Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation

Dysoxylum tpongense Pierre (local name ‘Huynh Dan Bap’) belonging to family Meliaceae, is a tree (3–10 m height), distributed in the mountainous areas (ca. 1000 m a.s.l.) in North Vietnam. From the dichloromethane fraction of the methanol extract of the leaves and stems of this plant, six dammarane...

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Tác giả chính: Ngoc Khanh Pham, Huu Tai Bui, Thu Huong Tran, Thi Ngoc Anh Hoang, Thi Ha Vu, Dinh Tung Do, Young Ho Kim, Seok Bean Song, Dao CuongTo, Manh Cuong Nguyen
Định dạng: Bài trích
Ngôn ngữ:English
Nhà xuất bản: Steroids 2021
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Truy cập trực tuyến:https://www.sciencedirect.com/science/article/abs/pii/S0039128X21001148?via%3Dihub
https://dlib.phenikaa-uni.edu.vn/handle/PNK/3299
https://doi.org/10.1016/j.steroids.2021.108902
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spelling oai:localhost:PNK-32992022-08-17T05:54:46Z Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation Ngoc Khanh Pham Huu Tai Bui Thu Huong Tran Thi Ngoc Anh Hoang Thi Ha Vu Dinh Tung Do Young Ho Kim Seok Bean Song Dao CuongTo Manh Cuong Nguyen Liver X receptor (LXR) Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB) Dysoxylum tpongense Pierre (local name ‘Huynh Dan Bap’) belonging to family Meliaceae, is a tree (3–10 m height), distributed in the mountainous areas (ca. 1000 m a.s.l.) in North Vietnam. From the dichloromethane fraction of the methanol extract of the leaves and stems of this plant, six dammarane triterpenes, one furanoid diterpene together with three sterols were isolated. Evaluation of biological activities of isolated compounds showed that cabraleahydroxylactone (5), cabraleahydroxylactone 3-acetate (6), and stigmast-4-en-3-one (10) possessed an anti-inflammatory effect against Liver X receptor (LXR) activation in HepG2 cell line model with IC50 values of 20.29 ± 3.69, 24.32 ± 2.99, and 7.09 ± 0.97 (μM), respectively. While three other triterpenoid compounds aglinin C 3- acetate (1), aglinin C (2), and 24-epi-cabraleadiol (4) presented the most significant inhibitory effect against TNF-α induced NF-κB activation in HepG2 cell line in a dose-dependent manner with IC50 values of 12.45 ± 2.37, 23.32 ± 3.25, and 13.95 ± 1.57 μM, respectively. As stigmast-4-en-3-one (10), with structure closely similar to cholesterol, acted selectively on LXRs but not on NF-kB activation pathway, this suggests that stigmast-4-en-3-one (10) can be potentially applied as an agonist on LXR signaling pathway. Pathways LXRs-NF-κB-iNOS expression have a close relationship and play a crucial role in proceeding metabolic abnormalities like atherosclerosis, obesity, inflammation, etc. Thus, the findings showed that dammarane-type triterpenoids from D. tpongense are worthy of further investigation for potential LXR agonists and potent anti-atherogenic agents against atherosclerotic lesion progression. 2021-10-27T02:05:04Z 2021-10-27T02:05:04Z 2021 Bài trích https://www.sciencedirect.com/science/article/abs/pii/S0039128X21001148?via%3Dihub https://dlib.phenikaa-uni.edu.vn/handle/PNK/3299 https://doi.org/10.1016/j.steroids.2021.108902 en Steroids
institution Digital Phenikaa
collection Digital Phenikaa
language English
topic Liver X receptor (LXR)
Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB)
spellingShingle Liver X receptor (LXR)
Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB)
Ngoc Khanh Pham
Huu Tai Bui
Thu Huong Tran
Thi Ngoc Anh Hoang
Thi Ha Vu
Dinh Tung Do
Young Ho Kim
Seok Bean Song
Dao CuongTo
Manh Cuong Nguyen
Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation
description Dysoxylum tpongense Pierre (local name ‘Huynh Dan Bap’) belonging to family Meliaceae, is a tree (3–10 m height), distributed in the mountainous areas (ca. 1000 m a.s.l.) in North Vietnam. From the dichloromethane fraction of the methanol extract of the leaves and stems of this plant, six dammarane triterpenes, one furanoid diterpene together with three sterols were isolated. Evaluation of biological activities of isolated compounds showed that cabraleahydroxylactone (5), cabraleahydroxylactone 3-acetate (6), and stigmast-4-en-3-one (10) possessed an anti-inflammatory effect against Liver X receptor (LXR) activation in HepG2 cell line model with IC50 values of 20.29 ± 3.69, 24.32 ± 2.99, and 7.09 ± 0.97 (μM), respectively. While three other triterpenoid compounds aglinin C 3- acetate (1), aglinin C (2), and 24-epi-cabraleadiol (4) presented the most significant inhibitory effect against TNF-α induced NF-κB activation in HepG2 cell line in a dose-dependent manner with IC50 values of 12.45 ± 2.37, 23.32 ± 3.25, and 13.95 ± 1.57 μM, respectively. As stigmast-4-en-3-one (10), with structure closely similar to cholesterol, acted selectively on LXRs but not on NF-kB activation pathway, this suggests that stigmast-4-en-3-one (10) can be potentially applied as an agonist on LXR signaling pathway. Pathways LXRs-NF-κB-iNOS expression have a close relationship and play a crucial role in proceeding metabolic abnormalities like atherosclerosis, obesity, inflammation, etc. Thus, the findings showed that dammarane-type triterpenoids from D. tpongense are worthy of further investigation for potential LXR agonists and potent anti-atherogenic agents against atherosclerotic lesion progression.
format Bài trích
author Ngoc Khanh Pham
Huu Tai Bui
Thu Huong Tran
Thi Ngoc Anh Hoang
Thi Ha Vu
Dinh Tung Do
Young Ho Kim
Seok Bean Song
Dao CuongTo
Manh Cuong Nguyen
author_facet Ngoc Khanh Pham
Huu Tai Bui
Thu Huong Tran
Thi Ngoc Anh Hoang
Thi Ha Vu
Dinh Tung Do
Young Ho Kim
Seok Bean Song
Dao CuongTo
Manh Cuong Nguyen
author_sort Ngoc Khanh Pham
title Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation
title_short Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation
title_full Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation
title_fullStr Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation
title_full_unstemmed Dammarane triterpenes and phytosterols from Dysoxylum tpongense Pierre and their anti-inflammatory activity against liver X receptors and NF-κB activation
title_sort dammarane triterpenes and phytosterols from dysoxylum tpongense pierre and their anti-inflammatory activity against liver x receptors and nf-κb activation
publisher Steroids
publishDate 2021
url https://www.sciencedirect.com/science/article/abs/pii/S0039128X21001148?via%3Dihub
https://dlib.phenikaa-uni.edu.vn/handle/PNK/3299
https://doi.org/10.1016/j.steroids.2021.108902
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