Active Substances from Callicarpa nudiflora Exert Anti-Cervicitis Effects and Regulate NLRP3-Associated Inflammation

Luohuazizhu suppository is a Traditional Chinese Medicine used in clinic to treat cervicitis, which is prepared from Callicarpa nudiflora Hook. et Arn (C. nudiflora), an herbal Chinese medicine named Luohuazizhu. This study aimed to figure out the active constituents of C. nudiflora and the potentia...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-10, Vol.26 (20), p.6217
Main Authors: Liu, Tianchi, Wang, Ruiqi, Liu, Chenpeng, Lu, Jiahong, Wang, Yitao, Dong, Lin, Zhang, Xiaopo
Format: Article
Language:English
Subjects:
active substances
anti-cervicitis
Antibiotics
Butanol
Callicarpa
Callicarpa nudiflora
Cell growth
Cervicitis
Chinese medicine
Clinics
Cytokines
Cytotoxicity
Dichloromethane
Diterpenes
diterpenoids
Drug dosages
Drug resistance
Ethanol
Herbal medicine
Inflammation
NLRP3
Pathogens
Petroleum ether
Thymus gland
Vagina
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Summary:Luohuazizhu suppository is a Traditional Chinese Medicine used in clinic to treat cervicitis, which is prepared from Callicarpa nudiflora Hook. et Arn (C. nudiflora), an herbal Chinese medicine named Luohuazizhu. This study aimed to figure out the active constituents of C. nudiflora and the potential mechanism for its anti-cervicitis effect. The ethanol extract in C. nudiflora (CNE) and the different fractions of CNE extracted by petroleum ether (CNE-p), dichloromethane (CNE-d), and n-butanol (CNE-b) were tested in vivo for their anti-cervicitis effects. Then the isolated compounds from the CNE-p were tested in vitro for their anti-inflammatory activities. The results displayed that CNE-p, CNE-d, and CNE-b exhibited adequate anti-cervicitis effects, with CNE-p showing the highest efficacy. Further experiment demonstrated that CNE-p could significantly inhibit the expression of NLRP3 in vitro. Six diterpenoids obtained from the CNE-p showed the ability to regulate inflammatory factor levels in vitro. Among these compounds, compounds 1 (callicarpic acid A) and 2 (syn-3,4-seco-12S-hydroxy-15,16-epoxy-4(18),8(17),3(16),14(15)-labdatetraen-3-oic acid) were the most effective agents, and they also inhibited the expression level of NLRP3 in vitro. The results confirmed that C. nudiflora has significant anti-cervicitis effects and the diterpenoids were most likely to be its active components. These data provide scientific support for the clinic usage of Luohuazizhu suppository and the development of new agents in treating cervicitis.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26206217