Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines
Pinocembrin (PCB), a flavonoid known for its anti-inflammatory properties, has been approved for various clinical trial applications. To evaluate deeper into the anti-inflammatory potential of the specific enantiomer of natural PCB, we conducted the first investigation into the efficacy of the pure...
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| Format: | Article |
| Language: | English |
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Wiley
2024-01-01
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| Series: | Advances in Pharmacological and Pharmaceutical Sciences |
| Online Access: | http://dx.doi.org/10.1155/2024/8811022 |
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| author | Hilwan Yuda Teruna Kamal Rullah Rudi Hendra Rahayu Utami Deri Islami Siti Munirah Mohd Faudzi Mohd Fadhlizil Fasihi Mohd Aluwi Kok Wai Lam |
| author_facet | Hilwan Yuda Teruna Kamal Rullah Rudi Hendra Rahayu Utami Deri Islami Siti Munirah Mohd Faudzi Mohd Fadhlizil Fasihi Mohd Aluwi Kok Wai Lam |
| author_sort | Hilwan Yuda Teruna |
| collection | DOAJ |
| description | Pinocembrin (PCB), a flavonoid known for its anti-inflammatory properties, has been approved for various clinical trial applications. To evaluate deeper into the anti-inflammatory potential of the specific enantiomer of natural PCB, we conducted the first investigation into the efficacy of the pure enantiomer (2S)-PCB in modulating inflammatory mediators induced by lipopolysaccharide (LPS) in both murine RAW 264.7 and human U937 macrophage cell lines. This particular compound was isolated from Goniothalamus macrophyllus (Annonaceae), a native plant of Indonesia. This plant has been used traditionally as an herbal medicine to alleviate inflammation. (2S)-PCB was isolated from the stem bark of G. macrophyllus by defatting with n-hexane followed by maceration with methanol. Purification was performed using several chromatographic techniques. The absolute configuration was determined using electronic circular dichroism (ECD) spectroscopy. This compound was then tested for its inhibitory activity on prostaglandin E2 (PGE2) and subjected to docking simulations. The results indicated that (2S)-PCB significantly suppressed the production of PGE2 induced by LPS in both RAW 264.7 and U937 cell lines. The docking simulations revealed that (2S)-PCB reduced PGE2 levels by suppressing mitogen-activated protein kinase (MAPK) activation through inhibiting p38 and extracellular signal-regulated kinases (ERK). These findings suggest that the compound may prevent worsening of septic shock caused by bacterial infection. |
| format | Article |
| id | doaj-art-5ec484ec3c8f4286ab9756e217389bef |
| institution | Kabale University |
| issn | 2633-4690 |
| language | English |
| publishDate | 2024-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Advances in Pharmacological and Pharmaceutical Sciences |
| spelling | doaj-art-5ec484ec3c8f4286ab9756e217389bef2025-02-03T06:51:37ZengWileyAdvances in Pharmacological and Pharmaceutical Sciences2633-46902024-01-01202410.1155/2024/8811022Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell LinesHilwan Yuda Teruna0Kamal Rullah1Rudi Hendra2Rahayu Utami3Deri Islami4Siti Munirah Mohd Faudzi5Mohd Fadhlizil Fasihi Mohd Aluwi6Kok Wai Lam7Department of ChemistryDepartment of Pharmaceutical ChemistryDepartment of ChemistryDepartment of PharmacyDepartment of PharmacyNatural Medicines and Product Research Laboratory (NaturMeds)Faculty of Industrial Sciences and TechnologyDrugs and Herbal Research CentrePinocembrin (PCB), a flavonoid known for its anti-inflammatory properties, has been approved for various clinical trial applications. To evaluate deeper into the anti-inflammatory potential of the specific enantiomer of natural PCB, we conducted the first investigation into the efficacy of the pure enantiomer (2S)-PCB in modulating inflammatory mediators induced by lipopolysaccharide (LPS) in both murine RAW 264.7 and human U937 macrophage cell lines. This particular compound was isolated from Goniothalamus macrophyllus (Annonaceae), a native plant of Indonesia. This plant has been used traditionally as an herbal medicine to alleviate inflammation. (2S)-PCB was isolated from the stem bark of G. macrophyllus by defatting with n-hexane followed by maceration with methanol. Purification was performed using several chromatographic techniques. The absolute configuration was determined using electronic circular dichroism (ECD) spectroscopy. This compound was then tested for its inhibitory activity on prostaglandin E2 (PGE2) and subjected to docking simulations. The results indicated that (2S)-PCB significantly suppressed the production of PGE2 induced by LPS in both RAW 264.7 and U937 cell lines. The docking simulations revealed that (2S)-PCB reduced PGE2 levels by suppressing mitogen-activated protein kinase (MAPK) activation through inhibiting p38 and extracellular signal-regulated kinases (ERK). These findings suggest that the compound may prevent worsening of septic shock caused by bacterial infection.http://dx.doi.org/10.1155/2024/8811022 |
| spellingShingle | Hilwan Yuda Teruna Kamal Rullah Rudi Hendra Rahayu Utami Deri Islami Siti Munirah Mohd Faudzi Mohd Fadhlizil Fasihi Mohd Aluwi Kok Wai Lam Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines Advances in Pharmacological and Pharmaceutical Sciences |
| title | Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines |
| title_full | Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines |
| title_fullStr | Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines |
| title_full_unstemmed | Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines |
| title_short | Inhibitory Effect of (2S)-Pinocembrin From Goniothalamus macrophyllus on the Prostaglandin E2 Production in Macrophage Cell Lines |
| title_sort | inhibitory effect of 2s pinocembrin from goniothalamus macrophyllus on the prostaglandin e2 production in macrophage cell lines |
| url | http://dx.doi.org/10.1155/2024/8811022 |
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