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Suppressive Effect of Two Cucurbitane-Type Triterpenoids from Momordica charantia on Cutibacterium acnes-Induced Inflammatory Responses in Human THP-1 Monocytic Cell and Mouse Models

1
Department of Biotechnology and Pharmaceutical Technology, Yuanpei University of Medical Technology, Hsinchu 300, Taiwan
2
Department of Human Development and Family Studies, National Taiwan Normal University, Taipei 106, Taiwan
3
Master Program in Food Safety, College of Nutrition, Taipei Medical University, Taipei 110, Taiwan
4
Hualien District Agricultural Research and Extension Station, Hualien 973, Taiwan
5
Department of Biological Science and Technology, National Pingtung University of Science and Technology, Pingtung 912, Taiwan
6
Department of Dermatology, Taipei Municipal Wan Fang Hospital and Taipei Medical University, Taipei 116, Taiwan
7
Program of Nutrition Science, School of Life Science, National Taiwan Normal University, Taipei 116, Taiwan
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Arduino A. Mangoni
Molecules 2021, 26(3), 579; https://doi.org/10.3390/molecules26030579
Received: 21 December 2020 / Revised: 19 January 2021 / Accepted: 20 January 2021 / Published: 22 January 2021
(This article belongs to the Special Issue Anti-inflammatory and Anti-allergy Agents in Medicinal Chemistry-III)
Cutibacterium acnes (formerly Propionibacterium acnes) is one of the major bacterial species responsible for acne vulgaris. Numerous bioactive compounds from Momordica charantia Linn. var. abbreviata Ser. have been isolated and examined for many years. In this study, we evaluated the suppressive effect of two cucurbitane-type triterpenoids, 5β,19-epoxycucurbita-6,23-dien-3β,19,25-triol (Kuguacin R; KR) and 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (TCD) on live C. acnes-stimulated in vitro and in vivo inflammatory responses. Using human THP-1 monocytes, KR or TCD suppressed C. acnes-induced production of interleukin (IL)-1β, IL-6 and IL-8 at least above 56% or 45%, as well as gene expression of these three pro-inflammatory cytokines. However, a significantly strong inhibitory effect on production and expression of tumor necrosis factor (TNF)-α was not observed. Both cucurbitanes inhibited C. acnes-induced activation of the myeloid differentiation primary response 88 (MyD88) (up to 62%) and mitogen-activated protein kinases (MAPK) (at least 36%). Furthermore, TCD suppressed the expression of pro-caspase-1 and cleaved caspase-1 (p10). In a separate study, KR or TCD decreased C. acnes-stimulated mouse ear edema by ear thickness (20% or 14%), and reduced IL-1β-expressing leukocytes and neutrophils in mouse ears. We demonstrated that KR and TCD are potential anti-inflammatory agents for modulating C. acnes-induced inflammation in vitro and in vivo. View Full-Text
Keywords: acne; Cutibacterium acnes; Momordica charantia; anti-inflammation; kuguacin R; 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (TCD) acne; Cutibacterium acnes; Momordica charantia; anti-inflammation; kuguacin R; 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (TCD)
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MDPI and ACS Style

Chuang, L.-T.; Huang, W.-C.; Hou, Y.-C.; Chyuan, J.-H.; Chang, H.; Chang, C.-I.; Tsai, T.-H.; Tsai, P.-J. Suppressive Effect of Two Cucurbitane-Type Triterpenoids from Momordica charantia on Cutibacterium acnes-Induced Inflammatory Responses in Human THP-1 Monocytic Cell and Mouse Models. Molecules 2021, 26, 579. https://doi.org/10.3390/molecules26030579

AMA Style

Chuang L-T, Huang W-C, Hou Y-C, Chyuan J-H, Chang H, Chang C-I, Tsai T-H, Tsai P-J. Suppressive Effect of Two Cucurbitane-Type Triterpenoids from Momordica charantia on Cutibacterium acnes-Induced Inflammatory Responses in Human THP-1 Monocytic Cell and Mouse Models. Molecules. 2021; 26(3):579. https://doi.org/10.3390/molecules26030579

Chicago/Turabian Style

Chuang, Lu-Te, Wen-Cheng Huang, Yu-Chen Hou, Jong-Ho Chyuan, Hsiang Chang, Chi-I Chang, Tsung-Hsien Tsai, and Po-Jung Tsai. 2021. "Suppressive Effect of Two Cucurbitane-Type Triterpenoids from Momordica charantia on Cutibacterium acnes-Induced Inflammatory Responses in Human THP-1 Monocytic Cell and Mouse Models" Molecules 26, no. 3: 579. https://doi.org/10.3390/molecules26030579

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