• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.821-828
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• 2011

Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied.

• Genomics & Informatics
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• 제6권4호
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• pp.227-230
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• 2008

Compounds of polyketide origin possess a wealth of pharmacological effects, including antibacterial, antifungal, antiparasitic, anticancer and immunosuppressive activities. Many of these compounds and their semisynthetic derivatives are used today in the clinic. Most of the gene clusters encoding commercially important drugs have also been cloned and sequenced and their biosynthetic mechanisms studied in great detail. The area of biosynthetic engineering of the enzymes involved in polyketide biosynthesis has recently advanced and been transferred into the industrial arena. In this work, we introduce a computational system to provide the user with a wealth of information that can be utilized for biosynthetic engineering of enzymes involved in post-PKS tailoring steps. Post-PKS tailoring steps are necessary to add functional groups essential for the biological activity and are therefore important in polyketide biosynthesis.

• 약학회지
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• 제29권1호
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• pp.1-10
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• 1985

The ether fraction obtained from dry fruit of Cornus officinalis was investigated for the anti-inflammatory action, acute toxicity and central nervous system activities. From several pharmacological examinations, it was found that the ether fraction suppressed considerably carrageenin edema at the dose of 600mg/kg p.o. in rats, inhibited the granuloma formation in rats as given 100mg/kg p.o. for 7 days and decreased the swelling of both of complete adjuvant injected and noninjected (contralateral) paws of the rats at the dose of 100mg/kg p.o. given for 14 days. The $LD_{50}$ of the fraction are estimated to be more than 2,000mg/kg p. o. and 642mg/kg i. p. in mice. And the fraction did not show any sedative, stimulative, analgesic and anticonvulsant action but exhibited hypothermic action. These results might be concluded that the ether fraction of Corni fructus showed anti-inflammatory action in both of acute and chronic type models without any considerable central nervous depressant activity and exhibited very weak acute toxicity in mice.

• 셀메드
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• 제5권4호
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• pp.24.1-24.7
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• 2015

Bahunia racemosa family, Caesalpiniaceae, is one of the precious resources of the earth. It has played a significant role in human civilization since ancient times. It is tall sized tree growing throughout India, Ceylon, China, and Timor. The different part of this plant contains β-sitosterol and β-amyrin, flavonols (kaempferol and quercetin) and two coumarins (scopoletin and scopolin), tannins etc. Various part of this plant has great pharmacological potential with a great utility and usage as folklore medicine as analgesic, antipyretic, anti-inflammatory, antispasmodic and antimicrobial activity. This review mainly focus on the exclusive review work on the traditional, phytochemical and pharmacological activities of this plant.

• Advances in Traditional Medicine
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• 제3권2호
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• pp.63-71
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• 2003

The psycho-pharmacological effect of BRHAT VATACHINTAMANI RASA (BVC) an Ayurvedic preparation was investigated, both in animal and clinical models. It was observed that BVC possess a sedative or quitening effect in that it significantly decreased the spontaneous motor activity, and also lowered the exploratory behavior of the amphetamine treated animals. This was further evident by increase in climbing out time and taming effect on animal in isolation induced aggression test. Apart from very high dose it seems have little effect on pentobarbital sleeping time and narcotic analgesic test. The drug BVC increases performance of the animal in forced locomotor test. The effect of VATACHINTAMANI RASA on clinical study was not significant.

• Journal of Ginseng Research
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• 제33권3호
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• pp.165-176
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• 2009

Korean ginseng, which contains ginsenosides and polysaccharides as its main constituents, is orally administered to humans. Ginsenosides and polysaccharides are not easily absorbed by the body through the intestines due to their hydrophilicity. Therefore, these constituents which include ginsenosides Rb1, Rb2, and Rc, inevitably come into contact with intestinal microflora in the alimentary tract and can be metabolized by intestinal microflora. Since most of the metabolites such as compound K and protopanaxatriol are nonpolar compared to the parental components, these metabolites are easily absorbed from the gastrointestinal tract. The absorbed metabolites may express pharmacological actions, such as antitumor, antidiabetic, anti-inflammatory, anti-allergic, and neuroprotective effects. However, the activities that metabolize these constituents to bioactive compounds differ significantly between individuals because all individuals possess characteristic indigenous strains of intestinal bacteria. Recently, ginseng has been fermented with enzymes or microbes to develop ginsengs that contain these metabolites. However, before using these enzymes and probiotics, their safety and biotransforming activity should be assessed. Intestinal microflora play an important role in the pharmacological action of orally administered ginseng.

• 생약학회지
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• 제7권2호
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• pp.99-109
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• 1976

Scolopendra corpus has been used as anticonvulsants and antispasmodics in the oriental medicine. It was previously shown that water extract of Scolopendra corpus had an inhibitory action on ileum in mouse. To investigate the anticonvulsant and antispasmodic activity of Scolopendra corpus, pharmacological studies have been carried out with the water extract of Scolopendra subspinipes mutilans $L.\;K_{OCH}$, which is widely distributed in Korea. 1. The extract depressed convulsions induced by picrotoxin and strychnine. 2. Sedative and antipyretic analgesic action were observed. 3. In mouse and rabbit, tone of intestinal smooth muscle was suppressed with the treatment of the extract and intestinal contraction induced by $BaCl_2$ was also inhibited, suggesting that the extract has a papaverine-like effect. Whereas, in guinea pig, intestinal and tracheal smooth muscle were stimulated, and the effect was antagonized by pre-and after-treatment of diphenhydramine, suggesting that the extract has a histamine-like effect. 4.Flow rate was increased when hind-limb of Toad was perfused with saline containing the extract, but returned to normal within 10 min. Hypotensive effect was observed in rabbit and the effect was abolished by vagotomy.

• Natural Product Sciences
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• 제9권3호
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• pp.143-153
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• 2003

Though a great deal of secondary metabolites and their bioactivities were discovered from the plants of the genus Hovenia, the structure-activity relationship was not well defined. To facilitate further pharmacological research and development in this area, we have summarized the progress of phytochemical and pharmacological research on the plants of the genus Hovenia.

• Archives of Pharmacal Research
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• 제27권12호
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• pp.1194-1201
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• 2004

Michael addition of certain nucleophiles on ${\alpha}$ , ${\beta}$-unsaturated ketones 1 led to the formation of adducts 2-7 as well as the reaction of arylidene derivatives with secondary amines afforded the amino compounds 9 and 11. Also, dialkylmalonates were treated with ${\alpha}$-cyano cinnamide to afford 13. On the other hand, double Michael cycloaddition of ethylcyanoacetate or tetrachlorophthalic anhydride to the suitable divinylketone were synthesized to produce 15-17. Selected compounds (13 and 6) were screened for muscle relaxant, anticonvulsant, and sedative activities using established pharmacological models. Their activities were compared with that of phenobarbital sodium taken as standard. Compound 6 was the most potent muscle relaxant while compounds 13a and 13c offered the highest anticonvulsant activity. Meanwhile compound 13c showed the highest potentiation of phenobarbital induced sleep in mice.

• Archives of Pharmacal Research
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• 제21권1호
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• pp.30-34
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• 1998

The ethanol extracts of Opuntia ficus-indica fructus (EEOF) and Opuntia ficus-indica stem (EEOS) were prepared and used to evaluate the pharmacological effects of cactus. Both the extracts inhibited the writhing syndrome induced by acetic acid, indicating that they contains analgesic effect. The oral administrations of EEOF and EEOS suppressed carrageenan-induced rat paw edema and also showed potent inhibition in the leukocyte migration of CMC-pouch model in rats. Moreover, the extracts suppressed the release of $\beta$-glucuronidase, a lysosomal enzyme in rat neutrophils. It was also noted that the extracts showed the protective effect on gastric mucosal layers. From the results it is suggested that the cactus extracts contain anti-inflammatory action having protective effect against gastric lesions.