• Proceedings of the PSK Conference
• /
• 2001.04a
• /
• pp.99.2-100
• /
• 2001

• Journal of the Korean Chemical Society
• /
• v.52 no.1
• /
• pp.30-35
• /
• 2008

purpose of the study was to synthesize new series of 5-cyano substituted pyrimidine analogues with different substitutions at N1 and 6 positions and to evaluate them for antibacterial and antifungal activities. The desired compounds were synthesized by tertiary condensation of ethylcyanoacetate, substituted thioureas and suitable aldehyde in presence of potassium carbonate using MORE technique. The antibacterial and antifungal activities were evaluated by cup plate method in the concentration of 25 mg. The zone of inhibition was measured in mm. All the compounds have shown significant antibacterial and antifungal activities. The maximum activity was shown by P1 and P5 against S.aureus and E.coli respectively, while P6 has shown significant activity against all types of microorganisms. The compound P8 has been found to be significantly effective against C. albicans. Norfloxacin and griseofulvin were used as standards to compare the activites of synthesized compounds. It is concluded that analogues containing p-hydroxy, p-methoxy substituted phenyl moiety at 6 position have been found to be more potent against gram-positive microorganisms, while analogues lacking these substituents on phenyl moiety possessed gram-negative activity. The compounds having p-dimethylamino substituent on phenyl moiety at 6 positions have shown moderate activity. Further, only fluorine containing analogue at N1 position was found to possess appreciable antifungal activity. This suggests that electron donating substituent on aryl moiety as well as electron withdrawing substituent at N1 plays important role in determining potency of the compounds.

• Journal of Life Science
• /
• v.17 no.1 s.81
• /
• pp.51-55
• /
• 2007

The fractions of Ulva lactuca were studied to verify the antioxidant activities. The fractions from the ethanol extract of U. lactuca were prepared by the systematic extraction procedure with the solvents such as hexane, ethyl ether, ethyl acetate, butanol and $H_2O$. Furthermore, ethyl ether, ethyl acetate and aqueous fractions of U. lactuca were purified using HPLC. The antioxidant activities of purified samples from ethyl ether, ethyl acetate, and aqueous fractions were investigated using 1,1-diphenyl-2-picryl-hydrazil (DPPH). L-ascorbic acid, a positive control showed the highest DPPH radical scavenging activity. In addition, purified sample from aqueous fraction also showed relatively high activity. Purified sample from ethyl acetate fraction showed moderate activity, but purified sample from ethyl ether fraction showed the lowest activity. Dose dependent patterns were observed on all three samples tested. The lipid peroxidation inhibition activities of these three purified samples were also investigated. Purified sample from ethyl ether fraction of U. lactuca showed the highest activity and as strong activity as that of $\alpha-tocopherol$, a positive control. These results suggest that U. lactuca may be a useful candidate for a natural antioxidant agent.

• Advances in Traditional Medicine
• /
• v.7 no.3
• /
• pp.244-253
• /
• 2007

The present study was carried out to investigate the antihyperglycemic, antihyperlipidemic and antioxidant effect of chloroform and methanol extract of whole plant of Ichnocarpus frutescens (CEIF and MEIF) in streptozotocin (STZ)-induced diabetic rats. Administration of CEIF and MEIF orally at the dose of 200 mg/kg and 400 mg/kg body weight resulted in significant (P<0.01) reduction in blood glucose levels. The body weights were significantly (P<0.001) reduced in STZ-induced diabetic rats when compared to normal rats while the extracts significantly (P<0.01) prevented the decrease in body weight in the CEIF and MEIF treated rats. The study was further undertaken to evaluate the antioxidant and antihyperlipidemic potential of CEIF and MEIF in STZ-induced diabetic rats. The increased levels of lipid peroxidation in the liver tissues of diabetic rats were significantly reverted back to normal levels and a significant increase in activity of antioxidant enzymes such as superoxide dismutase, catalase and the level of reduced glutathione in the liver of diabetic rats after the treatment with CEIF and MEIF was noticed. These results clearly indicate that CEIF and MEIF exhibit significant antihyperglycemic, antihyperlipidemic and in vivo antioxidant activity in STZ-induced diabetic rats and the results were found to be in a dose dependent manner.

• Parasites, Hosts and Diseases
• /
• v.61 no.3
• /
• pp.282-291
• /
• 2023

Despite the recent progress in public health measures, malaria remains a troublesome disease that needs to be eradicated. It is essential to develop new antimalarial medications that are reliable and secure. This report evaluated the pharmacokinetics and antimalarial activity of 1,2,6,7-tetraoxaspiro[7.11]nonadecane (N-89) using the rodent malaria parasite Plasmodium berghei in vivo. After a single oral dose (75 mg /kg) of N-89, its pharmacokinetic parameters were measured, and t_1/2 was 0.97 h, T_max was 0.75 h, and bioavailability was 7.01%. A plasma concentration of 8.1 ng/ml of N-89 was maintained for 8 h but could not be detected at 10 h. The dose inhibiting 50% of parasite growth (ED₅₀) and ED₉₀ values of oral N-89 obtained following a 4-day suppressive test were 20 and 40 mg/kg, respectively. Based on the plasma concentration of N-89, we evaluated the antimalarial activity and cure effects of oral N-89 at a dose of 75 mg/kg 3 times daily for 3 consecutive days in mice harboring more than 0.5% parasitemia. In all the N-89-treated groups, the parasites were eliminated on day 5 post-treatment, and all mice recovered without a parasite recurrence for 30 days. Additionally, administering oral N-89 at a low dose of 50 mg/kg was sufficient to cure mice from day 6 without parasite recurrence. This work was the first to investigate the pharmacokinetic characteristics and antimalarial activity of N-89 as an oral drug. In the future, the following steps should be focused on developing N-89 for malaria treatments; its administration schedule and metabolic pathways should be investigated.

• Natural Product Sciences
• /
• v.9 no.2
• /
• pp.91-92
• /
• 2003

The present investigation was carried out to evaluate the antinociceptive and sedative - hypnotic effect of a vacuum dried methanol extract of aerial parts of Artemisia pallens. In the tail-flick method with Swiss albino mice the methanol extract at the doses of (1500 mg/kg, 2000 mg/kg, and 2500 mg/kg) showed significant antinociceptive activity. Significant potentiation of Pentobarbitone sodium - induced sleeping time was observed in mice on co-administration of the various doses of the methanol extract of Artemisia pallens.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.23 no.1
• /
• pp.15-26
• /
• 2009

The purpose of this report was to provide the information about activity and safety of Yukmijihwang-tang by analyzing domestic/international papers and theses about Yukmijihwang-tang. Domestic/international papers and theses related to Yukmijihwang-tang were reviewed and analyzed. These papers were then classified by year, experimental method, and activity subject. The following results were obtained in this study. The study of Yukmijihwang-tang started from 1978 and was rapidly increased after 1990s. The study of Yukmijihwang-tang was continuously increased now and was mainly forcused on experimental model rather than clinical study. The paper of SCI journal or non-SCI journal was 27 volume and the other domestic paper was 64 volume. The total papers of Yukmijihwang-tang, 91 volume was analysed in this study. Allatoin, gallic acid, loganin, morroniside, paeoniflorin, paenol, urosolic acid were determined in Yukmijihwang-tang by using HPLC and HPLC-MS-MS. In classified Yukmijihwang-tang paper by experimental method and animal, more than a half study was in vivo experiment used rat. Furthermore clinical experiments were performed variously. As these studies were classified by subject, papers related to renal function were most abundant by 16 papers. Besides there were several papers related to cognitive vitality, anti-diabetic effect, immuno-regulation, reproductive activity, anti-oxidant effect, liver function, anti-cancer and blood pressure depress. According to basic research and clinic research data, it is supported that Yukmijihwang-tang was useful prescription in renal function, cognitive vitality, anti-diabetic effect and reproductive activity. Many study of basic and clinic research were performed and reported variously on Yukmijihwang-tang in domestic/international journal. According to basic research and clinic research data, it is supported that Yukmijihwang-tang was useful prescription in renal function, cognitive vitality, anti-diabetic effect and reproductive activity. However, studies on efficacy and mechanism of Yukmijihwang-tang should be conducted at the molecular biology level and studies on safety of Yukmijihwang-tang need to be completed at the clinical level.

• Advances in Traditional Medicine
• /
• v.5 no.1
• /
• pp.21-28
• /
• 2005

The leaf extracts of Araucaria bidwillii Hook. (Araucariaceae) were evaluated for their cytotoxic effect in various human cancer cell lines. Preliminary investigation by brine shrimp lethality assay indicated that $LC_{50}$ value of various successive extracts were found to be less than $1000\;{\mu}g/ml$, where the ethyl acetate extract showed maximum activity of less than $100\;{\mu}g/ml$. Further cytotoxic evaluation of various leaf extracts of Araucaria bidwilli Hook was carried out in four different human cancer cell lines-acute myeloblastic leukemia (HL-60), chronic myelogenic leukemia (K-562), breast adenocarcinoma (MCF-7) and cervical epithelial carcinoma (HeLa). Cytotoxicity was assessed by trypan blue dye exclusion method and 3-(4,5-dimethyl thiazole-2yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction assay. From the present investigation it was found that the ethyl acetate and methanol extract of Araucaria bidwilli Hook was found to be more effective in leukemic cell lines and was less effective in MCF-7 and HeLa. The $IC_{50}$ value of the ethyl acetate extract in leukemic cell lines was found to be $28.18\;and\;34.64\;{\mu}g/ml$ and methanol extract was found to be $33.11\;&\;39.81\;{\mu}g/ml$. It can be concluded that various extract from the leaves of Araucaria bidwillii Hook. posses cytotoxic activity tested in brine shrimps and various human carcinoma cell lines.

• BMB Reports
• /
• v.48 no.7
• /
• pp.419-425
• /
• 2015

Ginseng has been widely used for therapeutic and preventive purposes for thousands of years. However, orally administered ginseng has very low bioavailability and absorption in the intestine. Therefore, fermented ginseng was developed to enhance the beneficial effects of ginseng in the intestine. In this study, we investigated the molecular mechanisms underlying the anti-inflammatory activity of fermented wild ginseng (FWG). We found that FWG significantly alleviated the severity of colitis in a dextran sodium sulfate (DSS)-induced colitis mouse model, and decreased expression level of pro-inflammatory cytokines in colonic tissue. Moreover, we observed that FWG suppressed the infiltration of macrophages in DSS-induced colitis. FWG also attenuated the transcriptional activity of nuclear factor-κB (NF-κB) by reducing the translocation of NF-κB into the nucleus. Our data indicate that FWG contains anti-inflammatory activity via NF-κB inactivation and could be useful for treating colitis. [BMB Reports 2015; 48(7): 419-425]

• Archives of Pharmacal Research
• /
• v.14 no.1
• /
• pp.48-51
• /
• 1991

Amides from amino acid ester and nalidixic acid were synthesized. The solubility characteristics and partition coefficient of the compounds were studied. The hydrolysis of the compounds was studied in the simulated gastric fluid and simulated intestinal fluid. Some compounds showed better antibacterial activity than nalidixic acid.