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肽的长效递送系统：通过可注射微胶囊控释[D-色氨酸6]促黄体生成素释放激素抑制大鼠前列腺肿瘤

Long-acting delivery systems for peptides: inhibition of rat prostate tumors by controlled release of [D-Trp6]luteinizing hormone-releasing hormone from injectable microcapsules.

作者信息

Redding T W, Schally A V, Tice T R, Meyers W E

出版信息

Proc Natl Acad Sci U S A. 1984 Sep;81(18):5845-8. doi: 10.1073/pnas.81.18.5845.

DOI:10.1073/pnas.81.18.5845
PMID:6237365
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC391808/
Abstract

Intramuscular injection of [6-D-tryptophan]-luteinizing hormone-releasing hormone [( D-Trp6]LH-RH) in microcapsules of poly(DL-lactide-co-glycolide), designed to release a controlled dose of the peptide over a 30-day period, decreased the weights of androgen-dependent Dunning prostate tumors in rats and suppressed serum testosterone levels more effectively than daily subcutaneous administration of equivalent or double doses of unencapsulated [D-Trp6]LH-RH. The microcapsules or daily injections of [D-Trp6]LH-RH also significantly decreased tumor volumes. Microcapsules of [D-Trp6]LH-RH or related analogs that can be injected once a month should make the treatment of patients with prostate carcinoma and other neoplasms or disorders more convenient and efficacious.

摘要

将[6-D-色氨酸]-促黄体生成激素释放激素[（D-Trp6）LH-RH]包裹于聚（DL-丙交酯-共-乙交酯）微胶囊中进行肌内注射，该微胶囊设计为在30天内释放可控剂量的肽，与每日皮下注射同等剂量或双倍剂量的未包裹[D-Trp6]LH-RH相比，更有效地减轻了大鼠雄激素依赖性邓宁前列腺肿瘤的重量，并抑制了血清睾酮水平。[D-Trp6]LH-RH微胶囊或每日注射[D-Trp6]LH-RH也显著减小了肿瘤体积。每月注射一次的[D-Trp6]LH-RH微胶囊或相关类似物应会使前列腺癌和其他肿瘤或疾病患者的治疗更加方便和有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b1b/391808/0a5e5fcd9a7e/pnas00619-0230-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b1b/391808/346712ca0c0c/pnas00619-0230-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b1b/391808/0a5e5fcd9a7e/pnas00619-0230-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b1b/391808/346712ca0c0c/pnas00619-0230-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b1b/391808/0a5e5fcd9a7e/pnas00619-0230-b.jpg

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Long-acting delivery systems for peptides: inhibition of rat prostate tumors by controlled release of [D-Trp6]luteinizing hormone-releasing hormone from injectable microcapsules.肽的长效递送系统：通过可注射微胶囊控释[D-色氨酸6]促黄体生成素释放激素抑制大鼠前列腺肿瘤
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Endocrine manipulation of the Dunning prostatic adenocarcinoma.邓宁前列腺腺癌的内分泌调控
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From contraception to cancer: a review of the therapeutic applications of LHRH analogues as antitumor agents.从避孕到癌症：促黄体生成素释放激素类似物作为抗肿瘤药物的治疗应用综述
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Tumor growth inhibition in patients with prostatic carcinoma treated with luteinizing hormone-releasing hormone agonists.用促黄体生成素释放激素激动剂治疗的前列腺癌患者的肿瘤生长抑制
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Triptorelin embonate (6-month formulation).醋酸曲普瑞林（6 个月剂型）。
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Treatment of tuberculosis using a combination of sustained-release rifampin-loaded microspheres and oral dosing with isoniazid.使用载有利福平的缓释微球与异烟肼口服给药联合治疗结核病。
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Use of microsphere technology for targeted delivery of rifampin to Mycobacterium tuberculosis-infected macrophages.利用微球技术将利福平靶向递送至结核分枝杆菌感染的巨噬细胞。
Antimicrob Agents Chemother. 1998 Oct;42(10):2682-9. doi: 10.1128/AAC.42.10.2682.
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Utilization of an amorphous form of a water-soluble GPIIb/IIIa antagonist for controlled release from biodegradable microspheres.利用水溶性糖蛋白IIb/IIIa拮抗剂的无定形形式从可生物降解微球中实现控释。
Pharm Res. 1997 Sep;14(9):1146-50. doi: 10.1023/a:1012190304074.
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Bombesin antagonists inhibit in vitro and in vivo growth of human gastric cancer and binding of bombesin to its receptors.蛙皮素拮抗剂可抑制人胃癌的体外和体内生长以及蛙皮素与其受体的结合。
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Sustained suppression of the pituitary-gonadal axis by leuprorelin three-month depot microspheres in rats and dogs.亮丙瑞林三个月长效微球对大鼠和犬垂体-性腺轴的持续抑制作用。
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Inhibition of prostate tumor growth in two rat models by chronic administration of D-Trp6 analogue of luteinizing hormone-releasing hormone.通过长期给予促黄体生成素释放激素的D-色氨酸6类似物抑制两种大鼠模型中的前列腺肿瘤生长。
Proc Natl Acad Sci U S A. 1981 Oct;78(10):6509-12. doi: 10.1073/pnas.78.10.6509.
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New approach in the treatment of prostate cancer: complete instead of partial withdrawal of androgens.前列腺癌治疗的新方法：完全而非部分去除雄激素。
Prostate. 1983;4(6):579-94. doi: 10.1002/pros.2990040605.
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Gonadotropin-releasing hormone agonistic analogues in the treatment of advanced prostatic carcinoma.促性腺激素释放激素激动剂类似物在晚期前列腺癌治疗中的应用
Prostate. 1983;4(6):569-77. doi: 10.1002/pros.2990040604.
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Treatment of prostatic cancer with LH-RH analogues.用促性腺激素释放激素（LH-RH）类似物治疗前列腺癌。
Prostate. 1983;4(6):553-68. doi: 10.1002/pros.2990040603.
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Treatment with gonadotrophin releasing hormone analogue in advanced prostatic cancer.促性腺激素释放激素类似物治疗晚期前列腺癌。
Br Med J (Clin Res Ed). 1983 Apr 23;286(6374):1309-12. doi: 10.1136/bmj.286.6374.1309.
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Q J Med. 1984 Winter;53(209):17-27.
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Potential use of analogs of luteinizing hormone-releasing hormones in the treatment of hormone-sensitive neoplasms.促黄体生成激素释放激素类似物在激素敏感性肿瘤治疗中的潜在应用。
Cancer Treat Rep. 1984 Jan;68(1):281-9.