• Bulletin of the Korean Chemical Society
• /
• v.10 no.1
• /
• pp.1-5
• /
• 1989

The nonempirical molecular connectivity indexes of a number of mono- and disubstituted purines were calculated. Very good correlations were obtained between anticancer activity (log 1/c) and toxic activity (log 1/) of tIhese compounds and their molecular connectivity indexes and physicochemical constants. Our structure-activity relationship is discussed briefly in relation to theories of general QSAR.

• YAKHAK HOEJI
• /
• v.50 no.6
• /
• pp.367-371
• /
• 2006

Phellinus pini (Hymenocaetaceae) has been used for the immunomodulating activity hypolipidemic effect, gastric cancer non-insulin dependant diabetes, diarrhea, and menstrual irregularity. From the screening of each fraction for the inhibitory activity of NO production in lipopolysaccaride (LPS) activated RAW 264.7 cells, methanol extract of Phellinus pini and hexane soluble fraction exhibited inhibition of NO production compared with LPS control without toxicity. The hexane soluble fraction showed dose dependent inhibition of NO production. According to activity guided fractionation, the active hexane fr. was repeatedly chromatographed over silica gel, ergosta-4,6,8(14),22- tetraen-3-one was isolated. The compound inhibited NOS activation (IC$_{50}$ = 29.7 uM) and NO production of activated macrophage at 30 uM.

• Korean Journal of Environmental Agriculture
• /
• v.14 no.2
• /
• pp.163-170
• /
• 1995

This study was carried out to compare the acute toxicity(96hr) of 13 chemicals to carp (Cyprinus carpio L.) and israeli carp (Cyprinus israeli carpio L.) and the activities of acetylcholinesterase (AchE) and glutathione S-transferase (GST) in israeli carp exposed to five insecticides (diazinon, malathion, carbofuran, cartap, methomyl). $LC_{50}$ values of acute toxicity of the chemicals to israeli carp were endosulfan 0.0061ppm, captafol 0.041ppm, chlorothalonil 0.073ppm, butachlor 0.48ppm, captan 0.14ppm, carbofuran 1.13ppm, cartap 1.15ppm, diazinon 1.35ppm, nitrofen 3.72ppm, methomyl 4.39ppm, propanil 10.61ppm, malathion 11.78ppm and isoprothiolane 12.81ppm. The acute toxicity of endosulfan 0.0061ppm was 2100 times higher than that of isoprothiolane 12.81ppm. $LC_{50}$ values of acute toxicity of the chemicals to carp were endosulfan 0.0026ppm, captafol 0.062ppm, chlorothalonil 0.078ppm, captan 0.14ppm, and butachlor 0.47ppm, carbofuran 0.52ppm, nitrofen 0.58ppm, diazinon 0.81ppm, cartap 0.82ppm, methomyl 5.03ppm, propanil 10.67ppm, malathion 11.92ppm, and isoprothiolane 13.20ppm. The acute toxicity of endosulfan was 5,000 times higher than that of isoprothiolane. The toxicity of diazinon, carbofuran, cartap, endosulfan, and nitrofen to carp was approximately 2-6 times as high as that to israeli carp, but the toxicity of malathion, methomyl and captafol to israeli carp was slightly higher than that to carp. AchE activity was inhibited by 31% and 52% after 96hr’s exposure of israeli carp to diazinon and malathion respectively. GST activity in israeli carp was significantly induced by methomyl exposure for 96 hr.

• Journal of the Korean Applied Science and Technology
• /
• v.34 no.2
• /
• pp.418-425
• /
• 2017

This study investigated antioxidation activity through the content of total polyphenol, that of flavonoid and DPPH radical scavenging activity and measured the cytotoxicity against B16F10 melanoma and inhibiting function of melanin biosynthesis to evaluate antioxidation activity and melanocyte effect of pueraria lobata root extract. As the results of study, it was recognized that the toxicity did not show against B16F10 melanoma and the increase of generating melanin was inhibited as the results of measuring the inhibition function of melanin biosynthesis after inducing the generation of melanin by ${\alpha}$-MSH against B16F10 melanoma cell. The high contents of polyphenol and flavonoid was found as the contents of pueraria lobata root extract increases and DPPH radical scavenging activity as the results of antioxidation activity. Through this study, it was recognized that pueraria lobata root extract has the feasibility that can be used as the material of cosmetics as it has the excellent effect of antioxidation activity and inhibiting the generation of melanin against melanocyte, low toxicity against skin cell and its safety against melanocyte of skin was found.

• The Korean Journal of Physiology
• /
• v.23 no.1
• /
• pp.23-34
• /
• 1989

Gentamicin (GM) is a polybasic, aminoglycoside antibiotic used frequently for the treatment of serious gram-negative infections. The major limiting factors in the clinical use of GM as well as other aminoglycoside antibiotics are their nephrotoxicity and ototoxicity. The primary mechanism of cell injury in aminoglycoside toxicity appears to be the disruption of normal membrane function and the inhibition of $Na^{+}-K^{+}$ ATPase activity. There are both indirect and direct evidences which suggests that the effect of aminoglycoside antibiotics on $Na^{+}-K^{+}$ ATPase may explain, or contribute to, their toxicity. It has been shown that aminoglycoside reduce total ATPase activity (Kaku et al., 1973) and $Na^{+}-K^{+}$ ATPase activity (linuma et al., 1967) in the stria vascularis and spiral ligament of the guinea-pig cochlea. Lipsky and Lietman (1980) reported that aminoglycoside antibitoics inhibited the activity of $Na^{+}-K^{+}$ ATPase in microsomal fractions of the cortex and medulla of the guinea-pig kidney, isolated rat renal tubule and human erythrocyte ghosts. The present invstigation was undertaken to elucidate the mechanism of GM on human erythrocytes by examining its effect on $Na^{+}-K^{+}$ ATPase activity, actives sodium and potassium transport across red blood cell and $^{3}H-ouabain$ binding to red blood cell membranes. The results obtained are summarized as follows: 1) CM inhibited significantly both the activity of total ATPase and $Na^{+}-K^{+}$ ATPase at all concentrations tested. 2) GM inhibited active $^{22}Na$ efflux across red blood cell. When ouabain is present, the rate of $^{22}Na$ efflux was completely inhibited. When both GM and ouabain were added, the inhibitory effect of active $^{22}Na$ efflux was more pronounced. 3) Active $^{86}Rb$ influx was inhibited significantly by GM. In the presence of ouabain, the rate of $^{86}Rb$ influx is markedly inhibited. But $^{86}Rb$ influx is not appreciably altered by the presence of both GM and ouabain. 4) In the presence of GM, $^{3}H-ouabain$ binding to red blood cell membrane increased. From the above results, it may be concluded that the inhibition of active sodium and potassium transport across red blood cell by gentamicin appears to be due to the inhibition of $Na^{+}-K^{+}$ ATPase activity and an increase in ouabain binding to red blood cell membranes.

• Applied Biological Chemistry
• /
• v.35 no.5
• /
• pp.367-374
• /
• 1992

This study was performed to investigate effects of probable detoxifying enzyme activity and toxicity by pesticides and their combinations in the fresh water fish. Seven pesticides including IBP, isoprothiolane, cartap, ridomil, chlorothalonil, captafol and endosulfan were subjected to investigate for their acute toxicites and synergism possibilities. The $LC_{50}$ value of endosulfan was the lowest at showing 0.0079 ppm and that of metalaxyl was the highest as showing 40 ppm over. The synergism effects of relative pesticides were observed in the combinations of isoprothiolane+IBP and isoprothiolane+cartap. The changes of glycogen contents in fish liver were assayed for 5 pesticides and its highest inhibition effect of glycogen showed in IBP treated fish. The activity of probable detoxifying enzymes including carboxylesterase (CE), glutathion S-transferase (GST) and lactate dehydrogenase (LDH) were assayed in carp liver at dose of sublethal concentrations. Effects of pesticides on changes in each enzyme activities were as follows: carboxylesterase (CE) activities were the highest in IBP and gtutathion S-transferase (GST) activities were the highest in iosoprothiolane+IBP. Both activities of carboxylesterase (CE) and glutahtion S-transferase (GST) were increased by 5 chemicals. The highest LDH activity showed in isoprothiolane treated fish, while the lowest activity was observed in isoprothiolane+cartap. Sublethal exposure to cartap and isoprothiolane+cartap in carp exerted various effects on LDH activity.

• Restorative Dentistry and Endodontics
• /
• v.34 no.5
• /
• pp.415-423
• /
• 2009

The purpose of this study is to investigate the response of human pulp cell on Portland cement mixed with $\beta$-glycerophosphate. To investigate the effect of $\beta$-glycerophosphate and/or dexamethasone on human pulp cell, ALP activity on various concentration of $\beta$-glycerophosphate and dexamethasone was measured and mineral nodule of human pulp cell was stained with Alizarin red S. MTS assay and ALP activity of human pulp cell on Portland cement mixed with various concentration of $\beta$-glycerophosphate (10 mM, 100mM, 1M) was measured and the specimens were examined under SEM. Addition of $\beta$-glycerophosphate or dexamethasone alone had no effect however, the addition of 5 mM $\beta$-glycerophosphate and 100 nM dexamethasone had the largest increasement in ALP activity. There was no toxicity in all samples and the data showed that Portland cement mixed with 10 mM $\beta$-glycerophosphate had more increase in ALP activity compared with control. In conclusion, Portland cement mixed with $\beta$-glycerophosphate has no toxicity and promotes differentiation and mineralization of pulp cell compared with additive-free Portland cement. This implicated that application of Portland cement mixed with $\beta$-glycerophosphate might form more reparative dentin and in turn it would bring direct pulp capping to success.

• The Korean Journal of Pesticide Science
• /
• v.17 no.3
• /
• pp.185-192
• /
• 2013

This study was performed to evaluate the spray toxicity and leaf residual toxicity of 52 kinds of insecticides registered for strawberry against adult honeybee Apis mellifera. According to the IOBC standard, the acute toxicity by spraying showed below 30% was classified as non-toxic. Among tested insecticides, 32 insecticides (flonicamid, lufenuron, novaluron, three kinds of acetamiprid, thiacloprid, milbemectin, acequinocyl, TBI-1, two kinds of chlorfenapyr, chlorfluazuron, cyenopyrafen, cyfumetofen, etoxazole, fenpyroximate, flubendiamide, flufenoxuron, hexythiazox, metaflumizone, two kinds of methoxyfenozide, DBB-2032, pyridalyl, spiromesifen, tebufenpyrad, teflubenzuron, acetamiprid + methoxyfenozide, acrinathrin + spiromesifen, bifenazate + spiromesifen, cyenopyrafen + flufenoxuron) did not show any toxic effect, it is thought to be safe. And the others (20 insecticides) showed higher toxicity to honeybee. Insecticides which showed acute toxicity higher than 90% was selected and tested the residual toxicity. All insecticides except emamectin benzoate EC, and indoxacarb SC showed 100% mortality at one day after treatment (DAT). However, the toxicities of emamectin benzoate, indoxacarb SC, and abamectin did not show until 3, 7, 14 DAT, respectively. Nine insecticides such as indoxacarb WP, thiamethoxam WG, abamectin + chlorantraniliprole SC, acetamiprid + etofenprox WP, acetamiprid + indoxacarb WP, bifenthrin + clothianidin SC, bifenthrin + imidacloprid WP, bifenazate + pyridaben SC, chlorfenapyr + clothianidin SC showed over 90% residual toxicity until 31 Day. In pouring treatment, thiamethoxam WG showed 76.9% mortality at 28 DAT and 50.0% mortality at 31 DAT. After 35 days, thiamethoxam WG showed no effect to honeybee. Bifenthrin + clothianidin SC and tefluthrin + thiamethoxam GR showed 57.1 and 80.0% mortality at 24 DAT, respectively. In spraying treatment, thiamethoxam WG and bifenthrin+clothianidin SC showed very high residual toxicity with 100% mortality in thirty-five DAT. After spraying treatment with thiamethoxam WG, bifenthrin+clothianidin SC, bifenthrin + imidacloprid WP, thiamethoxam WG showed 100% residual toxicity until 21 DAT and there was no activity after 28 DAT. Bifenthrin+clothianidin SC and bifenthrin+imidacloprid WP showed very high residual toxicity until 49 DAT.

• Toxicological Research
• /
• v.23 no.4
• /
• pp.391-403
• /
• 2007

The study was conducted to assess the repeated dose and reproduction and developmental toxicities of acetanilide, an intermediate for drug production, as a part of OECD Screening Information Data Set (SIDS) program. The test agent was administered by gavage at dose levels of 0, 22, 67, 200 and 600 mg/kg to Sprague-Dawley rats (12/group/sex) during pre-mating and mating period for males(up to 30 days) and females and pregnancy and early lactation period for females (up to 39-50 days). At 22 mg/kg, decreases in HGB, HCT (males) and MCHC (females), hyperplasia of spleen red pulp, hyperplasia of femur bone marrow (both sexes) were observed. At 67 mg/kg, salivation (males), reduced food consumption (both sexes), decreases in RBC, HGB, HCT and MCHC (males), increases in MCV (males) and spleen weight (males), hyperplasia of spleen red pulp and femur bone marrow (both sexes) were observed. At 200 mg/kg, decreases in locomotor activity and salivation (both sexes), reduced food consumption (both sexes), decreases in RBC, HGB, HCT and increases in MCV, MCH, BUN, T-BIL (males), enlargement of spleen (both sexes), increased weight of spleen (males), hyperplasia of spleen red pulp and femur bone marrow and extramedullary hematopoiesis of liver (both sexes), atrophy of thymus and corpus luteum hyperplasia of ovary (females) were observed. At 600 mg/kg, decreases in locomotor activity, cyanosis (both sexes), reddish tear, and salivation (males), mortality (4 out of 12 females), decreased body weight (females), reduced food consumption (both sexes), decreases in RBC, HGB, HCT and MCHC and increases in WBC, MCV, MCH, reticulocyte, neutrophil, lymphocyte, monocyte, AST, ALT, BUN, T-BIL, ALB, Ca and A/G ratio (males), enlargement of spleen, increased weights of spleen (both sexes), liver (males), kidney and ovary, decreased weights of thymus (females), hyperplasia of spleen red pulp, hyperplasia of femur bone marrow and extramedullary hematopoiesis of liver (both sexes), and atrophy of thymus and corpus luteum hyperplasia of ovary (females) were observed. Regarding the reproduction and development toxicities, there were no treatment-related changes in precoital time, mating index, fertility index and pregnancy index at all doses tested. At 22 and 67 mg/kg, there were no adverse effects on all the parameters observed. At 200 mg/ kg, decreased body weight of pups (day 4 p.p.) were observed. At 600 mg/kg, decreased body weight of pups (day 0 and 4 p.p.) and viability index (day 4 p.p.), increased incidence of newborns dead or with abnormal clinical signs were observed. The results suggest that the NOAELs for general toxicity are < 22 mg/kg, LOAELs are 22 mg/kg and the NOAELs for reproductive toxicity are 67 mg/kg.

• The Journal of Internal Korean Medicine
• /
• v.31 no.2
• /
• pp.254-263
• /
• 2010

Objectives : The neuroprotective effects of bee venom (BV) have been demonstrated in many studies, but bee venom has many side effects. So we used sweet bee venom (SBV), which has high molecular elements removed to reduce the side effects. I examined the neuroprotective effect of sweet bee venom in 1-methyl-4-phenylpyridine ($MPP^+$)-induced human neuroblastoma SH-SY5Y cells. Methods : To observe the possible toxicity of SBV itself, SH-SY5Y cells were treated with SBV in various concentrations for 3 h and $MPP^+$ in concentrations (1 and 5mM) for 24h. To investigate the protective effect of SBV against $MPP^+$ toxicity, SH-SY5Y cells were pretreated with vehicle or nontoxic concentrations of SBV for 3h and the cells were not washed, followed by incubation with respective concentrations of SBV and 1 mM $MPP^+$ for 24h. To investigate the protective effect of SBV against $MPP^+$ toxicity, SH-SY5Y cells were pretreated with vehicle or nontoxic concentrations of SBV for 3h and the cells were not washed, followed by incubation with respective of SBV(0.5%), 1 mM $MPP^+$, 5uM AKT inhibitor(LY984002) and 10uM ERK inhibitor(PD98059) for 24 h. The protective effect was measured by cell viability assay. To investigate the degree of apoptosis, caspase-3 enzyme activity was measured in control, $MPP^+$, SBV+$MPP^+$. Results : SBV (0.5%) pretreatment protected the SH-SY5Y cells against $MPP^+$-induced apoptotic cell death. The cell viability was higher in the SH-SY5Y cells that were pretreated with vehicle or nontoxic concentrations of SBV than those not pretreated. The caspase-3 activity was lower in the pretreated groups than these not pretreated. ERK and AKT enzymes have a role in the neuroprotective effects of the sweet bee venom. Conclusions : The results demonstrate that SBV has a protective effect on dopaminergic neurons against $MPP^+$ toxicity. This data suggest that SBV could be a potential therapeutic tool for neurodegenerative diseases such as Parkinson's disease(PD).