• Archives of Pharmacal Research
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• v.22 no.5
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• pp.524-528
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• 1999

cis-Annonacin (1) and the mixture of (2,4)-cis-and trans-isoannonacins (2 and 3), three known mono-tetrahydrofuran annonaceous acetogenins, have been isolated form the seeds of Annona cherimolia by the use of the brine shrimp lethality test (BST) for bioactivity directed fractionation. Their structures were elucidated based on spectroscopic and chemical methods. 1 showed potent cytotoxicities in the brine shrimp lethality test (BST) and among six human solid tumor cell lines with notable selectivity for the pancreatic cell line (PaCa-2) at about 1,000 times the potency of adriamycin. The mixture of 2 and 3 is over 10,000 times cytotoxic as adriamycin in the pancreatic cell line (PaCa-2). All of the compounds are about 10 to 100 times as cytotoxic as adriamycin in the prostate cell line (PC-3).

• Archives of Pharmacal Research
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• v.24 no.4
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• pp.300-306
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• 2001

A novel and two known bioactive mono-tetrahydrofuran (THF) annonaceous acetogenins, annomocherin (1), annonacin (2) and annomontacin (3), have been isolated from the fractionated ethanolic extracts of the seeds of Annona cherimolia, guided by the brine shrimp lethality test (BST). Their structures were elucidated on the basis of spectroscopic and chemical methods. All compounds have a relative stereochemistry of threo/trans/threo for the mono-THF ring with two flanking hydroxyls. Compound 1 has a double bond at C-23/ 24 of aliphatic chain. Compound 1 was isolated from natural sources for the first time, and was named annomocherin. Two known Compounds 2 and 3 which have never been isolated from this species before, were obtained. Compound 1 exhibited potent and selective cytotoxicities against the breast carcinoma (MCF-7) and kidney carcinoma (A-498) cell lines with 100 to 1,000 times the potency of adriamycin. In brine shrimp lethality test (BST), 1-3 exhibited cytotoxicity.

• Korean Journal of Veterinary Research
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• v.63 no.3
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• pp.22.1-22.4
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• 2023

The increasing resistance of head lice Pediculus humanus capitis to many drugs has highlighted the need for new alternatives to control head lice in adults. The effect of two types of extracts (aqueous and alcoholic) of Citrullus colocynthis fruit on adult lice was tested in vitro. The results showed that the alcoholic extract with a concentration of 20% showed similar efficacy in killing adult lice to that of Natroba 9% w/w, with values ranging between 87% to 98% within 18 minutes, followed by a 20% aqueous extract with a 44% to 79% death rate. A 10% concentration of both types of extracts had moderate lethality for lice, while a 5% concentration did not show strong lethality for adult lice. These results revealed significant differences between the control group and those treated with alcoholic and aqueous extract concentrations of C. colocynthis fruits at the probability level p ≤ 0.05.

• Toxicological Research
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• v.32 no.3
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• pp.215-223
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• 2016

This study is to investigate the biological, biochemical and cytotoxic effects of puffer fish (Arothron stellatus) toxin extracts under in-vitro condition. Extracted toxins from various organs of puffer fish were purified by using active charcoal column, and Bio-gel-P2 column chromatography. The lethality of toxin was tested in crabs, which consists of neurotoxic compounds. The degree of the brine shrimp lethality assay was found directly proportional to the concentration of the toxin extracts, which was well supported by hemolytic assay. The experimental results suggested that the gonad was found higher toxins than the liver and muscles. The mortality rate of brine shrimp nauplii was increased with the raise of concentrations of toxin level. Among the different doses and time dependent cytotoxic effect of human cervical carcinoma (HeLa) cells were showed $4.0{\mu}g/mL$ of toxin, which was effectively inhibited cancer cell proliferation. HPLC and TLC analysis was revealed that the A. stellatus toxin contains tetrodotoxin (TTX), related compounds 4-epi TTX and anhydro-TTX. The present results suggested that the A. stellatus contain TTX as a major and anh-TTX as a minor toxin. It could be the potential candidate in the field of anticancer drug discovery against human cervical cancer cells. The present data is confirming that the puffer fish toxin as an interesting source of novel bioactive natural compounds with potent applications in pharmacology.

• The Korean Journal of Physiology and Pharmacology
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• v.5 no.4
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• pp.333-342
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• 2001

Adriamycin is a commonly used chemotherapeutic agent for cancer, including acute leukemia, lymphoma, and a number of solid human tumors. However, recent studies have recognized severe cardiotoxicity after an acute dose, which are likely the result of generation of free radicals and lipid peroxidation. Therefore, the clinical uses of adriamycin have been limited. Melatonin, the pineal gland hormone known for its ability to modulate circardian rhythm, has recently been studied in its several functions, including cancer growth inhibition, stimulating the immune system, and acting as an antioxidant and radical scavenging effects. In the present study, we evaluated the effect of melatonin administration on adriamycin-induced cardiotoxicity in rat. Heart slices were prepared using a Stadie-Riggs microtome for the measurement of malondialdehyde (MDA) content used as an index of lipid peroxidation and lactate dehydrogenase (LDH) release as an indicator of lethal cell injury. Serious adriamycin-induced lethality was observed in rat by a single intraperitoneal injection in a dose-dependent manner. A single injection of adriamycin (25 mg/kg, i.p.) induced a lethality rate of 86%, with melatonin (10 mg/kg s.c. for 6 days) treatment reducing the adriamycin-induced lethality rate to 20%. The severe body weight loss caused by adriamycin was also significantly attenuated by melatonin treatment. Treatment of melatonin marked reduced adriamycin-induced the levels of MDA formation and LDH release. A cell damage indicated by the loss of myofibrils, swelling of the mitochondria as well as cytoplasmic vacuolization was seen in adriamycin-treated group. Melatonin attenuated the adriamycin-induced structural alterations. These data provide evidence that melatonin prevents adriamycin-induced cardiotoxicity and might serve as a combination with adriamycin to limit free radical-mediated cardiotoxicity.

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

• Molecules and Cells
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• v.26 no.1
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• pp.81-86
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• 2008

RNA interference (RNAi) was performed on several essential genes in the pinewood nematode Bursaphelenchus xylophilus, which causes pine wilt disease. Double-stranded RNA (dsRNA) was delivered to larvae or adult worms by soaking, electroporation, or microinjection. Soaking and electroporation of L2-L3 stage worms in solutions containing dsRNA for essential genes induced over 25% lethality after 5 days, and gene-specific phenotypes were observed. This lethality agreed with significant reductions of the targeted transcripts, as assayed by reverse-transcription coupled with real time PCR. Microinjection was the most efficient route as measured by the hatching rate of F1 embryos, which was reduced by 46%. When adult worms were soaked in dsRNA, lethality was induced in the F1 larvae, revealing the persistence of knockdown phenotypes. The penetrance of the RNAi phenotypes for essential genes was relatively low but consistent, indicating that RNAi should be useful for studying the in vivo functions of B. xylophilus gene products.

• Applied Biological Chemistry
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• v.27 no.2
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• pp.55-63
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• 1984

Lethal effect on Chinese radish Kimchi was investigated by using a pilot scale Kimchi pasteurizer. A simulation model was presented so as to predict the change in viable cell concentration of the Kimchi during pasteurization. D values of microorganisms in the Kimchi were found to be 2.21, 1.62, 0.73, 0.39 and 0.21min at 60, 64, 70, 75 and $80^{\circ}C$, correspondingly, and thereby z value was $19^{\circ}C$. One cycle time required was 0.99min at flow rate of 4 l/min. The ratio of lethality in preheating section to total lethality was 0.3 and the ratio of lethality in holding, precooling and cooling sections to total lethality was 0.7. The experimental data were in good agreement with the values simulated by two model equations to which linear and exponential temperature profiles were applied at $65^{\circ}C\;and\;70^{\circ}C$ in holding section.

• Korean Journal of Environmental Biology
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• v.18 no.1
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• pp.41-45
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• 2000

Which sublethal cadmium pretreatment may prevent from lethal cadmium's killing mice and which cadmium pretreatment-induced protection against cadmium lethality to mice may be related with their hepatic glutathione contents were investigated. When cadmium chloride was subcutaneously injected to mice (ICR strain) at various doses, all mice died, which treated with cadmium at dose of 300 $\mu$moles/kg or more, and none died, which treated with cadmium at dose of 80 $\mu$moles/kg or less. Subcutaneous pretreatment of sublethal cadmium decreased sacrifice of mice which subsequently injected with lethal cadmium, with most effectiveness at pretreatment dose of cadmium of 40 $\mu$moles/kg b.w. and at 48 hours of interval between sublethal cadmium pretreatment and lethal cadmium treatment. Even if a great part of the cadmium-pretreated mice were sacrificed while treated with lethal cadmium, they survived longer than the non-pretreated mice. Sublethal cadmium pretreatment (40 $\mu$moles/kg b.w.) 48 hours before lethal cadmium treatment to mice didn't decrease hepatic glutathione contents of the survived mice, while decreases in the glutathione in livers were observed in the mice just after died. These results indicate that sublethal cadmium pretreatment-induced protection against cadmium lethality to mice may be related to their hepatic glutathione contents. [Cd pretreatment, Cd lethality, Hepatic glutathione contents].

• Journal of Korean Academy of Nursing
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• v.45 no.2
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• pp.183-191
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• 2015

Purpose: For the current article an examination was done as to whether engaging in sexual intercourse before or during adolescence has a negative impact on the suicidal behaviors of suicide ideation, suicide attempt, and suicide lethality and whether the impact varies according to the context of sexual intercourse and/or gender. Methods: Adolescents who experienced casual sex and romantic sex were compared to adolescents who retained their virginity. Data was from samples drawn from the three waves (2010~2012) of the Korea Youth Risk Behavior Web-Based Survey. Logistic models were used to adjust for a wide array of confounding variables. Results: Any type of sexual intercourse increases risk of all suicidal behaviors. Sexual intercourse in a romantic relationship exhibits enhanced risk of suicidal behaviors compared to casual sex. Adjusting for experience of sexual violence, however, decreases risk of romantic sex substantially, turning some estimates statistically insignificant. In addition, risks for suicide lethality are greater for girls than boys. Conclusion: Romantic sex put adolescents at higher risk for suicidal behaviors than casual sex owing to prevalent sexual violence in the relationships. Girls suffer more substantively adverse outcomes than boys. These results suggest that adolescents will benefit from comprehensive education on sexuality and sexual behaviors regarding how to form and maintain a romantic relationship that is characterized by personal integrity and mutual respect. It is also important to help victims of sexual violence recover from traumatic events by providing emotional support and effective counseling.