Fatima Samreen, Mohapatra Lucy, Mishra Deepak, Tripathi Alok S, Khan Anwar
Amity Institute of Pharmacy, Lucknow, Amity University Uttar Pradesh, Sector 125, Noida, Uttar Pradesh, India.
Era College of Pharmacy, Era University, Lucknow, Uttar Pradesh, India.
Reprod Sci. 2025 Feb;32(2):382-394. doi: 10.1007/s43032-024-01771-w. Epub 2025 Jan 10.
PCOS is a common endocrine disorder in women particularly in their reproductive age. GABA has been implicated in the pathogenesis of PCOS through its central role in the hypothalamus. Hence, in this study we investigated the effect of Nipecotic acid (NPA) in Letrozole induced PCOS in female Wistar rats as NPA has been proven as a GABA uptake inhibitor. In this study 30 female Wistar rats were divided into 5 groups each group containing 6 animals and treated as follows-Healthy control: Vehicle, 0.5% carboxymethylcellulose (CMC); Diseased control: Letrozole 1 mg/kg orally in 0.5% CMC; Test group-1: Letrozole + NPA (2.5 mg/kg i.p.); Test group-2: Letrozole + NPA (5 mg/kg i.p.) and Standard group: Letrozole + Clomiphene citrate (1 mg/kg in 0.5% CMC orally). Body weight, feed intake, water intake and vaginal smear was recorded on daily basis till the completion of the treatment tenure, whereas serum oestrogen, testosterone and GABA; ovary and uterus histopathology; lipid profile; OGTT; GsH, MDA and TNF-alpha in ovary tissue were estimated in the end of the treatment tenure. NPA treated groups demonstrated an improvement in the irregularities of the oestrous cycle with respect to PCOS control group. Further, NPA at both doses significantly (p < 0.001) reduced oxidative stress and inflammation in the ovary. It significantly (p < 0.001) reduced the serum testosterone and significantly (p < 0.001) elevated the serum oestrogen level. Histopathological reports depicted NPA reduced follicular cysts and promoted ovulation. These results emphasize the possibility of NPA as a treatment option for PCOS related reproductive and metabolic disorders, addressing the unmet need for effective PCOS management.
多囊卵巢综合征(PCOS)是女性尤其是育龄期女性常见的内分泌紊乱疾病。γ-氨基丁酸(GABA)因其在下丘脑的核心作用而与PCOS的发病机制有关。因此,在本研究中,我们研究了尼克酸(NPA)对来曲唑诱导的雌性Wistar大鼠PCOS的影响,因为NPA已被证明是一种GABA摄取抑制剂。在本研究中,30只雌性Wistar大鼠被分为5组,每组6只动物,并进行如下处理:健康对照组:赋形剂,0.5%羧甲基纤维素(CMC);疾病对照组:0.5% CMC中口服来曲唑1 mg/kg;试验组-1:来曲唑+ NPA(2.5 mg/kg腹腔注射);试验组-2:来曲唑+ NPA(5 mg/kg腹腔注射);标准组:来曲唑+枸橼酸氯米芬(0.5% CMC中1 mg/kg口服)。在治疗期结束前每天记录体重、采食量、饮水量和阴道涂片,而在治疗期结束时测定血清雌激素、睾酮和GABA;卵巢和子宫组织病理学;血脂谱;口服葡萄糖耐量试验(OGTT);卵巢组织中的谷胱甘肽(GsH)、丙二醛(MDA)和肿瘤坏死因子-α(TNF-α)。与PCOS对照组相比,NPA治疗组的发情周期不规则情况有所改善。此外,两种剂量的NPA均显著(p < 0.001)降低了卵巢中的氧化应激和炎症。它显著(p < 0.001)降低了血清睾酮水平,并显著(p < 0.001)提高了血清雌激素水平。组织病理学报告显示NPA减少了卵泡囊肿并促进了排卵。这些结果强调了NPA作为PCOS相关生殖和代谢紊乱治疗选择的可能性,满足了有效管理PCOS的未满足需求。