• Archives of Pharmacal Research
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• v.7 no.2
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• pp.127-132
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• 1984

Systematic pharmacological astudies on pipeline have revealed that this compound elicited diverse pharmacological activities; CNS depressant activity characterized by antagonism against electo shock seizure and by muscle relaxant activity in mice; antipyretic activity in tyyhoid vaccinated rabbits; analgesic activity as evaluated by tail-clip pressure and writhing syndrome in mice; antiinflammatory activity in carrageenin-induced edema in rats.

• Biomolecules & Therapeutics
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• v.27 no.1
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• pp.101-106
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• 2019

Most diabetic patients experience diabetic mellitus (DM) urinary bladder dysfunction. A number of studies evaluate bladder smooth muscle contraction in DM. In this study, we evaluated the change of bladder smooth muscle contraction between normal rats and DM rats. Furthermore, we used pharmacological inhibitors to determine the differences in the signaling pathways between normal and DM rats. Rats in the DM group received an intraperitoneal injection of 65 mg/kg streptozotocin and measured blood glucose level after 14 days to confirm DM. Bladder smooth muscle contraction was induced using acetylcholine (ACh, $10^{-4}M$). The materials such as, atropine (a muscarinic receptor antagonist), U73122 (a phospholipase C inhibitor), DPCPX (an adenosine $A_1$ receptor antagonist), udenafil (a PDE5 inhibitor), prazosin (an ${\alpha}_1$-receptor antagonist), papaverine (a smooth muscle relaxant), verapamil (a calcium channel blocker), and chelerythrine (a protein kinase C inhibitor) were pre-treated in bladder smooth muscle. We found that the DM rats had lower bladder smooth muscle contractility than normal rats. When prazosin, udenafil, verapamil, and U73122 were pre-treated, there were significant differences between normal and DM rats. Taken together, it was concluded that the change of intracellular $Ca^{2+}$ release mediated by PLC/IP3 and PDE5 activity were responsible for decreased bladder smooth muscle contractility in DM rats.

• Archives of Pharmacal Research
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• v.14 no.1
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• pp.87-92
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• 1991

In order to evaluate the pharmacological activities of Chinese medicine, nine Umbelliferae plants were selected and their restoring activity against dexamethasone-induced disorders, liver protective activity, antimicrobial activity, anti-inflammatory activity and antimutagenic activity were tested and compared. Angelica dahurica. Angelica acutiloba and Ostericum koreanum showed various activities in these tests at the dose used in this study.

• Journal of Applied Biological Chemistry
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• v.44 no.2
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• pp.77-83
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• 2001

For defining the possibilities of the commercial mass liquid culture of Cordyceps sinensis, the pharmacological activities of mycelia were analyzed. The mycelium of C. sinensis consists of carbohydrate (5.1%) and fat (1.3%), and contains a low content of protein (0.7%) and ash (0.5%), and 92.4% moisture. The molecular sugar ratio of carbohydrate was composed mainly of glucose, mannose (1.0 : 0.9), in addition a small amount of galactose and arabinose (0.2 : 0.1). The cellular materials of mycelia were fractionated into ethylacetate (EA), MeOH (M) and hot-water extract fraction (HW). HW fraction showed the most potent intestinal immune system modulating activity, anti-coagulant activity, and anti-complementary activity, and M fraction had the inhibition activity of radical generation as effective as genistine. These results reveal that the mycelium of liquid cultured C. sinensis showed pharmacological activities and could be used for commercial purpose.

• YAKHAK HOEJI
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• v.27 no.4
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• pp.263-270
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• 1983

Effective BuOH fraction was extracted from Puerariae radix (Pueraria thunbergiana), and several pharmacological activities were examined. From several pharmacological examinations, it was found that BuOH fraction has an antipyretic activity against typhoid vaccine pyrexia in rabbit, a papaverine-like antispasmodic activity on isolated ileum and jejunum of rat, an analgesic effects on mice treated by 0.7% HAc, and an anti-inflammatory activity of carrageenin edema in rat. It was found that BuOH fraction has detoxication effects on acute and subacute toxic rat induced by alcohol in consequence of biochemical tests of serum. Therefore it was considered that BuOH fraction has preventive and therapeutic effects in alcohol intoxication.

• Advances in Traditional Medicine
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• v.8 no.1
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• pp.93-96
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• 2008

The ethanolic extract of Ficus racemosa Lin. (Moraceae) bark and fruit were tested for its possible antinociceptive activity study on acetic acid induced writhing method in mice. Both the bark and fruit extracts at a dose of 500 mg/kg body weight showed significant antinociceptive activity on the experimental animals. The fruit extract showed most potent inhibition of acetic acid induced writhing in mice (61.38%, P < 0.001) where as the bark extract showed inhibition only 42.6% (P < 0.001) and all the result were statistically significant.

• YAKHAK HOEJI
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• v.53 no.6
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• pp.303-313
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• 2009

Traditionally, Cham dang-gui (Angelica gigas Nakai) is one of the most popular herbal medicines in Asian countries including Korea. A. gigas has been used as a functional food product for treatment anemia, women's health care, a sedative, an anodyne or a tonic agent. Decursin and decursinol angelate isolated from the roots of A. gigas are pyranocoumarin compounds. Recently, as the global herbal medication market is increasing, investigations about pharmacological effects of decursin and decursinol angelate are rapidly increasing. We summarized previous studies about pharmacological effects of decursin and decursinol angelate, and reviewed relation with pharmacological effects of decursin and decursinol angelate on human disorder, focused on the approach for new drug development. Pharmacological effects of decursin and decursinol angelate were classified as anti-tumor activity, anti-bacterial activity, improvements of the circulating system, inhibition of cytochrome P-450 activity, anti-inflammation activity, anti-oxidant activity and cognitive-enhancing activites. The activity of A. gigas with improvement of the circulating system may have wide therapeutic potential for circulatory diseases, including diabetes, hyperlipidemia and atherosclerosis. Also, anti-inflammation activity A. gigas may be beneficial for the treatment and prevention of asthma, atopic dermatitis and rheumatism arthritis. This relation could potentially lead to the development of herbal new drugs. In order to development a new drug containing decursin and decursinol angelate, it is also necessary to consider the safety profile, and the information in this review would contribute to development a new drug from herbal medicine.

• Biomolecules & Therapeutics
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• v.28 no.2
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• pp.202-210
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• 2020

Fluoxetine is used widely as an antidepressant for the treatment of cancer-related depression, but has been reported to also have anti-cancer activity. In this study, we investigated the cytotoxicity of fluoxetine to human gastric adenocarcinoma cells; as shown by the MTT assay, fluoxetine induced cell death. Subsequently, cells were treated with 10 or 20 µM fluoxetine for 24 h and analyzed. Apoptosis was confirmed by the increased number of early apoptotic cells, shown by Annexin V- propidium iodide staining. Nuclear condensation was visualized by DAPI staining. A significant increase in the expression of cleaved PARP was observed by western blotting. The pan-caspase inhibitor Z-VAD-FMK was used to detect the extent of caspase-dependent cell death. The induction of autophagy was determined by the formation of acidic vesicular organelles (AVOs), which was visualized by acridine orange staining, and the increased expression of autophagy markers, such as LC3B, Beclin 1, and p62/SQSTM 1, observed by western blotting. The expression of upstream proteins, such as p-Akt and p-mTOR, were decreased. Autophagic degradation was evaluated by using bafilomycin, an inhibitor of late-stage autophagy. Bafilomycin did not significantly enhance LC3B expression induced by fluoxetine, which suggested autophagic degradation was impaired. In addition, the co-administration of the autophagy inhibitor 3-methyladenine and fluoxetine significantly increased fluoxetine-induced apoptosis, with decreased p-Akt and markedly increased death receptor 4 and 5 expression. Our results suggested that fluoxetine simultaneously induced both protective autophagy and apoptosis and that the inhibition of autophagy enhanced fluoxetine-induced apoptosis through increased death receptor expression.

• Journal of Pharmacopuncture
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• v.20 no.3
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• pp.194-200
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• 2017

Moringa oleifera Lam. or munga is one of the most important plant widely cultivated in India. It belongs to family Moringaceae. This plant is widely used as nutritional herb and contains valuable pharmacological action like anti-asthmatic, anti-diabetic, hepatoprotective, anti-inflammatory, anti-fertility, anti-cancer, anti-microbial, anti-oxidant, cardiovascular, anti-ulcer, CNS activity, anti-allergic, wound healing, analgesic, and antipyretic activity, Moringa oleifera Lam. The plant is also known as Horse - radish tree, Drumstick tree. Every part of this plant contains a valuable medicinal feature. It contain rich source of the vitamin A, vitamin C and milk protein. Different types of active phytoconstituents like alkaloids, protein, quinine, saponins, flavonoids, tannin, steroids, glycosides, fixed oil and fats are present. This plant is also found in the tropical regions. Some other constituents are niazinin A, niazinin B and niazimicin A, niaziminin B. The present review discusses the phytochemical composition, medicinal uses & pharmacological activity of this plant.

• YAKHAK HOEJI
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• v.58 no.4
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• pp.255-261
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• 2014

Poly-pharmacy has been on the rise because of aging of population and chronic disease. Most of drug metabolism happens in the liver by CYP isozymes and the metabolism by CYP450 enzymes. The Cytochrome P450 (CYP) is a superfamily of enzymes that catalyzes the oxidations of many endogenous and exogenous compounds. Primary human Hepatocytes (HH) are considered as the gold standard model for In vitro drug interaction studies. However, there are several limitations (cost, limited life span) for using HH cells. HepaRG cells are being used as a possible alternative. HepaRG cells were cultured in William E medium containing the positive control inducers (1A2: 10, 25, 50 ${\mu}M$ omeprazole, 2C9 and 2C19: 10 ${\mu}M$ rifampin, 3A4: 10, 25, 50 ${\mu}M$ rifampin) at $37^{\circ}C$, 5 % $CO_2$ in a humidified atmosphere. This study was to evaluate the induction of CYP isozymes (1A2, 2C9, 2C19 and 3A4) using LC-MS/MS. We evaluated the potential induction ability of Bosentan, as a drug of pulmonary artery hypertension, in HepaRG cells. For reference, dose of the Bosentan is determined to the basis of the $C_{max}$ (835 mg/ml) value. The enzyme activity demonstrated that CYP2C9 and 3A4 were induced up to 20 times by Bosentan. Like as In vivo, the enzyme activity of CYP2C9 and CYP3A4 is significantly induced in a dose-dependent by Bosentan.