{"title":"阿魏酸和对香豆酸酰胺衍生物抗菌/抗氧化剂的设计、合成和表征","authors":"Chandani G. Halpani, Satyendra Mishra","doi":"10.1016/j.pscia.2023.100023","DOIUrl":null,"url":null,"abstract":"<div><p>Ferulic acid and <em>p</em>-coumaric acid, cinnamic derivatives of phenolic acid, have antibacterial, prooxidant, and antioxidant effects. In this study ferulic acid and <em>p</em>-coumaric acid amide derivatives were investigated for their antibacterial and antioxidant properties are described in this communication. The most effective conjugates against <em>B subtilis</em> were <strong>5b</strong> (IC<sub>50</sub>: 215 ± 1.3 μM) and <strong>4d</strong> (IC<sub>50</sub>: 336 ± 2.7 μM) and against <em>P. aeruginosa</em> were <strong>4b</strong> (IC<sub>50</sub>: 365 ± 2.8 μM) and <strong>5b</strong> (IC<sub>50</sub>: 341 ± 3.6 μM), whereas the none of conjugates were more effective against <em>E. coli</em> than reference Kanamycin. Conjugates <strong>5b</strong> was the most effective against <em>B subtilis</em> of all the synthesized conjugates, with IC<sub>50</sub> values of (IC<sub>50</sub>: 215 ± 1.3 μM). The free radical scavenging capacity of each compound was determined using the DPPH and ABTS assays. Conjugates <strong>4b</strong> (IC<sub>50</sub>: 53 ± 3.6 μM)<strong>, 4c</strong> (IC<sub>50</sub>: 58 ± 1.3 μM)<strong>, 4d</strong> (IC<sub>50</sub>: 57 ± 2.5 μM), <strong>5b</strong> (IC<sub>50</sub>: 29 ± 1.5 μM) and <strong>4a</strong> (IC<sub>50</sub>: 56 ± 4.3 μM) have greater antioxidant capacity than ferulic acid and ascorbic acid in the DPPH assay. Whereas in the ABTS assay, compounds <strong>4b (</strong>IC<sub>50</sub>: 7 ± 1.8 μM), <strong>5b (</strong>IC<sub>50</sub>: 5 ± 0.7 μM), <strong>4a (</strong>IC<sub>50</sub>: 9 ± 3.2 μM), <strong>4g (</strong>IC<sub>50</sub>: 7 ± 2.3 μM), and <strong>5a (</strong>IC<sub>50</sub>: 8 ± 4.3 μM) showed more antioxidant activity than ferulic acid, <em>p</em>-coumaric acid and ascorbic acid. Thus, a large library of compounds derived from bile acid can be easily synthesized for extensive structure-activity relationship studies in order to identify the most appropriate antibacterial and antioxidant agents.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"2 ","pages":"Article 100023"},"PeriodicalIF":0.0000,"publicationDate":"2023-10-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2773216923000211/pdfft?md5=7e8e62c9a09a0b64e96c5bd87a97948f&pid=1-s2.0-S2773216923000211-main.pdf","citationCount":"0","resultStr":"{\"title\":\"Design, synthesis, characterization of ferulic acid and p-coumaric acid amide derivatives as an antibacterial/antioxidant agent\",\"authors\":\"Chandani G. Halpani, Satyendra Mishra\",\"doi\":\"10.1016/j.pscia.2023.100023\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Ferulic acid and <em>p</em>-coumaric acid, cinnamic derivatives of phenolic acid, have antibacterial, prooxidant, and antioxidant effects. In this study ferulic acid and <em>p</em>-coumaric acid amide derivatives were investigated for their antibacterial and antioxidant properties are described in this communication. The most effective conjugates against <em>B subtilis</em> were <strong>5b</strong> (IC<sub>50</sub>: 215 ± 1.3 μM) and <strong>4d</strong> (IC<sub>50</sub>: 336 ± 2.7 μM) and against <em>P. aeruginosa</em> were <strong>4b</strong> (IC<sub>50</sub>: 365 ± 2.8 μM) and <strong>5b</strong> (IC<sub>50</sub>: 341 ± 3.6 μM), whereas the none of conjugates were more effective against <em>E. coli</em> than reference Kanamycin. Conjugates <strong>5b</strong> was the most effective against <em>B subtilis</em> of all the synthesized conjugates, with IC<sub>50</sub> values of (IC<sub>50</sub>: 215 ± 1.3 μM). The free radical scavenging capacity of each compound was determined using the DPPH and ABTS assays. Conjugates <strong>4b</strong> (IC<sub>50</sub>: 53 ± 3.6 μM)<strong>, 4c</strong> (IC<sub>50</sub>: 58 ± 1.3 μM)<strong>, 4d</strong> (IC<sub>50</sub>: 57 ± 2.5 μM), <strong>5b</strong> (IC<sub>50</sub>: 29 ± 1.5 μM) and <strong>4a</strong> (IC<sub>50</sub>: 56 ± 4.3 μM) have greater antioxidant capacity than ferulic acid and ascorbic acid in the DPPH assay. Whereas in the ABTS assay, compounds <strong>4b (</strong>IC<sub>50</sub>: 7 ± 1.8 μM), <strong>5b (</strong>IC<sub>50</sub>: 5 ± 0.7 μM), <strong>4a (</strong>IC<sub>50</sub>: 9 ± 3.2 μM), <strong>4g (</strong>IC<sub>50</sub>: 7 ± 2.3 μM), and <strong>5a (</strong>IC<sub>50</sub>: 8 ± 4.3 μM) showed more antioxidant activity than ferulic acid, <em>p</em>-coumaric acid and ascorbic acid. Thus, a large library of compounds derived from bile acid can be easily synthesized for extensive structure-activity relationship studies in order to identify the most appropriate antibacterial and antioxidant agents.</p></div>\",\"PeriodicalId\":101012,\"journal\":{\"name\":\"Pharmaceutical Science Advances\",\"volume\":\"2 \",\"pages\":\"Article 100023\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-10-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S2773216923000211/pdfft?md5=7e8e62c9a09a0b64e96c5bd87a97948f&pid=1-s2.0-S2773216923000211-main.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Science Advances\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2773216923000211\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Science Advances","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2773216923000211","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Design, synthesis, characterization of ferulic acid and p-coumaric acid amide derivatives as an antibacterial/antioxidant agent
Ferulic acid and p-coumaric acid, cinnamic derivatives of phenolic acid, have antibacterial, prooxidant, and antioxidant effects. In this study ferulic acid and p-coumaric acid amide derivatives were investigated for their antibacterial and antioxidant properties are described in this communication. The most effective conjugates against B subtilis were 5b (IC50: 215 ± 1.3 μM) and 4d (IC50: 336 ± 2.7 μM) and against P. aeruginosa were 4b (IC50: 365 ± 2.8 μM) and 5b (IC50: 341 ± 3.6 μM), whereas the none of conjugates were more effective against E. coli than reference Kanamycin. Conjugates 5b was the most effective against B subtilis of all the synthesized conjugates, with IC50 values of (IC50: 215 ± 1.3 μM). The free radical scavenging capacity of each compound was determined using the DPPH and ABTS assays. Conjugates 4b (IC50: 53 ± 3.6 μM), 4c (IC50: 58 ± 1.3 μM), 4d (IC50: 57 ± 2.5 μM), 5b (IC50: 29 ± 1.5 μM) and 4a (IC50: 56 ± 4.3 μM) have greater antioxidant capacity than ferulic acid and ascorbic acid in the DPPH assay. Whereas in the ABTS assay, compounds 4b (IC50: 7 ± 1.8 μM), 5b (IC50: 5 ± 0.7 μM), 4a (IC50: 9 ± 3.2 μM), 4g (IC50: 7 ± 2.3 μM), and 5a (IC50: 8 ± 4.3 μM) showed more antioxidant activity than ferulic acid, p-coumaric acid and ascorbic acid. Thus, a large library of compounds derived from bile acid can be easily synthesized for extensive structure-activity relationship studies in order to identify the most appropriate antibacterial and antioxidant agents.
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