Characterization, Release Pattern, and Cytotoxicity of Liposomes Loaded With α-Mangostin Isolated From Pericarp of Mangosteen (Garcinia mangostana L.)

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.

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Glutamic Acid Uptake Inhibition Assay in Cultured Hep G2 Cells as an Alternative Method for Evaluating Potential In Vivo Eye Irritation

Alternatives to Laboratory Animals ◽

10.1177/026119298901600405 ◽

1989 ◽

Vol 16 (4) ◽

pp. 344-352

Author(s):

Paul J. Dierickx

Keyword(s):

Glutamic Acid ◽

Corneal Opacity ◽

Acid Uptake ◽

Hep G2 ◽

Hep G2 Cells ◽

Eye Irritation ◽

Uptake Inhibition ◽

Range Finding ◽

G2 Cells

Glutamic acid (GA) content was measured in cultured Hep G2 cells, after treatment of the cells with test compounds. The results with 37 chemicals were compared with their respective rabbit eye irritation data, of which 17 were determined according to the OECD test, and the other 20 in range-finding studies. The chemicals were mainly organic solvents (alcohols, esters, amines, acids and others). The xenobiotics were applied to the cells for 4 hours at 5 different concentrations. The cells were then incubated for 15 minutes with tritiated GA. GA uptake inhibition was measured by liquid scintillation counting, and the results were expressed as the GI50 value, which is the concentration of test compound required to induce a 50% reduction in GA uptake. A linear correlation coefficient r = 0.66 was found between the log GI50 and the mean corneal opacity scores. This value is comparable to that obtained in total protein and uridine uptake inhibition studies. However, r = 0.81 was found when the log GI50 was compared with range-finding scores, indicating that a closer relationship exists between cytotoxicity and the latter.

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Human proapolipoprotein A-II is cleaved following secretion from Hep G2 cells by a thiol protease.

Journal of Biological Chemistry ◽

10.1016/s0021-9258(17)42584-1 ◽

1984 ◽

Vol 259 (24) ◽

pp. 15556-15563 ◽

Cited By ~ 9

Author(s):

J I Gordon ◽

H F Sims ◽

C Edelstein ◽

A M Scanu ◽

A W Strauss

Keyword(s):

Hep G2 ◽

Hep G2 Cells ◽

Thiol Protease ◽

G2 Cells

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The Hep G2 Cell Line as a Possible Alternative to Isolated Hepatocytes in Cytotoxicity Studies

Alternatives to Laboratory Animals ◽

10.1177/026119298801600105 ◽

1988 ◽

Vol 16 (1) ◽

pp. 16-22

Author(s):

Marina Marinovich ◽

Jose L. Lorenzo ◽

Liliana M. Flaminio ◽

Agnese Granata ◽

Corrado L. Galli

Keyword(s):

Cell Line ◽

Rat Hepatocytes ◽

Prostaglandin E ◽

Human Hepatoma ◽

Hep G2 ◽

Hep G2 Cells ◽

Isolated Rat Hepatocytes ◽

G2 Cells ◽

Isolated Rat

The hepatotoxicity of carbon tetrachloride (CC14) was evaluated in vitro in freshly isolated rat hepatocytes and in the human hepatoma cell line, Hep G2. Toxicity was assessed by the leakage of cytosolic enzymes (lactate dehydrogenase and aspartate aminotransferase) and cell viability (trypan blue exclusion). The established human cells were less sensitive to CCl4-induced injury; higher doses of the toxic agent and longer incubation times were necessary to elicit cell damage. Micromolar concentrations of prostaglandin E2 significantly decreased enzyme leakage in both Hep G2 cells and rat hepatocytes challenged with CC14; a stable derivative of prostacyclin (ZK 36374) was ineffective. These results suggest that human hepatoma Hep G2 cells may represent a valid alternative to isolated rat hepatocytes for an initial approach to the in vitro evaluation of cell toxicity.

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