Sixteen novel and four known（4a, 4d, 4e, 4h） amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five compounds（4g, 4j-4m） showed potent activating effect on both melanogenesis and tyrosinase in vitro compared with positive control（8-MOP）, the most widely used drugs for vitiligo in clinic. Noticeably, compotmds 4h and 4j, which contain morpholine and piperazine, were recognized as the most effective stimnlator of melanogenesis and tyrosianse in B16 cells separately. These derivatives may serve as lead compounds for further drug discovery for the treatment of vitiligo.展开更多
Furocoumarins are an important class of heterocyclic compounds with a fused tricyclic structure of coumarin and furan rings.They are commonly found in bioactive natural products and have a diverse range of biological ...Furocoumarins are an important class of heterocyclic compounds with a fused tricyclic structure of coumarin and furan rings.They are commonly found in bioactive natural products and have a diverse range of biological and pharmaceutical properties,including cytotoxicity,photosensitivity,insecticidal,antibacterial,and antifungal activity,among others.The elegant linear/angular tricyclic skeleton and superior pharmacological properties,make them ideal for building and developing advanced biological scaffolds for biomedical applications.As a result,the family of furocoumarins has been the focus of intensive research,and lots of encouraging progress have been achieved in recent years.This review summarizes the most recent methods reported for the synthesis of the furocoumarin derivative family,along with their applications in medicinal chemistry covering from 2018 to 2022.展开更多
Species from Moraceae family stand out in popular medicine and phytotherapy, have been for example used as expectorants, bronchodilators, anthelmintics and treatment of skin diseases, such as vitiligo, due to the pres...Species from Moraceae family stand out in popular medicine and phytotherapy, have been for example used as expectorants, bronchodilators, anthelmintics and treatment of skin diseases, such as vitiligo, due to the presence of compounds with proven biological activity, as the coumarins. Coumarins are lactones with 1,2-benzopyrone basic structure, and are widely distributed in the plant kingdom, both in free form, and in glycosylated form. This work reports a literature review, describing the data of 13C NMR from 53 coumarins isolated from the family Moraceae, and data comparison between genera who presented photochemical studies, in order to contribute to the chemotaxonomy of this family.展开更多
文摘Sixteen novel and four known（4a, 4d, 4e, 4h） amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five compounds（4g, 4j-4m） showed potent activating effect on both melanogenesis and tyrosinase in vitro compared with positive control（8-MOP）, the most widely used drugs for vitiligo in clinic. Noticeably, compotmds 4h and 4j, which contain morpholine and piperazine, were recognized as the most effective stimnlator of melanogenesis and tyrosianse in B16 cells separately. These derivatives may serve as lead compounds for further drug discovery for the treatment of vitiligo.
基金financial support from the National Natural Science Foundation of China(Nos.21971211 and 22171232)the Natural Science Foundation of Zhejiang Province(No.2022XHSJJ007)+3 种基金the Qiantang River Talent Foundation(No.QJD1902029)Westlake Universitysupported by Instrumentation and Service Centers for Molecular Science and for Physical Science(ISCMS and ISCPS)by the Mass Spectrometry&Metabolomics Core Facility at the Center for Biomedical Research Core Facilities and Westlake University HPC Center。
文摘Furocoumarins are an important class of heterocyclic compounds with a fused tricyclic structure of coumarin and furan rings.They are commonly found in bioactive natural products and have a diverse range of biological and pharmaceutical properties,including cytotoxicity,photosensitivity,insecticidal,antibacterial,and antifungal activity,among others.The elegant linear/angular tricyclic skeleton and superior pharmacological properties,make them ideal for building and developing advanced biological scaffolds for biomedical applications.As a result,the family of furocoumarins has been the focus of intensive research,and lots of encouraging progress have been achieved in recent years.This review summarizes the most recent methods reported for the synthesis of the furocoumarin derivative family,along with their applications in medicinal chemistry covering from 2018 to 2022.
文摘Species from Moraceae family stand out in popular medicine and phytotherapy, have been for example used as expectorants, bronchodilators, anthelmintics and treatment of skin diseases, such as vitiligo, due to the presence of compounds with proven biological activity, as the coumarins. Coumarins are lactones with 1,2-benzopyrone basic structure, and are widely distributed in the plant kingdom, both in free form, and in glycosylated form. This work reports a literature review, describing the data of 13C NMR from 53 coumarins isolated from the family Moraceae, and data comparison between genera who presented photochemical studies, in order to contribute to the chemotaxonomy of this family.
