Synthetic flavokawain analog (E)-1-(2'-hydroxy-4',6'-dimethoxyphenyl)-3-(3-methoxy-4-(3-morpholinopropoxy)phenyl)prop-2-en-1-one (FK-morph) effectively regresses endometriotic implants in rats

Chen J, Jing Chen, Zhenghuan Rao, Rao Z, Qinqin Li, Li Q, Tao Jiang, Jiang T, Yuan Chen, Chen Y, Xia Gu, Gu X, Miao M, Mengyue Miao, Daifeng Hu, Hu D, Zhou H, Hui Zhou, Teichmann AT, A. Teíchmann, Alexander Tobias Teichmann, Yang Y, Youzhe Yang
European journal of pharmacology · 2022 · vol. 933 , pp. 175240 · doi:10.1016/j.ejphar.2022.175240 · PMID:36055364 · W4293722853
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The synthetic flavokawain analog FK-morph effectively regressed endometriotic implants in rats by reducing inflammatory factors, promoting apoptosis, and attenuating angiogenesis, potentially via PI3K/Akt and NF-κB pathway inhibition.

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Abstract

Endometriosis is an estrogen-dependent inflammatory gynecological disorder that is pathologically defined as the growth of endometrial glands and stroma outside of the uterine cavity. It is estimated that more than 15% of women of reproductive age are affected by endometriosis. Immunological and inflammatory responses, anti-apoptotic effects and angiogenesis processes have been reported to be involved in endometriosis. Surgery and pharmacotherapy are applied in the treatment of this disease. Frustratingly, a high recurrence rate and/or side effects are observed during and after the treatments. In our previous study, we designed and synthesized serial analogs of naturally occurring flavokawain chalcones. Among these molecules, FK-morph exhibited excellent anti-inflammatory activity and showed therapeutic potential in vitro and in vivo. In the current study, we demonstrate the beneficial effects of FK-morph on a surgically induced endometriosis rat model. After treatment with FK-morph, the volumes and adhesion scores of implants in rats were effectively reduced and the levels of inflammatory cytokines and related chemokines in peritoneal fluid and blood were significantly downregulated. FK-morph also mediated cell apoptosis of endometriosis foci. In addition, the angiogenesis process was attenuated by decreasing the expression of VEGF. Meanwhile, the underlying mechanism was further explored. FK-morph effectively reduced the expression of Akt, p-Akt, PI3K, p-PI3K and NF-κB in endometriosis lesions. Overall, the results revealed the efficacy of FK-morph against endometriosis by reducing the levels of inflammatory factors, accelerating apoptosis and attenuating angiogenesis, which may be associated with blocking the activation of the PI3K/Akt and NF-κB signaling pathways.

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Condition tags

endometriosis

MeSH descriptors

Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones Chalcones

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

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