A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms
Background: Rhinovirus (RV) infection is a major cause of common colds and asthma exacerbations, with no antiviral drug available. Curcumin exhibits broad-spectrum antiviral activities, but its therapeutic effect is limited by a poor pharmacokinetics profile. Curcumin-like diarylpentanoid analogs, p...
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| Format: | Article |
| Language: | English |
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Springer
2024
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| Online Access: | http://psasir.upm.edu.my/id/eprint/115523/ http://psasir.upm.edu.my/id/eprint/115523/1/115523.pdf |
| _version_ | 1848866799230124032 |
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| author | Liew, Kong Yen Chee, Hui-Yee Abas, Faridah Leong, Sze Wei Harith, Hanis Hazeera Ahmad Israf, Daud Sulaiman, Mohd Roslan Tham, Chau Ling |
| author_facet | Liew, Kong Yen Chee, Hui-Yee Abas, Faridah Leong, Sze Wei Harith, Hanis Hazeera Ahmad Israf, Daud Sulaiman, Mohd Roslan Tham, Chau Ling |
| author_sort | Liew, Kong Yen |
| building | UPM Institutional Repository |
| collection | Online Access |
| description | Background: Rhinovirus (RV) infection is a major cause of common colds and asthma exacerbations, with no antiviral drug available. Curcumin exhibits broad-spectrum antiviral activities, but its therapeutic effect is limited by a poor pharmacokinetics profile. Curcumin-like diarylpentanoid analogs, particularly 2-benzoyl-6-(3,4-dihydroxybenzylidene)cyclohexen-1-ol (BDHBC) and 5-(3,4-dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one (DHHPD), have better solubility and stability compared to curcumin. Objectives: Therefore, this study aims to evaluate and compare the antiviral effects of curcumin, BDHBC, and DHHPD in an in vitro model of RV infection. Methods: The inhibitory effects on RV-16 infection in H1 HeLa cells were assessed using cytopathic effect (CPE) reduction assay, virus yield reduction assay, RT-qPCR, and Western blot. Antiviral effects in different modes of treatment (pre-, co-, and post-treatment) were also compared. Additionally, intercellular adhesion molecule 1 (ICAM-1) expression, RV binding, and infectivity were measured with Western blot, flow cytometry, and virucidal assay, respectively. Results: When used as a post-treatment, BDHBC (EC50: 4.19 µM; SI: 8.32) demonstrated stronger antiviral potential on RV-16 compared to DHHPD (EC50: 18.24 µM; SI: 1.82) and curcumin (less than 50% inhibition). BDHBC also showed the strongest inhibitory effect on RV-induced CPE, virus yield, vRNA, and viral proteins (P1, VP0, and VP2). Furthermore, BDHBC pre-treatment has a prophylactic effect against RV infection, which was attributed to reduced basal expression of ICAM-1. However, it did not affect virus binding, but exerted virucidal activity on RV-16, contributing to its antiviral effect during co-treatment. Conclusion: BDHBC exhibits multiple antiviral mechanisms against RV infection and thus could be a potential antiviral agent for RV. Graphical Abstract: (Figure presented.) |
| first_indexed | 2025-11-15T14:26:20Z |
| format | Article |
| id | upm-115523 |
| institution | Universiti Putra Malaysia |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T14:26:20Z |
| publishDate | 2024 |
| publisher | Springer |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | upm-1155232025-04-21T02:51:01Z http://psasir.upm.edu.my/id/eprint/115523/ A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms Liew, Kong Yen Chee, Hui-Yee Abas, Faridah Leong, Sze Wei Harith, Hanis Hazeera Ahmad Israf, Daud Sulaiman, Mohd Roslan Tham, Chau Ling Background: Rhinovirus (RV) infection is a major cause of common colds and asthma exacerbations, with no antiviral drug available. Curcumin exhibits broad-spectrum antiviral activities, but its therapeutic effect is limited by a poor pharmacokinetics profile. Curcumin-like diarylpentanoid analogs, particularly 2-benzoyl-6-(3,4-dihydroxybenzylidene)cyclohexen-1-ol (BDHBC) and 5-(3,4-dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one (DHHPD), have better solubility and stability compared to curcumin. Objectives: Therefore, this study aims to evaluate and compare the antiviral effects of curcumin, BDHBC, and DHHPD in an in vitro model of RV infection. Methods: The inhibitory effects on RV-16 infection in H1 HeLa cells were assessed using cytopathic effect (CPE) reduction assay, virus yield reduction assay, RT-qPCR, and Western blot. Antiviral effects in different modes of treatment (pre-, co-, and post-treatment) were also compared. Additionally, intercellular adhesion molecule 1 (ICAM-1) expression, RV binding, and infectivity were measured with Western blot, flow cytometry, and virucidal assay, respectively. Results: When used as a post-treatment, BDHBC (EC50: 4.19 µM; SI: 8.32) demonstrated stronger antiviral potential on RV-16 compared to DHHPD (EC50: 18.24 µM; SI: 1.82) and curcumin (less than 50% inhibition). BDHBC also showed the strongest inhibitory effect on RV-induced CPE, virus yield, vRNA, and viral proteins (P1, VP0, and VP2). Furthermore, BDHBC pre-treatment has a prophylactic effect against RV infection, which was attributed to reduced basal expression of ICAM-1. However, it did not affect virus binding, but exerted virucidal activity on RV-16, contributing to its antiviral effect during co-treatment. Conclusion: BDHBC exhibits multiple antiviral mechanisms against RV infection and thus could be a potential antiviral agent for RV. Graphical Abstract: (Figure presented.) Springer 2024-10-12 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/115523/1/115523.pdf Liew, Kong Yen and Chee, Hui-Yee and Abas, Faridah and Leong, Sze Wei and Harith, Hanis Hazeera and Ahmad Israf, Daud and Sulaiman, Mohd Roslan and Tham, Chau Ling (2024) A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms. DARU Journal of Pharmaceutical Sciences, 32. pp. 729-744. ISSN 2008-2231 https://link.springer.com/article/10.1007/s40199-024-00542-x?error=cookies_not_supported&code=b045a627-1eab-42d3-942c-f3e426ee307e 10.1007/s40199-024-00542-x |
| spellingShingle | Liew, Kong Yen Chee, Hui-Yee Abas, Faridah Leong, Sze Wei Harith, Hanis Hazeera Ahmad Israf, Daud Sulaiman, Mohd Roslan Tham, Chau Ling A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms |
| title | A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms |
| title_full | A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms |
| title_fullStr | A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms |
| title_full_unstemmed | A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms |
| title_short | A synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in H1 hela cells via multiple antiviral mechanisms |
| title_sort | synthetic curcumin-like diarylpentanoid analog inhibits rhinovirus infection in h1 hela cells via multiple antiviral mechanisms |
| url | http://psasir.upm.edu.my/id/eprint/115523/ http://psasir.upm.edu.my/id/eprint/115523/ http://psasir.upm.edu.my/id/eprint/115523/ http://psasir.upm.edu.my/id/eprint/115523/1/115523.pdf |