• Proceedings of the Korean Society of Applied Pharmacology
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• 2001.11a
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• pp.21-22
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• 2001

Phospholipase A$_2$(PLA$_2$) comprise a family of enzymes that hydrolyze the acyl bond at the sn-2 position of phospholipids to generate free fatty acids including arachidonic acid and lysophospholipids. Distinct forms of PLA$_2$are involved in digestion, inflammation, and intercelluar-and intracellular signaling pathways. The released arachidonic acid, which is enriched at the sn-2 position, serves as the precursor for eicosanoids such as prostaglandins and leukotrienes. During oxygenation of arachidonic acid to hydroxy endoperoxide, reactive oxygen radicals are generated. On the other hand, lysophospholipids increase membrane fluidity and can be cytotoxic with its detergent-like action. Thus, the biochemical features of the products of PLA$_2$activity suggest that PLA$_2$may be implicated in many destructive cellular processes.

• Archives of Pharmacal Research
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• v.29 no.12
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• pp.1067-1073
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• 2006

Cisplatin, a platinum coordinated complex, is a widely used antineoplastic agent for the treatment of metastatic tumors of the testis, metastatic ovarian tumors, lung cancer, advanced bladder cancer and many other solid tumors. The cytotoxic action of the drug is often thought to be associated with its ability to bind DNA to form cisplatin-DNA adducts. The development of resistance to cisplatin during treatment is common and constitutes a major obstacle to the cure of sensitive tumors. Although to understand the clinically relevant mechanisms of resistance, many studies have been aimed at clarifying the biochemical/molecular alterations of cisplatin-resistance cells, these studies did not conclusively identify the basis of cellular resistance to cisplatin. In this review, cisplatin resistance was discussed in terms of the relevant transporters, such as copper transporters (CTRs), organic cation transporters (OCTs) and multi-drug resistance related transporters (MDRs). These transporters seem to be contributed to cisplatin resistance through the reduction of drug accumulation in the cell. Better understanding the mechanism of cisplatin resistance associated with transporters will provide the useful informations for overcoming the cisplatin resistance.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.7
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• pp.3275-3279
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• 2012

Recently, population-based studies of type 2 diabetes patients have provided evidence that metformin treatment is associated with a reduced cancer incidence and mortality, but its mode of action remains unclear. Here we report effects of metformin on hepatocellular carcinoma (HCC) Hep-G2 cells and details of molecular mechanisms of metformin activity. Our research indicates that metformin displays anticancer activity against HCC through inhibition of the mTOR translational pathway in an AMPK-independent manner, leading to G1 arrest in the cell-cycle and subsequent cell apoptosis through the mitochondrion-dependent pathway. Furthermore, we showed that metformin strongly attenuated colony formation and dramatically inhibited Hep-G2 tumor growth in vivo. In conclusion, our studies suggested that metformin might have potential as a cytotoxic drug in the prevention and treatment of HCC.

• Journal of Microbiology and Biotechnology
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• v.28 no.7
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• pp.1086-1093
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• 2018

Honokiol, a bioactive compound isolated from the cone and bark of Magnolia officinalis, has been shown to have various activities including inhibition of the growth of Candida albicans. We investigated the roles of the Hsp90-calcineurin pathway in the antifungal activity of honokiol. The pharmacologic tool was employed to evaluate the effects of Hsp90 and calcineurin in the antifungal activity of honokiol. We also evaluated the protective effects of the calcineurin inhibitor cyclosporin A (CsA) on honokiol-induced mitochondrial dysfunction by the fluorescence staining method. The Hsp90 inhibitor potentiated the antifungal activity of honokiol. A C. albicans strain with the calcineurin gene deleted displayed enhanced sensitivity to honokiol. However, co-treatment with calcineurin inhibitor CsA attenuated the cytotoxic activity of honokiol due to the protective effect on mitochondria. Our results provide insight into the action mechanism of honokiol.

• Korean Journal of Pharmacognosy
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• v.28 no.1
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• pp.54-58
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• 1997

The cytotoxic activities of methanolic extract and its fractions of Ailanthi Cortex Radicis and column chromatographic eluates of its dichloromethane fraction (DCM fr.) were investigated. DCM fr. Showed the strongest cytotoxicity against hepatoma cells. Furthermore, the active equates 1-3, 8 and 9 were obtained. Effects on free radical generation and the growth of vascular endothelial cells were tested to elucidate the action mechanism of anticancer activity. Eluates 1-3 stimulated free radical generation, while eluates 8 and 9 showed no changes. Especially, eluates 8 and 9 efffectively inhibited the proliferation of vascular endothelial cells in a dose- dependant manner. It is speculated that the anticancer effects of eluates 1-3, 8 and 9 might be due to free radical generation and inhibition of endothelial cell growth, respectively.

• Natural Product Sciences
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• v.23 no.4
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• pp.281-285
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• 2017

The purpose of this study was to confirm the anti-tumor activity of an ethanol extract of Saussurea laniceps against pancreatic tumor and to isolate the active compound from S. laniceps extract. Treatment with S. laniceps extract and hispidulin inhibited proliferation of pancreatic cell lines, such as Capan-1, Capan-2, Panc-1 and S2-013 in a dose-dependent manner using the hollow fiber assay. Hispidulin showed typical hallmarks of apoptotic cell death a significant anti-tumor activity on Capan-2 cells at a dose of 100 mg/kg and 200 mg/kg. S. laniceps has potential cytotoxic and apoptotic effects on human pancreatic carcinoma cells. Its mechanism of action might be associated with the apoptotic cell death through DNA fragmentation.

• Korean Journal of Plant Resources
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• v.20 no.3
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• pp.221-225
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• 2007

The plant Ligularia fischeri var. spiciformis (Compositae) is a candidate for available functional foods. It has been used to treat diabetes mellitus and rheumatoid arthritis. We have reported the isolation of a new eremophilanolide named 6-oxoeremophilenolide and cytotoxic intermedeol together with the isolation of hydrophilic constituents, chlorogenic acid, 3,4-di-O-caffeoylquinic acie (3), and 5-O-[1-butyl]-3,4-di-O-caffeoylquinic acid. Compound 3 was again isolated by combination of silica gel- and ODS column chromatography for the anti-nociceptive action. Compound 3 and 4 were assayed in hot plate- and writhing tests in the rat. Although the three derivatives of caffeic acid exhibited significant anti-nociceptive effects at 10 mg/kg dose (i.p.),(activity potency: 4>3). These results suggest that compound 3 is responsible for at least rheumatoid arthritis, and caffeic acid moiety is the active moiety of dicaffeoylquinic acid.

• CELLMED
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• v.9 no.4
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• pp.3.1-3.6
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• 2019

Melissa parviflora Benth. is an aromatic perennial herb of Lamiaceae family. It is one of the most influencial plant and used from centuries in Unani system of medicine for the treatment of various malady such as Epilepsy (mirgi), hemiplegia (falij), migraine (shaqeeqa), insomnia (sehar), indigestion (sue hazm) and palpitation (khafqaan) etc. The Persian physician Avicenna endorsed it for heart problems. It has antitubercular, antipyretic, analgesic and stomachic properties, also used to remove bad breath from mouth, strengthen the gums but its main action is as a tranquillizer and nervine relaxant, it is greatly esteemed for its calming properties. Preliminary performed phytochemical analysis revealed that tannin, flavonoid and saponins are the major components of the plant extract. The plants containing saponins or flavonoids exhibit anticonvulsant activity whereas the flavonoids show various biological activities including antioxidant, anti-inflammatory and cytotoxic-antitumor etc. Keeping in view the tremendous medicinal importance of the plant Badranjboya in Unani Medicine, this review provides updated information on its phytochemistry, therapeutic uses and pharmacological properties.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.247.2-247.2
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• 2002

A synthetic naphthoquinone alkaloid. 2-amino-3-ethoxycarbonyl-l-methyl pyrolo (3,2-b) naphtho-4,9-dione (compound 1), showed a potent cytotoxicity in a panel of cancer cell lines with an IC50 ranged from 0.1 to 0.3 microgram/mL. Prompted by a potent cytotoxic activity, the mechanism action study was performed with cultured A549 of human lung cancer cells. Flow cytometric G2-M cell cycle arrest and microscopic investigation was also characterized with apoptotic morphological features. (omitted)

• Journal of Sasang Constitutional Medicine
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• v.13 no.3
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• pp.102-113
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• 2001

The purpose of this research was to investigate the effects of Seungyangikkitang (SIT) on the immune cells in BALB/c mice. SIT (500mg/kg) was administerd p.o. once a day for 7 days. SIT enhanced the proliferation of thymocytes, but decreased the proliferation of splenocytes. SIT enhanced the subpopulation of cytotoxic T cells in thymocytes and helper T cells in splenocytes, but did not affect the subpopulation of B220/Thy1 cells. SIT enhanced the production of γ-interferon and interleukin-2 in thymocytes, splenocytes and serum, but did not affect the production of interleukin-4. SIT suppressed the production of nitric oxide, but enhanced the lucigenin chemiluminescence and the engulfment of FITC-conjugated E. coli particles in peritoneal macrophages. These results suggest that SIT has a potent activity on the specific immunity via the cytokine secretion of Th1 cells and the non-specific immunity via the phagocytic activity of macrophages in vivo.