• Archives of Pharmacal Research
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• v.22 no.2
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• pp.137-142
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• 1999

Anti-ulcer activity of newly synthesized acylquinoline derivatives was investigated. For the in vitro screening, the effects of compounds on gastric $H^{+}/K^{+}$ ATPase isolated from hog and rabbit were examined. Among them, AU-090, AU-091, AU-254, AU-413 and AU-466 exhibited good in vitro activity on both enzymes. To correlate the in vitro activity with in vivo action, the effects of the compounds on the basal gastric acid secretion were studied. Some derivatives showed considerable anti-secretory activities, and AU-413 was selected for further studies. AU-413 protected gastric damage induced by either ethanol or NaOH dose dependently when given orally. $ED_{50}$ values of 12 mg/kg, p.o. (ethanol) and 41 mg/kg, p.o. (NaOH) were obtained. In addition, histamine-stimulated gastric secretion was reduced upon AU-413 administration. Taken together, newly synthesized acylquinoline derivatives, especially AU-413, is worthy of further investigation to be developed as an anti-ulcer agent.

• Natural Product Sciences
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• v.14 no.3
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• pp.192-195
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• 2008

Three known compounds, puerarol (1), pueroside B (2), and ononin (3), were isolated from an EtOAc-soluble fraction of the roots of Pueraria lobata. The isolates (1 - 3) were subjected to an in vitro bioassay to evaluate their inhibitory activity on the formation of advanced glycation end products (AGEs). Puerarol (1) exhibited a remarkable inhibitory activity on AGEs formation with $IC_{50}$ value of $2.05{\pm}0.32{\mu}M$ as compared with positive control, aminoguanidine ($IC_{50}$ value : $905.32{\pm}7.58{\mu}M$).

• Journal of Pharmaceutical Investigation
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• v.3 no.1_2
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• pp.16-22
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• 1973

Biological determination of Pivampicillin hydrochloride was examined and an available method has been established. Unhydrolyzed Pivampicillin hydrochloride has no antibacterial activity, but it exhibits an antibacterial activity hydrolyzed with liberation of ampicillin by nonspecific enzymes present in blood and tissues from various species in vitro and in vivo. Using these properties, Pivampicillin hydrochloride can be determined as ampicillin by use of an agar-diffusion method with Bacillus subtilis as the assay organism.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.248.3-249
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• 2002

Nitric oxide (NO) has been shown to play an important role in the regulation of vascular tone. platelet function. neurotransmission. and immune function. NO is synthesized from the L-arginine by NO synthase (NOS). Three distinct isoforms of NOS have been identified: calcium/calmodulin-dependent endothelial (eNOS) and neuronal (nNOS) isoforms which are constitutive and produce small quantities of NO, and an inducible isoform (iNOS) which is markedly induced in response to lipopolysaccharide (LPS) or inflammatory cytokines. (omitted)

• Archives of Pharmacal Research
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• v.17 no.5
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• pp.304-308
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• 1994

Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the phamacological properties of KR-25018 were compared with those of morphine, capsaicin, and nonsteroidal antiinflammatory drugs (NSAIDs). The analgesic activities were evaluated in several animal models, using different stimuli, such as phenylbenzoquinone(PBQ)-induced weithing test, tail-filck test in mice and adjuvant arthritic flexion test in rat. The relationship of phamacological properties of KR-25018 to that of centrally acting opioids was assessed by the blocking test using naloxone. The analgesic potency of the KR-25018 $(MPED_{50}=0.89{\;}p.o.{\;}in{\;}PBQ-induced{\;}weithing{\;}test, {\;}MPED_{50}$=0.61$ s.c. in tail-flick test in mice0, with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.

• Natural Product Sciences
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• v.3 no.1
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• pp.38-41
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• 1997

The hypoglycemic effect of the extract of Ficus racemosa leaves was studied on streptozotocin-induced diabetic rats. Petroleum ether $(60-80^{\circ}C)$ extract of the plant obtained by soxhlet extraction from coarsely pulverised leaves was used. In the $LD_{50}$ determination of the extract no abnormalities were observed at the dose range of 3 g/kg (p.o.) of the extract. The extract (200 mg/kg and 400 mg/kg orally) caused a reduction of blood glucose levels in streptozotocin-induced diabetic rats by 28.9% (P<0.00l) and 34.6% (P<0.001) respectively at the end of 9 days. The results. of this study indicate that the petroleum ether $(60-80^{\circ}C)$ extract of the leaves possesses significant hypoglycemic activity in hyperglycemic animals compared with glybenclamide as standard drug.

• Advances in Traditional Medicine
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• v.8 no.1
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• pp.39-46
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• 2008

In the Indian traditional medicine, Lippia nodiflora (Verbenaceae) whole plant is claimed to possess powerful diuretic activity. However, the diuretic potential of this plant is not yet investigated. The aim of this study was to evaluate the diuretic potential of methanol extract of Lippia nodiflora (MELN) in rats. Control (0.9% saline solution, 25 ml/kg, b.w) or urea (1 g/kg b.w) or frusemide (5 mg/kg b.w) and different concentrations of MELN (200 and 400 mg/kg b.w) were intraperitoneally administered (n = 6 per each treatment group) to hydrated rats and their urine output was monitored over a period of 5 h and 24 h after drug administration. The diuretic responses with its electrolyte excretion potency of the extract were highly remarkable in comparison with control animals. The extract at doses of 200 and 400 mg/kg shows a significant increase in volume of urine with increase in $Na^{+}$, $Ca^{2+}$ and $Cl^{-}$ excretion accompanied by the excretion of $K^{+}$ in dose dependent manner. This study suggests that the active component(s) in MELN had similar diuretic effect to that of frusemide. These results validate the traditional use of Lippia nodiflora as a diuretic agent.

• Biomolecules & Therapeutics
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• v.30 no.5
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• pp.435-446
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• 2022

The present study evaluated the anti-cancer activity of histone deacetylase (HDAC)-inhibiting CKD-581 in multiple myeloma (MM) and its pharmacological mechanisms. CKD-581 potently inhibited a broad spectrum of HDAC isozymes. It concentration-dependently inhibited proliferation of hematologic cancer cells including MM (MM.1S and RPMI8226) and T cell lymphoma (HH and MJ). It increased the expression of the dishevelled binding antagonist of β-catenin 3 (DACT3) in T cell lymphoma and MM cells, and decreased the expression of c-Myc and β-catenin in MM cells. Additionally, it enhanced phosphorylated p53, p21, cleaved caspase-3 and the subG1 population, and reversely, downregulated cyclin D1, CDK4 and the anti-apoptotic BCL-2 family. Finally, administration of CKD-581 exerted a significant anti-cancer activity in MM.1S-implanted xenografts. Overall, CKD-581 shows anticancer activity via inhibition of the Wnt/β-catenin signaling pathway in hematologic malignancies. This finding is evidence of the therapeutic potential and rationale of CKD-581 for treatment of MM.

• Bulletin of the Korean Chemical Society
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• v.32 no.7
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• pp.2260-2266
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• 2011

4-Chlorotetrazolo[1,5-a]quinoxaline (III) was synthesized by azide (2+3) cycloaddition of 2,3-dichloroquinoxaline (II). Compound (III) on further refluxing with hydrazine hydrate furnished 4-hydrazinotetrazolo[1,5-a]quinoxaline (IV). Further refluxing of (IV) with different aromatic aldehydes in methanol yielded corresponding Schiff's bases V(a-j). Various 4-aminotetrazolo[1,5-a]quinoxaline based azetidinones VII(a-j) were synthesized by stirring the compounds V(a-j), at low temperature, with equimolar mixture of chloroacetylchloride & triethylamine in dry benzene, while 4-aminotetrazolo[1,5-a]quinoxaline based thiazolidinones VIII(a-j) were synthesized by refluxing Schiff's bases V(a-j) with thioglycolic acid in oil-bath. The structures of all the compounds were confirmed on the basis of $^1H$-NMR & FT-IR spectral data. All the newly synthesized compounds were screened for in-vitro antimicrobial activity against E. coli, S. aureus, K. pneumoniae & P. aeruginosa & antifungal activity against C. albicans. Few of them have exhibited the promising activity.

• YAKHAK HOEJI
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• v.38 no.3
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• pp.265-273
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• 1994

ln vitro and in vivo antibacterial activities of DWQ-013(1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid), a new fluoroquinolone antibacterial agent, were compared with those of ciprofloxacin, sparfloxacin and ofloxacin against aerobic and anaerobic standard strains and clinical isolates. DWQ-013 had a broad spectrum and potent antibacterial activity against Gram-positive and Gram-negative bacteria. The antibacterial activity of DWQ-013 against Staphylococcus aureus was equal to that of sparfloxacin(SPFX) and superior to those of ciprofloxacin(CPFX). The antibacterial activity against Gram-negative bacteria was slightly lower than those of ciprofloxacin and sparfloxacin. MIC of DWQ-013 against Pseudomonas aeruginosa$(0.781{\sim}1.563\;{\mu}g/ml)$ was usually equal to that of sparfloxacin$(0.781\;{\mu}g/ml)$ and was inferior to that of ciprofloxacin$(0.098\;{\mu}g/ml)$. The number of viable cells was decreased rapidly after addition of DWQ-013 at concentration of $1{\sim}2$ folds of MIC.