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皮下注射新型蜂毒后，采用夹心 ELISA 法研究蜂毒来源的磷脂酶 A2 的药代动力学和组织分布。

Pharmacokinetics and Tissue Distribution of Bee Venom-Derived Phospholipase A2 Using a Sandwich ELISA after Subcutaneous Injection of New Composition Bee Venom in Rats.

机构信息

College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, 43 Jibong-ro, Bucheon-si 14662, Republic of Korea.

INISTst R&D Center, 19th F, Higgs U-Tower, 184, Jungbu-daero, Yongin-si 17095, Republic of Korea.

出版信息

Int J Mol Sci. 2023 Jun 16;24(12):10214. doi: 10.3390/ijms241210214.

DOI:10.3390/ijms241210214
PMID:37373367
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10299594/
Abstract

Bee venom is a traditional drug used to treat the nervous system, musculoskeletal system, and autoimmune diseases. A previous study found that bee venom and one of its components, phospholipase A2, can protect the brain by suppressing neuroinflammation and can also be used to treat Alzheimer's disease. Thus, new composition bee venom (NCBV), which has an increased phospholipase A2 content of up to 76.2%, was developed as a treatment agent for Alzheimer's disease by INISTst (Republic of Korea). The aim of this study was to characterize the pharmacokinetic profiles of phospholipase A2 contained in NCBV in rats. Single subcutaneous administration of NCBV at doses ranging from 0.2 mg/kg to 5 mg/kg was conducted, and pharmacokinetic parameters of bee venom-derived phospholipase A2 (bvPLA2) increased in a dose-dependent manner. Additionally, no accumulation was observed following multiple dosings (0.5 mg/kg/week), and other constituents of NCBV did not affect the pharmacokinetic profile of bvPLA2. After subcutaneous injection of NCBV, the tissue-to-plasma ratios of bvPLA2 for the tested nine tissues were all <1.0, indicating a limited distribution of the bvPLA2 within the tissues. The findings of this study may help understand the pharmacokinetic characteristics of bvPLA2 and provide useful information for the clinical application of NCBV.

摘要

蜂毒是一种传统药物，用于治疗神经系统、肌肉骨骼系统和自身免疫性疾病。先前的一项研究发现，蜂毒及其成分之一磷脂酶 A2 可以通过抑制神经炎症来保护大脑，并且还可用于治疗阿尔茨海默病。因此，韩国 INISTst 开发了一种新的组成蜂毒（NCBV），其磷脂酶 A2 含量高达 76.2%，作为阿尔茨海默病的治疗剂。本研究旨在表征 NCBV 中所含磷脂酶 A2 的药代动力学特征。对大鼠进行了 0.2mg/kg 至 5mg/kg 剂量的单次皮下给药，蜂毒衍生的磷脂酶 A2（bvPLA2）的药代动力学参数呈剂量依赖性增加。此外，多次给药（0.5mg/kg/周）后没有观察到蓄积，NCBV 的其他成分也不会影响 bvPLA2 的药代动力学特征。皮下注射 NCBV 后，在所测试的九种组织中，bvPLA2 的组织-血浆比均<1.0，表明 bvPLA2 在组织内的分布有限。本研究的结果可能有助于了解 bvPLA2 的药代动力学特征，并为 NCBV 的临床应用提供有用信息。

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