{"title":"姜黄素非甾体抗炎药偶联物的合成及生物学评价","authors":"Sarika Chaudhary","doi":"10.26420/austinjanalpharmchem.2023.1153","DOIUrl":null,"url":null,"abstract":"The present research work involves the synthesis of a total of four Curcumin-NSAIDs conjugates and their subsequent biological screening for Rheumatoid Arthritis, Anti-inflammatory, and Anti-ulcer activities. Curcumin is a phytochemical having versatile therapeutic potential. The idea of conjugating curcumin with various NSAIDs is somewhat novel in the sense that it helps in obtaining the target of incorporating certain desired properties in the curcumin like enhanced bioavailability, reduction in the side effects and also giving good therapeutic potential in terms of determination of rheumatoid arthritis, anti-inflammatory and anti-ulcer activities of synthesized conjugates using appropriate animal models. Additionally, studies have been done on the in vivo bioavailability of curcumin-NSAIDs conjugates and curcumin in Sprague-Dawley rats and on the antiarthritic efficacy of curcumin-NSAIDs conjugates and curcumin in a modified streptococcal cell wall-induced arthritis model in Balb/c mice to resemble rheumatoid arthritis in human. Curcumin-NSAID conjugates have shown improved stability in all of the studies mentioned when compared to curcumin and curcumin-NSAID conjugates; they also increased curcumin’s bioavailability by more than five folds and significantly reduced arthritis symptoms in a streptococcal cell wall-induced arthritis model when compared to other conjugates and curcumin. The structural features of all the synthesized compounds have been confirmed by appropriate spectral analysis. Other supporting techniques employed for structural and purity aspects include Melting point determination, Thin Layer Chromatography analysis, and Recrystallization. Therefore, conjugating curcumin with medicinal molecules proved to be a creative way to increase its bioavailability and enhance its wide range of pharmacological effects.","PeriodicalId":91055,"journal":{"name":"Austin journal of analytical and pharmaceutical chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and Biological Evaluation of Curcumin-NSAIDs Conjugates\",\"authors\":\"Sarika Chaudhary\",\"doi\":\"10.26420/austinjanalpharmchem.2023.1153\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The present research work involves the synthesis of a total of four Curcumin-NSAIDs conjugates and their subsequent biological screening for Rheumatoid Arthritis, Anti-inflammatory, and Anti-ulcer activities. Curcumin is a phytochemical having versatile therapeutic potential. The idea of conjugating curcumin with various NSAIDs is somewhat novel in the sense that it helps in obtaining the target of incorporating certain desired properties in the curcumin like enhanced bioavailability, reduction in the side effects and also giving good therapeutic potential in terms of determination of rheumatoid arthritis, anti-inflammatory and anti-ulcer activities of synthesized conjugates using appropriate animal models. Additionally, studies have been done on the in vivo bioavailability of curcumin-NSAIDs conjugates and curcumin in Sprague-Dawley rats and on the antiarthritic efficacy of curcumin-NSAIDs conjugates and curcumin in a modified streptococcal cell wall-induced arthritis model in Balb/c mice to resemble rheumatoid arthritis in human. Curcumin-NSAID conjugates have shown improved stability in all of the studies mentioned when compared to curcumin and curcumin-NSAID conjugates; they also increased curcumin’s bioavailability by more than five folds and significantly reduced arthritis symptoms in a streptococcal cell wall-induced arthritis model when compared to other conjugates and curcumin. The structural features of all the synthesized compounds have been confirmed by appropriate spectral analysis. Other supporting techniques employed for structural and purity aspects include Melting point determination, Thin Layer Chromatography analysis, and Recrystallization. Therefore, conjugating curcumin with medicinal molecules proved to be a creative way to increase its bioavailability and enhance its wide range of pharmacological effects.\",\"PeriodicalId\":91055,\"journal\":{\"name\":\"Austin journal of analytical and pharmaceutical chemistry\",\"volume\":\"1 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-01-17\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Austin journal of analytical and pharmaceutical chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.26420/austinjanalpharmchem.2023.1153\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Austin journal of analytical and pharmaceutical chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.26420/austinjanalpharmchem.2023.1153","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and Biological Evaluation of Curcumin-NSAIDs Conjugates
The present research work involves the synthesis of a total of four Curcumin-NSAIDs conjugates and their subsequent biological screening for Rheumatoid Arthritis, Anti-inflammatory, and Anti-ulcer activities. Curcumin is a phytochemical having versatile therapeutic potential. The idea of conjugating curcumin with various NSAIDs is somewhat novel in the sense that it helps in obtaining the target of incorporating certain desired properties in the curcumin like enhanced bioavailability, reduction in the side effects and also giving good therapeutic potential in terms of determination of rheumatoid arthritis, anti-inflammatory and anti-ulcer activities of synthesized conjugates using appropriate animal models. Additionally, studies have been done on the in vivo bioavailability of curcumin-NSAIDs conjugates and curcumin in Sprague-Dawley rats and on the antiarthritic efficacy of curcumin-NSAIDs conjugates and curcumin in a modified streptococcal cell wall-induced arthritis model in Balb/c mice to resemble rheumatoid arthritis in human. Curcumin-NSAID conjugates have shown improved stability in all of the studies mentioned when compared to curcumin and curcumin-NSAID conjugates; they also increased curcumin’s bioavailability by more than five folds and significantly reduced arthritis symptoms in a streptococcal cell wall-induced arthritis model when compared to other conjugates and curcumin. The structural features of all the synthesized compounds have been confirmed by appropriate spectral analysis. Other supporting techniques employed for structural and purity aspects include Melting point determination, Thin Layer Chromatography analysis, and Recrystallization. Therefore, conjugating curcumin with medicinal molecules proved to be a creative way to increase its bioavailability and enhance its wide range of pharmacological effects.