Triptorelin ([DTrp6]-LH-RH)

Triptorelin ([DTrp6]-LH-RH) is a highly selective agonist of gonadotropin-releasing hormone (GnRH)^[1]. Triptorelin binds to GnRH receptors to stimulate the release of gonadotropins, thereby regulating sex hormone levels^[2]. Triptorelin can be used to treat a variety of sex hormone-related diseases, such as prostate cancer, endometriosis, and uterine fibroids^[3]. Triptorelin can also be used to control puberty development and inhibit precocious puberty^[4].

In vitro, gold nanoparticles conjugated with Triptorelin peptide (Triptorelin-AuNPs) were used to pretreat MCF-7 breast cancer cells at a concentration of 20μg/ml for 24 hours, followed by irradiation with 6MeV X-rays at doses of 2, 4, 6, and 8Gy. Triptorelin significantly enhanced the cells' sensitivity to radiation, while reducing cell survival and increasing apoptosis rates^[5]. Triptorelin (10nM–10μM) was used to treat the LNCaP prostate cancer cell line for 9 days. Triptorelin exhibited a dose-dependent inhibitory effect on LNCaP cells. Triptorelin (10μM) caused cell cycle arrest in the G0/G1 phase, reducing the proportion of cells in the S phase ^[6].

In vivo, Triptorelin (10, 20, 40μg; once daily) was administered via subcutaneous injection to 35-day-old KM mice for 7 consecutive days. Triptorelin significantly inhibited the growth and development of the uterus in mice, reduced uterine weight, and decreased endometrial epithelial thickness (EET) and uterine wall thickness (UWT)^[7]. Triptorelin (1mg/kg) was administered via intraperitoneal injection for 15 consecutive days after mice were treated with cyclophosphamide (75mg/kg) and/or doxorubicin (7.5mg/kg). Triptorelin significantly reduced the destructive effects of cyclophosphamide and/or doxorubicin on the utero-ovarian tissue in mice. Triptorelin significantly increased the number of primordial and pre-antral follicles and granulosa cells, and decreased the number of atretic follicles. Triptorelin also significantly improved the volume of the ovary and oocytes in the antral follicles in the damaged groups^[8].

References:
[1] Leone Roberti Maggiore U, Scala C, Remorgida V, et al. Triptorelin for the treatment of endometriosis. Expert Opin Pharmacother. 2014 Jun;15(8):1153-79.
[2] Fanelli D, Moroni R, Berti G, et al. GnRH analogue triptorelin acetate induces ovulation in jennies during oestrus. Reprod Domest Anim. 2024 Apr;59(4):e14555.
[3] Ploussard G, Mongiat-Artus P. Triptorelin in the management of prostate cancer. Future Oncol. 2013 Jan;9(1):93-102.
[4] Bertelloni S, Mucaria C, Baroncelli GI, et al. Triptorelin depot for the treatment of children 2 years and older with central precocious puberty. Expert Rev Clin Pharmacol. 2018 Jul;11(7):659-667.
[5] Tavakkoli E, Hashemi SM, Montazerabadi A, et al. In vitro study of effect of gold nanoparticles conjugated with triptorelin peptide on the radiosensitivity of breast cancer cells (MCF-7). Discov Oncol. 2025 Mar 26;16(1):404.
[6] Ravenna L, Salvatori L, Morrone S, et al. Effects of triptorelin, a gonadotropin-releasing hormone agonist, on the human prostatic cell lines PC3 and LNCaP. J Androl. 2000 Jul-Aug;21(4):549-57.
[7] Wei S, Guo H, Gong Z, Zhang F, et al. Triptorelin and cetrorelix induce immune responses and affect uterine development and expressions of genes and proteins of ESR1, LHR, and FSHR of mice. Immunopharmacol Immunotoxicol. 2016 Jun;38(3):197-204.
[8] Bahmanpour S, Ameri N, Zareifard N, et al. The Protective Effect of GnRH Agonist Triptorelin on the Histomorphometric Parameters of the Utero-ovarian Tissue in the Doxorubicin- and Cyclophosphamide-treated Mice. Cell Biochem Biophys. 2025 Mar;83(1):573-586.

Triptorelin ([DTrp6]-LH-RH)是一种促性腺激素释放激素（GnRH）的高选择性激动剂^[1]。Triptorelin通过与GnRH受体结合，刺激促性腺激素的释放，进而调节性激素水平^[2]。Triptorelin可用于治疗多种与性激素相关的疾病，如前列腺癌、子宫内膜异位症和子宫肌瘤等^[3]。Triptorelin还可用于控制青春期发育，抑制性早熟^[4]。

在体外，Triptorelin肽偶联的金纳米颗粒（Triptorelin-AuNPs）在20μg/ml的浓度下预处理MCF-7乳腺癌细胞24小时，随后以6MeV X射线进行2、4、6、8Gy的辐射处理，Triptorelin显著增强了细胞对辐射的敏感性，同时降低了细胞存活率并增加了凋亡率^[5]。Triptorelin（10nM–10μM）处理LNCaP前列腺细胞系9天，Triptorelin对LNCaP细胞表现出剂量依赖的抑制作用。Triptorelin（10μM）可使LNCaP细胞周期停滞在G0/G1期，减少S期细胞比例^[6]。

在体内，Triptorelin（10、20、40μg；每天一次）通过皮下注射，用于处理35天龄的KM小鼠，连续7天。Triptorelin显著抑制了小鼠子宫的生长和发育，降低了子宫重量，减少了子宫内膜上皮厚度（EET）和子宫壁厚度（UWT）^[7]。Triptorelin（1mg/kg）在小鼠接受环磷酰胺（75mg/kg）和/或阿霉素（7.5mg/kg）治疗后，通过腹腔注射连续给药15天。Triptorelin显著降低了环磷酰胺和/或阿霉素对小鼠子宫-卵巢组织的破坏性影响，Triptorelin显著增加了原始和前窦卵泡以及颗粒细胞的数量，降低了闭锁卵泡的数量。Triptorelin还显著改善了受损组小鼠的卵巢体积和窦卵泡中的卵母细胞的体积^[8]。