• Natural Product Sciences
• /
• v.13 no.1
• /
• pp.54-60
• /
• 2007

The plant Ichnocarpus frutescens (Linn) R.Br. (Family-Apocynaceae) has been indicated for the treatment of various diseases, one amongst it is cancer. The purpose of this study was to investigate experimentally the possible antitumor activity and antioxidant role of Ichnocarpus frutescens in the mice transplanted with Ehrlich ascites carcinoma (EAC). The chloroform and methanol extract of whole plant of Ichnocarpus frutescens (CEIF and MEIF) were administered intraperitoneally at the dose of 150 mg/kg and 300 mg/kg, body weight per day for 7 days after 24 h of tumor inoculation in mice. Treatment with CEIF at the dose of 150 mg/kg and 300 mg/kg remarkably decreased the tumor volume, packed cell volume, viable cell count and increased the nonviable cell count of EAC tumor bearing mice when compared to e effect of MEIF at 150 mg/kg and 300 mg/kg. Further the EAC mice treated with CEIF and MEIF showed significant decrease in the level of lipid peroxidation and significant increase in the level of antioxidant enzymes such as glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT), however the decreasing and increasing capacity of CEIF was less in both doses as compared to MEIF. Based on these results, it can be concluded that the chloroform and methanol extact of Ichnocarpus frutescens exhibit significant antitumor and antioxidant activity in EAC bearing mice.

• Natural Product Sciences
• /
• v.11 no.2
• /
• pp.63-66
• /
• 2005

A rare flavonol glycoside identified as $eupalitin-3-O-{\beta}-D-glucoside$ (I) was isolated from Tephrosia spinosa (Leguminosae) and its anti-inflammatory activity was evaluated against carrageenin induced paw edema. The compound exhibited significant activity when compared to the standard drug indomethacin.

• YAKHAK HOEJI
• /
• v.41 no.2
• /
• pp.233-240
• /
• 1997

The in vitro antibacterial activity of DWP20418 (1R, 5S, 6S)-6-[1-(R)-Hydroxyethyl)-l-methyl-2-[(2S,4S)-2-(piperazinylcarbonyl)-1-(R)-hydroxyethyl)pyrrolidine-4-thio]carb apen-2-em-3-carboxylic acid), a new carbapenem antibiotic, was compared with those of imipenem (IPM) and meropenem (MEPM). DWP20418 was comparable or slightly more superior to MEPM against gram-positive bacteria, and it showed more potent activity to IPM against gram-negative bacteria. DWP20418 was particularly active against MRSA, and its $MIC_{90}$ of methicillin-susceptible S. aureus, low methicillin-resistant S. aureus and high methicillin-resistant S. aureus were 0.391, 25 and 50 ${\mu}g/ml$, respectively. With a view of $MIC_{90}$, DWP20418 was comparable than the other carbapenems against P. aeruginosa and E. coli isolates. The activity of DWP20418 was not affected in the presence of $Mg^{2+},\;Ca^{2+}$ or horse serum. But inoculum size and alterations in pH of medium affected its antibacterial activity. DWP20418 showed rapidly bactericidal activity within 1h, and regrowth was not observed even incubation of 24hrs at the concentrations near the MIC.

• Asian Pacific Journal of Cancer Prevention
• /
• v.13 no.4
• /
• pp.1097-1104
• /
• 2012

Background/Aim: Pristimerin isolated from Celastrus and Maytenus spp can inhibit proteasome activity. However, whether pristimerin can modulate cancer metastasis is unknown. Methods: The impacts of pristimerin on the purified and intracellular chymotrypsin proteasomal activity, the levels of regulator of G protein signaling 4 (RGS 4) expression and breast cancer cell lamellipodia formation, and the migration and invasion were determined by enzymatic, Western blot, immunofluorescent, and transwell assays, respectively. Results: We found that pristimerin inhibited human chymotrypsin proteasomal activity in MDA-MB-231 cells in a dose-dependent manner. Pristimerin also inhibited breast cancer cell lamellipodia formation, migration, and invasion in vitro by up-regulating RGS4 expression. Thus, knockdown of RGS4 attenuated pristimerin-mediated inhibition of breast cancer cell migration and invasion. Furthermore, pristimerin inhibited growth and invasion of implanted breast tumors in mice. Conclusion: Pristmerin inhibits proteasomal activity and increases the levels of RGS4, inhibiting the migration and invasion of breast cancer cells.

• Journal of Microbiology and Biotechnology
• /
• v.26 no.5
• /
• pp.953-958
• /
• 2016

Chitosan-based film-forming gel is regarded as a promising vehicle for topical delivery of antimicrobial agents to skin wounds, since it protects from microbial infection and the cationic polymer itself possesses antibacterial activity. In this study, possible synergistic interaction against common skin pathogens between the cationic polymer and tyrothricin (TRC), a cyclic polypeptide antibiotic, was investigated, by determining the concentration to inhibit 90% of bacterial isolates (MIC). The addition of the polysaccharide to TRC dramatically reduced the MIC values of TRC by 1/33 and 1/4 against both methicillin-resistant and methicillin-susceptible Staphylococcus aureus, respectively. The synergism of TRC and chitosan combination against both strains was demonstrated by the checkerboard method, with a fractional inhibitory concentration index below 0.5. Moreover, co-treatment of TRC and chitosan exhibited antibacterial activity against Pseudomonas aeruginosa, due to the antibacterial activity of chitosan, whereas TRC itself did not inhibit the gram-negative bacterial growth. These findings suggested that the use of chitosan-based film for topical delivery of TRC could be an alternative to improve TRC antimicrobial activity against strains that are abundant in skin wounds.

• Environmental Mutagens and Carcinogens
• /
• v.26 no.2
• /
• pp.48-52
• /
• 2006

Our investigation of the seaweed extracts, Ulva lactuca. The biological activities antioxidant, antimicrobial activity, antifungal and haemolytic activity of ethy-ether and ethyl-acetate extracts from the seaweed, Ulva lactuca were investigated. They were separately extracted using ethyl-ether and ethyl-acetate from dried samples at room temperature and freeze dried. Seaweed extracts were found to cause significant free radical scavenging effects on DPPH (1,1-diphenyl-2-picrylhydrazyl). Seaweed extracts had not significant haemolytic activity against human erythrocyte. This extracts exhibited in vitro broad-spectrum antimicrobial activity of gram-negative, gram-positive bacteria and without antifungal activity.

• Archives of Pharmacal Research
• /
• v.15 no.3
• /
• pp.204-207
• /
• 1992

Glycylglycine, alanylalanine and alanylglycine were synthesized, their free carboxylic and amino groups were converted to methyl esters of N-acetylglycyglycine, N-acetylalanylglycine and N-acetylalanylalanine. The synthesized compounds were evaluated for antiepileptic activity, plasmaprotein binding, $TD_{50}$ and potentiating effect of phenobarbitone sodium.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.2
• /
• pp.535-540
• /
• 2012

A series of benzamide-based histone deacetylases (HDACs) inhibitors possessing N-(aminopyridine) residue as the zinc binding site of HDAC were synthesized and evaluated. Among these derivatives, compounds with N-(2-amino-4-pyridine) benzamide moiety have been found as the most potent ones. Moreover, introduction of appropriate substituents on the terminal aryl group acting as the surface-recognition domain could significantly improve the antiproliferative activity. In particular, the compound 4k possessed favorable pharmacokinetic characteristics and exhibited potent antitumor activity on xenograft model in mice at well tolerated doses, thus suggesting a good therapeutic index.

• Natural Product Sciences
• /
• v.8 no.3
• /
• pp.97-99
• /
• 2002

In the present study, Pisonia grandis leaves were extracted with chloroform and methanol. The extracts were vacuum dried to yield the respective chloroform (CE) and methanol extract (ME). CE and ME were evaluated for analgesic, anti-inflammatory (acute and chronic) and diuretic activity at 2 dose levels (250 and 500 mg/kg). Significant analgesic and anti-inflammatory activities were associated with CE and ME. CE at the dose level of 500 mg/kg was found to exhibit equivalent chronic anti-inflammatory activity as diclofenac at 50 mg/kg dose level. Significant diuretic activity was exhibited by ME. Graded dose response for all the activities were observed for the extracts.

• Archives of Pharmacal Research
• /
• v.28 no.5
• /
• pp.509-517
• /
• 2005

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.