Superior therapeutic and anti‐angiogenesis effects of oral Pro‐drug of green tea EGCG than other catechins, GnRH analogue and VEGFR inhibitor for treatment of endometriosis
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香港中文大學研究人員

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摘要Objective:
Green tea epigallocatchin‐3‐gallate (EGCG) inhibit angiogenesis of endometriosis, but suffer from poor bioavailability. Octacetate derivatives as prodrug of EGCG (Pro‐EGCG) increase stability and bioavailability and selectively enhance the efficacy to inhibit angiogenesis and growth of endometriosis. We aimed to compare oral Pro‐EGCG with
other catechins, GnRH analogue and VEGFR inhibitor.
Design:
Endometrial cells from patients and animal models of endometriosis were employed to study anti‐angiogenesis and anti‐endometriosis effects. Endometriosis was induced by syngeneic endometrium subcutaneous transplantation in mice. Then the mice were randomly administered with either EGCG, Pro‐EGCG, Decapeptyl, Vatalanib/PTK787 or
vehicle for 8 weeks and then withdrawn for 4 weeks.
Materials and methods:
Lesion size were monitored during the interventions. Lesion weight and histology were examined at the end of interventions. Anti‐angiogenesis, anti‐apoptosis, and antioxidative activities were compared. Body, uterus and ovary weights, blood glucose, female reproductive hormone levels, liver and renal functions, endometrial glands and
thickness, and follicle counts were determined.
Results:
Lesion sizes under Pro‐EGCG treatment at 25‐50mg/kg and 50mg/kg po were significantly smaller than 3mg/kg Decapeptyl sc, 50mg/kg Vatalanib/PTK787 ip and 50mg/kg ECGC ip after 3 weeks, while 50mg/kg EGCG po has no effects. Pro‐EGCG at 25mg/kg achieved and maintained the smallest lesion size at 4 weeks and after 8 weeks.
Under Pro‐EGCG treatment, endometriotic lesion development showed limited endometrial‐like structures and decreased glandular epithelium, restricted microvessel development and decreased oxidative stress and enhanced anti‐oxidative capacity. Lesion sizes under pro‐EGCG at 25‐50mg/kg po remained underdeveloped after withdrawal. Whereas lesion sizes after withdrawal of Decapeptyl, Vatalanib/PTK787 and EGCG ip rebound. There were no significant changes in body, uterus and ovary weights; blood glucose, E2 and P levels; endometrial gland counts and thickness; and antral follicle counts.
Conclusion:
There is an urgent need in seeking better therapeutic approaches for endometriosis. Oral EGCG shows no effects but oral Pro‐EGCG demonstrates significant biological activities with superior efficacy and safety profiles than other current and new medical treatment. Pro‐EGCG as an anti‐angiogenesis agent will be a novel treatment for endometriosis.
著者Wang Chi Chiu , Man Chi Wai Gene, Zhang Tao , Chu Kai On , Xu Hui , Chan Tak Hang Bill
會議名稱The 13th World Congress on Endometriosis
會議開始日17.05.2017
會議完結日20.05.2017
會議地點Vancouver
會議國家/地區加拿大
出版年份2017
語言美式英語
關鍵詞green tea, EGCG, pro‐drug

上次更新時間 2018-18-01 於 03:06