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通过无普朗尼克立方液晶递送刺松藻素:释放一种入侵性海洋藻类色素的治疗潜力

Caulerpin Delivery via Pluronic-Free Cubosomes: Unlocking the Therapeutic Potential of a Pigment from an Invasive Marine Algae.

作者信息

Krautforst Karolina, Kulbacka Julita, Fornasier Marco, Mocci Rita, Porcheddu Andrea, Pusceddu Antonio, Moccia Davide, Murgia Sergio, Bazylińska Urszula

机构信息

Department of Chemical and Geological Sciences, University of Cagliari, s.s. 554 bivio Sestu, I-09042 Monserrato, CA, Italy.

Department of Physical and Quantum Chemistry, Faculty of Chemistry, Wroclaw University of Science and Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland.

出版信息

Mol Pharm. 2025 Aug 4;22(8):4747-4761. doi: 10.1021/acs.molpharmaceut.5c00340. Epub 2025 Jul 1.

DOI:10.1021/acs.molpharmaceut.5c00340
PMID:40592545
Abstract

Pancreatic cancer remains one of the deadliest cancers due to its resistance to conventional therapies, necessitating the development of novel treatment strategies. This study investigates the anticancer potential of caulerpin, a bisindole alkaloid derived from the invasive marine alga , encapsulated in biocompatible cubosomes. Caulerpin was sustainably extracted via microwave-assisted methods and formulated into lipid-based bicontinuous cubic liquid crystalline nanoparticles using Pluronic-free surfactants (sodium taurocholate and Span 80), resulting in high encapsulation efficiency and structural stability at physiological temperature (37 °C). The formulation included cubosomes coexisting with L3 sponge nanoparticles and vesicles. studies on BxPC-3 pancreatic cancer cells demonstrated that encapsulated caulerpin significantly outperformed the free compound, inducing marked apoptotic features such as cytoskeletal disruption and cell shrinkage, as confirmed by holotomographic microscopy and F-actin bioimaging. The enhanced therapeutic efficacy is attributed to the improved protection and sustained intracellular availability of encapsulated caulerpin, which is not rapidly metabolized as in its free form. These findings suggest that caulerpin-loaded cubosomes may represent a promising nanotechnology-based strategy for pancreatic cancer treatment.

摘要

由于胰腺癌对传统疗法具有抗性,它仍然是最致命的癌症之一,因此需要开发新的治疗策略。本研究调查了封装在生物相容性立方液晶纳米粒中的柯里拉京(一种从入侵性海洋藻类中提取的双吲哚生物碱)的抗癌潜力。柯里拉京通过微波辅助方法可持续提取,并使用不含普朗尼克的表面活性剂(牛磺胆酸钠和司盘80)制成基于脂质的双连续立方液晶纳米颗粒,在生理温度(37°C)下具有高封装效率和结构稳定性。该制剂包括与L3海绵纳米颗粒和囊泡共存的立方液晶纳米粒。对BxPC-3胰腺癌细胞的研究表明,封装的柯里拉京明显优于游离化合物,诱导了明显的凋亡特征,如细胞骨架破坏和细胞收缩,这通过全层析显微镜和F-肌动蛋白生物成像得到证实。治疗效果的增强归因于封装的柯里拉京得到更好的保护和持续的细胞内可用性,它不会像游离形式那样迅速代谢。这些发现表明,负载柯里拉京的立方液晶纳米粒可能代表一种有前途的基于纳米技术的胰腺癌治疗策略。

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本文引用的文献

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Pharmacological inhibition of hypoxia induced acidosis employing a CAIX inhibitor sensitizes gemcitabine resistant PDAC cells.使用碳酸酐酶IX(CAIX)抑制剂对缺氧诱导的酸中毒进行药理学抑制可使吉西他滨耐药的胰腺导管腺癌(PDAC)细胞致敏。
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苦叶筒衍生化合物的细胞毒性和抗单纯疱疹病毒-1 作用。
Molecules. 2024 Aug 15;29(16):3859. doi: 10.3390/molecules29163859.
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Cubosomes and hexosomes stabilized by sorbitan monooleate as biocompatible nanoplatforms against skin metastatic human melanoma.山梨醇酐单油酸酯稳定的 Cubosomes 和 Hexosomes 作为生物相容性的纳米平台用于对抗皮肤转移性人黑色素瘤。
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Cubosomes functionalized with antibodies as a potential strategy for the treatment of HER2-positive breast cancer.抗体功能化 Cubosomes 作为治疗 HER2 阳性乳腺癌的潜在策略。
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