• Biomolecules & Therapeutics
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• 제5권3호
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• pp.316-322
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• 1997

CJ-50001 is a recombinant granulocyte-colony stimulating factor (rG-CSF) synthesized by recombi-nant DNA technology using E. coli as an expression system. The general pharmacological properties of CJ-50001 were evaluated in mice, rats, dogs and isolated guinea pig ileum. The doses are 100, 300 and 1, 0007g/kg, i.v. for mice and rats, 1, 10 and 100$\mu$g/kg, 1.v. for dogs and 1 and 10$\mu$g/ml for isolated guinea pig ileum. Intravenous administration of CJ-50001 at this dose range did not affect general behavior, central nervous system, smooth muscles, gastrointestinal system, cardiovascular and respiratory system and water and electro-lytes excretion. In summary, CJ-50001 had no harmful pharmacological erect in these studies even up to the 200-fold expected clinical dose, 2507g/man.

• Biomolecules & Therapeutics
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• 제5권3호
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• pp.299-305
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• 1997

In order to investigate the pharmacological properties of ι-muscone, effects of ι-muscone and musk were studied on the cardiovascular system with various experimental models. In isolated rat aorta, ι-muscone and musk made the relaxation of blood vessels in maximum contractile response to phenylephrine (10$^{-6}$ M) in endothelium-containing rings of the rat aorta, but not in endothelium-denuded rings. However, ι-muscone and musk in the presence of the inhibitor of NO synthase and guanylate cyclase did not make the relaxation of blood vessels. In spontaneously hypertensive rats (SHRs), ι-muscone and musk slightly reduced blood pressure but significantly decreased heart rate. In the isolated perfused rat hearts, ι-muscone and musk did not affect significantly on LVDP, contractile force, coronary flow and (-dp/dt)/(+dp/dt). These results suggest that ι-muscone and musk have weak cardiovascular effects with relaxation of blood vessel and decrease of heart rate, but without significant cardiac functions.

• Biomolecules & Therapeutics
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• 제8권1호
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• pp.99-106
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• 2000

Aspalatone [3-(2-methyl-4proponyl)]-2-acetyloxybenzoate, CAS 147249-33-0) is a compound having an antithrombotic action. General pharmacological properties of aspalatone were studied. Aspalatone had no effect on central nervous system and no anticonvulsant effect up to 1200 mg/kg p.o. However, the compound has hypothermic and analgesic effect. When administered intravenously in rabbits, aspalatone did not affect blood pressure, heat rate and respiration rate and depth, and it did not inhibit transient hypotensive effect of acetylcholine. The compound did not affect isolated guinea-pig ileum and tracheal strip at a concentration of 1${\times}$$10^{-4}$, and did not inhibit histamine-induced contraction of guinea-pig ileum. It also did not affect isolated rat stomach fundus and estrogenated rat uterus at 1${\times}$$10^{-4}$, and did not inhibit contraction produced by acetylcholine or oxytocin. The pupil size and intestinal propulsion were not influenced at a large dose of was shown. The compound showed a slight increase in urine volume and led to decreased excretion of potassium in urine of rats. The results suggest that aspalatone may have no considerable adverse effects in general pharmacological aspect.

• Advances in Traditional Medicine
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• 제6권3호
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• pp.208-214
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• 2006

In this study the Ayurvedic formulation Dasamularista was studied for its preliminary pharmacological properties using laboratory mice. Dasamularista showed a decrease in food intake and stool formation, while the water content of stool and water intake was higher and the volume of the urine was less. Dasamularista in a slight extent reduced the intestinal motility. This constipating effect was further supported by the significant anti-diarrhoeal property of the formulation in castor oil induced dairrhoea. The tested formulation markedly increased the latent period of diarrhoea and reduced the purging index value. Dasamularista did not alter the acetic acid induced abdominal writhing. Significant reduction on the onset of sleeping time and increased duration of sleep was observed in pentobarbital induced sleeping time test.

• Bulletin of the Korean Chemical Society
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• 제30권7호
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• pp.1445-1451
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• 2009

New benzotriazoles (5-8) or dibenzodiazepine derivatives (11-18) were synthesized starting from 3-[(2-amino- 4,5-disubstitutedphenyl)amino]-5,5-disubstitutedcyclohex-2-enones (1-4) through internal coupling of their diazonium salts or internal Mannich reaction in the presence of aromatic aldehydes. Pharmacological evaluation of benzotriazole and dibenzodiazepine derivatives for their clozapine-like properties revealed that dibenzodiazepine 11 bearing 4-bromophenyl group exhibited the same antipsychotic activity as the reference drug clozapine while the activity of benzotriazole 7 was 25% lesser than that of clozapine. Moreover, compounds 7 and 11 did not show significant CNS depressant activity as well as no or slight neurotoxicity on contrast to clozapine when tested in mice using forced swim, rotarod and horizontal screen tests.

• Biomolecules & Therapeutics
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• 제7권1호
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• pp.97-104
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• 1999

A new antibiotic bead, CJ-40003 is a combination of three antibiotics, tobramycin, vancomycin and cefazolin embedded in bone cement, for the treatment of osteomyelitis. To evaluate the general pharmacological properties of CJ-40003, the effects of its active ingredients were investigated in mice, rats, dogs and isolated guinea pig ileum. The combination of three antibiotics (CA) did not affect general behavior, central nervous system, smooth muscles, gastrointestinal system, cardiovascular and respiratory system and water and electrolytes excretion when administered intravenously at the doses of 0.3, 1 and 3 mg/kg, respectively, into experimental animals. The CA had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 1, 3 and 10 $\mu\textrm{g}$/ml, respectively. In conclusion, the active ingredients of CJ-40003 showed no pharmacological effect in these studies.

• Natural Product Sciences
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• 제25권2호
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• pp.92-102
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• 2019

Centella asiatica (Linn.) Urban (Umbelliferae) which is also known as 'pegaga' is highly consumed and eaten raw as 'ulam' in Malaysia. C. asiatica is used in traditional medicines to treat various health conditions such as rheumatism, inflammation, syphilis, skin diseases and diarrhoea. Various reports exhibited that the crude extracts and isolated bioactive compounds of C. asiatica possessed a broad range of pharmacological activities such as anti-oxidant, anti-diabetic, anti-tumor, wound healing, anti-microbial, anti-inflammatory, immunomodulatory, hepatoprotective and memory enhancing properties. The pharmacological validation on anti-microbial and immunomodulatory of C. asiatica is very limited and several existence review papers related for this plant had not been focused for both activities. This review therefore attempts to combine the existing literature to offer immense scope for researchers engaged in validation of the traditional claims and bioactivities of this plant related with anti-microbial and immunomodulatory potential.

• Asian Pacific Journal of Cancer Prevention
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• 제15권5호
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• pp.2287-2290
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• 2014

Background: In the past few years, a considerable number of preclinical studies have been proposed metformin as a potential anticancer agent, but some of these studies suffer from a number of methodological limitations such as assessment of cytotoxicity in the presence of supraphysiological glucose concentrations or applying suprapharmacological levels of the drug. These objections have limited the translation of published preclinical data to the clinical setting. The present study aimed to investigate direct anticancer effects of metformin on different molecular subtypes of breast cancer with pharmacological concentrations and under normoglycemic conditions in vitro. Materials and Methods: Breast cancer cell lines from luminal A, luminal B, ErbB2 and triple-negative molecular subtypes were treated with a pharmacological concentration of metformin (2mM) at a glucose concentration of 5.5mM. Time-dependant cell viability was assessed by dye exclusion assay. MTTbased cytotoxicity assays were also performed with metformin alone or in combination with paclitaxel. Results: Metformin did not show any growth inhibitory effects or time-dependant cytotoxicity on breast cancer cell lines in the presence of normal glucose concentrations at the therapeutic plasma level. No augmentation of the antineoplastic properties of paclitaxel was apparent under the tested conditions. Conclusions: Metformin is probably unable to exert cytotoxic or cytostatic effects on breast cancer subtypes at pharmacological concentrations and normal plasma glucose levels. These results highlight the importance of establishing a higher steady-state plasma concentration of metformin in the clinical setting for assessment of anticancer effects in normoglycemic patients.

• Journal of Pharmaceutical Investigation
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• 제30권3호
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• pp.159-166
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• 2000

Kunitz-type soybean trypsin inhibitor (SBTI) and chondroitin sulfate (A, and C type) were conjugated using sodium periodate method. And the physicochemical, pharmacokinetic properties and immunogenecity of the conjugates (Chon-A-SBTI or Chon-C-SBTI) were characterized. We expected the conjugation using chondroitin sulfate to reduce the immunogenecity and to improve the pharmacological effect. As the results, the mean molecular weight of the conjugate highly increased. After I.V. injection of the radiolabeled conjugates or native SBTI into mice, it was found that native SBTI showed rapid elimination from plasma, whereas Chon-A-SBTI and Chon-C-SBTI were slowly eliminated. Organ distribution of the two agents at 30 min after I.V. injection was different : Chon-A-SBTI or Chon-C-SBTI accumulated to a large extent in the liver (13% in Chon-A-SBTI and 16% in Chon-C-SBTI), whereas native SBTI was taken up more rapidly by the kidney (107% dose/g of tissue) and excreated into the urine (26%). In addition we evaluated the therapeutic value of the conjugates by using the sublethal septic shock model caused by pseudomonal elastase and tested the immunogenecity by passive cutaneous anaphylaxis shock (PCA). The conjugates were more effective than native SBTI against pseudomonal elastase induced septic shock in guinea pig. In case of the conjugates, the pharmacological and therapeutic effect lasted over 3 hours long. In immunogenecity test, both of the conjugates showed the reduction of their immunogenecity, especially Chon-A-SBTI looked most effective.

• 약학회지
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• 제41권6호
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• pp.817-828
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• 1997

In order to investigate pharmacological properties of New Woohwangchungsimwon Pill (NWCH) and Woohwangchungsimwon Pill(WCH), effects of NWCH and WCH on cerebral ischemia and central nervous system were compared. Cerebral ischemia insult was performed using unilateral carotid artery occlusion in Mongolian gerbils. The histological observations showed preventive effect of NWCH and WCH treatments with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by NWCH and WCH treatment. In contrast to what was seen with ATP, the lactate and lipid peroxide were both elevated in vehicle-treated ischemic gerbils. This elevation was inhibited by NWCH and WCH treatments. In central nervous system, NWCH and WCH had sedative effect in rotarod and spontaneous activity test, but no effects on the hexobarbital-induced sleeping time. And, NWCH and WCH had weak anticonvulsion effects in electric shock- and pentetrazol-induced convulsion test. NWCH and WCH increased the respiration rate, but decreased the respiration depth in rats. Furthermore, NWCH and WCH showed antistress effect. Our findings suggest that the pharmacological profiles of NWCH on cerebral ischemia and central nervous system are similar to that of WCH.