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Characterization, Release Pattern, and Cytotoxicity of Liposomes Loaded With α-Mangostin Isolated From Pericarp of Mangosteen (Garcinia mangostana L.)
Natural Product Communications ( IF 1.8 ) Pub Date : 2020-11-24 , DOI: 10.1177/1934578x20974559
Thi Kieu Trang Phan 1 , Toan Quoc Tran 2, 3 , Dung Thuy Nguyen Pham 4, 5 , Duong Thanh Nguyen 3, 6
Affiliation  

The pericarp of Garcinia mangostana L. is a rich source of α-mangostin, which exhibits a wide range of pharmacological and biological activities. However, clinical use of this compound is limited due to its low water solubility. Therefore, its formulation with various delivery systems has been developed. In the present study, α-mangostin was isolated from G. mangostana pericarp extract and loaded onto newly synthesized liposomes. The system was evaluated for in vitro drug release at pH 5.5 and 7.4 during 96 hours of experiment, followed by cytotoxicity measurement against Hep-G2 cells. α-Mangostin was obtained in a high yield (1.86%) and its chemical structure was confirmed using nuclear magnetic resonance and Fourier-transform infrared spectroscopy. The compound was then loaded onto liposomes with relatively high efficiency (55.3% ± 2.3%). The compound was released in a sustained manner and exhibited significant cytotoxic activity against Hep-G2 cells. The present study provides important insights into liposome applications for α-mangostin delivery, thus improving the compound’s limitations and enabling further in vivo studies on its safety and efficacy.



中文翻译:

表征,释放模式,和脂质体的细胞毒性装有隔离山竹果皮α倒捻子素(倒捻子L.)

芒果的果皮是α-芒果的丰富来源,具有广泛的药理和生物学活性。然而,由于该化合物的低水溶性,其临床用途受到限制。因此,已经开发了其具有各种递送系统的制剂。在本研究中,α倒捻子素从分离G.柿的果皮提取物,并加载到新合成的脂质体。对系统进行了体外评估在96小时的实验过程中,在pH 5.5和7.4下释放药物,然后测量对Hep-G2细胞的细胞毒性。α-Mangostin以高收率(1.86%)获得,并通过核磁共振和傅里叶变换红外光谱法确认了其化学结构。然后将化合物以相对较高的效率(55.3%±2.3%)加载到脂质体上。该化合物以持续的方式释放并显示出对Hep-G2细胞的明显细胞毒活性。本研究为脂质体在α-芒果素的递送中的应用提供了重要的见识,从而改善了该化合物的局限性,并使其在体内的安全性和功效得以进一步研究。

更新日期:2020-11-25
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