Xinjiang Key Laboratory of Biological Resources and Genetic Engineering, College of Life Science and Technology, Xinjiang University, Urumqi 830017, China.
Molecules. 2022 Jul 7;27(14):4364. doi: 10.3390/molecules27144364.
Cecropins (CECs) are insect venom-derived amphiphilic peptides with numerous pharmacological effects, including anti-inflammatory, antibacterial, antiviral, and anti-tumor activities. Cecropins induce tumor cell death by disrupting phospholipid membrane integrity. However, non-specific cytotoxicity and in vivo rapid degradation limit clinical application. Nanotechnologies provide novel strategies for tumor eradication, including nanocarriers that can precisely target drugs to tumor tissue. We report the fabrication of CEC-encapsulated zeolitic imidazolate framework 8 (ZIF-8) nanoparticles (CEC@ZIF-8 NPs) via the preparation of CEC@ZIF-8 NPs in pure water by one-pot stirring. This method yielded morphologically uniform NPs with 20 wt% drug loading capacity and 9% loading efficiency. The NP formulation protected CECs from proteasome degradation, enhanced peptide bioavailability, promoted HeLa tumor cell uptake, and increased antitumor efficacy compared to free CECs. In conclusion, this ZIF-8 encapsulation strategy may enhance the clinical applicability of CECs and other antitumor peptides.
蜂毒素（CECs）是一种具有多种药理作用的昆虫毒液衍生的两亲性肽，包括抗炎、抗菌、抗病毒和抗肿瘤活性。CECs 通过破坏磷脂膜完整性诱导肿瘤细胞死亡。然而，非特异性细胞毒性和体内快速降解限制了其临床应用。纳米技术为肿瘤消除提供了新的策略，包括可以将药物精确靶向肿瘤组织的纳米载体。我们通过一锅搅拌法在纯水中制备 CEC@ZIF-8 NPs，报告了 CEC 包封的沸石咪唑酯骨架 8（ZIF-8）纳米颗粒（CEC@ZIF-8 NPs）的制备。该方法得到了形态均匀的 NPs，载药量为 20wt%，载药效率为 9%。与游离 CEC 相比，该纳米颗粒制剂保护 CEC 免受蛋白酶体降解，提高了肽的生物利用度，促进了 HeLa 肿瘤细胞摄取，并提高了抗肿瘤功效。总之，这种 ZIF-8 包封策略可能会增强 CEC 及其它抗肿瘤肽的临床适用性。
