• The Korean Journal of Pharmacology
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• v.11 no.2
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• pp.55-59
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• 1975

Safety study of the continuous releasing dichlorvos-resin insecticide $(Mopari^{\circledR})$ was conducted in human volunteers and domestic fowls. For the purpose, the potential hazards in using the insecticide were observed in terms of the inhibition of plasma cholinesterase activity and the changes in the liver function (GOT, GPT, Alkaline phosphatase, Bilirubin, Thymol turbidity), the blood picture (RBC, WBC with differential count, Hemoglobin, Hematocrit and ESR) and the urine picture (sugar, albumin, pH and microscopic findings) in 40 healthy adult volunteers and 60 leghorn domestic fowls. In case of the human study the observation was continued for 2 months during the application of the insectiside ($1{\sim}3$ solid formulations/$30m^3$) in the living rooms of ordinary Korean dwelling houses or in the office. In the animal test, however, 1 to 5 solid formulations of the insecticide were applied in the fowl cage of $9.2m^3$ for 5 weeks. Any significant inhibition of the plasma cholinesterase activity was not observed in both the human volunteer and the fowl throughout the experimental period. And the liver function as well as the blood and urine pictures were also not changed after exposure to the vaporizing insecticide. It is considered from the result that the amount of dichlorvos released into the air by the continuous vaporizing dichlorvos-resin insecticide presents no significant hazardous effect on humans or animals in the present experimental condition.

• Asian-Australasian Journal of Animal Sciences
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• v.17 no.10
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• pp.1374-1377
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• 2004

The present study was conducted to explore the possibilities of estrus induction and superovulation in a native Indian breed of goats called 'Black Bengal'. Forty-two adult non-pregnant females were divided in two groups, of which 18 goats were subjected to a superovulatory treatment comprising of equine chorionic gonadotropin (eCG), Prostaglandin (PGF2$\alpha$) and human chorionic gonadotropin (hCG) to induce superovulation. The remaining 24 goats received no treatment and served as controls for the parameter under study as well as recipients for embryo transfer studies. The average duration of estrus was found to be significantly increased in treated goats (34.2${\pm}$3.4 h) compared to controls 3.0${\pm}$2.4 h). The average duration between PGF administration and occurrence of estrus was 2.0${\pm}$5.2 h. After mid ventral laparotomy, superovulatory responses indicated a significant increase in the number of follicles, which was 8.27${\pm}$0.37 in the treatment group compared to 4.16${\pm}$0.17 in the control group. The number of corpora lutea was also significantly increased in treated animals compared to control (2.90${\pm}$0.86 vs. 0.74${\pm}$0.04) respectively per ovary per goat.

• Molecules and Cells
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• v.38 no.4
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• pp.336-342
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• 2015

Propyl gallate (PG) used as an additive in various foods has antioxidant and anti-inflammatory effects. Although the functional roles of PG in various cell types are well characterized, it is unknown whether PG has effect on stem cell differentiation. In this study, we demonstrated that PG could inhibit adipogenic differentiation in human adipose tissue-derived mesenchymal stem cells (hAMSCs) by decreasing the accumulation of intracellular lipid droplets. In addition, PG significantly reduced the expression of adipocyte-specific markers including peroxisome proliferator-activated receptor-${\gamma}$ (PPAR-${\gamma}$), CCAAT enhancer binding protein-${\alpha}$ (C/EBP-${\alpha}$), lipoprotein lipase (LPL), and adipocyte fatty acid-binding protein 2 (aP2). PG inhibited adipogenesis in hAMSCs through extracellular regulated kinase (ERK) pathway. Decreased adipogenesis following PG treatment was recovered in response to ERK blocking. Taken together, these results suggest a novel effect of PG on adipocyte differentiation in hAMSCs, supporting a negative role of ERK1/2 pathway in adipogenic differentiation.

• Bulletin of the Korean Chemical Society
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• v.26 no.11
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• pp.1695-1700
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• 2005

Catechol-O-methyltransferase (COMT, EC 2.1.1.6) is an S-adenosylmethionine (SAM, AdoMet) dependent methyltransferase, and is related to the functions of the neurotransmitters in various mental processes, such as Parkinson’s disease. COMT inhibitors represent a new class of antiparkinson drugs, when they are coadministered with levodopa. Based on x-ray structure of rat COMT (rCOMT), the three dimensional structure of human COMT (hCOMT) was constructed by comparative homology modeling using MODELLER. The catalytic site of these two proteins showed subtle differences, but these differences are important to determine the characterization of COMT inhibitor. Ligand docking study is carried out for complex of hCOMT and COMT inhibitors using AutoDock. Among fifteen inhibitors chosen from world patent, nine models were energetically favorable. The average value of heavy atomic RMSD was 1.5 $\AA$. Analysis of ligand-protein binding model implies that Arg201 on hCOMT plays important roles in the interactions with COMT inhibitors. This study may give insight to develop new ways of antiparkinson drug.

• Journal of Rhinology
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• v.60 no.1
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• pp.2-10
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• 2022

Background: Although the role of human papillomavirus (HPV) in sinonasal inverted papilloma (SNIP) has been investigated, the link between HPV infection and SNIP recurrence remains controversial. This meta-analysis aimed to investigate the association between HPV infection and recurrence of SNIP. Methods: The PubMed, Web of Science, Google Scholar, and Cochrane Library databases were searched (until 16 June 2021) to collect all relevant articles. The pooled odds ratio (OR) with 95% confidence interval (CI) was calculated using the fixed effects model. In addition, subgroup analysis, assessment of publication bias, and sensitivity analyses were performed. Results: Fourteen eligible articles, including 592 patients with SNIP, were included in this study. Pooled analysis revealed that HPV-positive cases exhibited a significantly higher OR of tumour recurrence than HPV-negative counterparts). A significant association between HPV infection and tumour recurrence remained stable in subgroup analyses according to the publication year of the studies. Conclusions: Our meta-analysis demonstrates that HPV infection is significantly associated with the recurrence of SNIP, suggesting the pathological role of HPV in SNIP. These results suggest that HPV infection should be considered in the management of SNIP.

• Journal of the Korean Applied Science and Technology
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• v.33 no.2
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• pp.286-292
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• 2016

1, 2-Hexanediol galactoside (HD-gal) has been synthesized from 1, 2-hexanediol (HD), a cosmetic preservative, using recombinant Escherichia coli ${\beta}$-galactosidase (${\beta}$-gal) at the high lactose concentration (300 g/l). To confirm the molecular structure of synthesized HD-gal, NMR ($^1H$- and $^{13}C$-) spectroscopy and mass spectrometry of HD-gal were conducted. $^1H$ NMR spectrum of HD-gal showed multiple peaks corresponding to the galactocyl group, which is an evidence of galactocylation on HD. Downfield proton peaks at ${\delta}_H$ 4.44 ppm and multiple peaks from ${\delta}_H$3.96~3.58 ppm were indicative of galactocylation on HD. Up field proton peaks at ${\delta}_H$ 1.60~1.35 ppm and 0.92 ppm showed the presence of $CH_2$ and $CH_3$ protons of HD. $^{13}C$ NMR spectrum revealed the presence of 21 carbons suggestive of ${\alpha}$- and ${\beta}$-anomers of HD-gal. Among 12 carbon peaks from each anomers, the 3 peaks at dC 68.6, 60.9 and 13.2 ppm were assigned to be overlapped showing only 21 peaks out of total 24 peaks. The mass value (protonated HD-gal, m/z = 281.1601) from mass spectrometry analysis of HD-gal, and $^1H$ and $^{13}C$ NMR spectral data were in well agreement with the expecting structure of HD-gal. For further study, the minimum inhibitory concentrations (MICs) of HD-gal against bacteria will be investigated, and, in addition, cytotoxicity to human skin cells of HD-gal will be examined. It is expected that it will eventually be able to develop a new cosmetic preservative, which have low cytotoxicity against human skin cell and maintains antimicrobial effect.

• YAKHAK HOEJI
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• v.44 no.5
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• pp.399-405
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• 2000

We have synthesized a novel platinum (II) coordination complex containing trans-ι-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis (diphenylphosphino)ethane (DPPE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt (trans-ι-DACH) (DPPE)].2NO$_3$(PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocarcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against MKN-45/S, MKN-45/ADR and MKN-45/CDDP cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells, and human renal cortical tissues, determined using the MTT assaying technique, the ($^3$H)-thymidine uptake and the glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum (II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.19
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• pp.8337-8343
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• 2014

Paclitaxel is one of the best anticancer agents that has been isolated from plants, but its major disadvantage is its dose-limiting toxicity. In this study, we obtained evidence that the active mutant IPP5 ($8-60hIPP5^m$), the latest member of the inhibitory molecules for protein phosphatase 1, sensitizes human cervix carcinoma cells HeLa more efficiently to the therapeutic effects of paclitaxel. The combination of $8-60hIPP5^m$ with paclitaxel augmented anticancer effects as compared to paclitaxel alone as evidenced by reduced DNA synthesis and increased cytotoxicity in HeLa cells. Furthermore, our results revealed that $8-60hIPP5^m$ enhances paclitaxel-induced G2/M arrest and apoptosis, and augments paclitaxel-induced activation of caspases and release of cytochrome C. Evaluation of signaling pathways indicated that this synergism was in part related to downregulation of NF-${\kappa}B$ activation and serine/threonine kinase Akt pathways. We noted that $8-60hIPP5^m$ downregulated the paclitaxel-induced NF-${\kappa}B$ activation, $I{\kappa}B{\alpha}$ degradation, PI3-K activity and phosphorylation of the serine/threonine kinase Akt, a survival signal which in many instances is regulated by NF-${\kappa}B$. Together, our observations indicate that paclitaxel in combination with $8-60hIPP5^m$ may provide a therapeutic advantage for the treatment of human cervical carcinoma.

• Biomolecules & Therapeutics
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• v.17 no.2
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• pp.211-216
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• 2009

To understand the relationship between the metabolism of wogonoside from the rhizome of Scutellaria baicalensis, and its anti-pruritic effect, we anaerobically incubated it with human fecal microflora, identified its metabolite identified, and investigated its anti-pruritic effect in compound 48/80 or histamineinduced pruritic mice. Wogonoside was metabolized to wogonin, with metabolic activity of $6.9{\pm}5.1\;nmol/h/mg$ wet weight of fecal microflora. Orally administered wogonoside had more potent anti-scratching behavioral effect in compound 48/80 or histamine-treated mice than intraperitoneally treated one, apart from orally administered its metabolite, wogonin, which was more potent than the orally administered one. Wogonoside showed more potent anti-pruritic effects when administered at 5 h prior to the pruritic agent treatment than when administered at 1 h before. However, wogonin orally administered 1 h before the treatment with pruritic agents showed a more potent anti-pruritic effect than when treated at 5 h before. Orally administered wogonoside may be metabolized to wogonin in the intestine and its anti-scratching behavioral effect may be dependent on its metabolism by intestinal microflora.

• Archives of Pharmacal Research
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• v.29 no.4
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• pp.310-317
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• 2006

We investigated the effects of trinitrobenzene sulfonic acid (TNBS), an amino-group reagent, on the human ether-a-go-go-related gene (HERG) $K^+$ channels expressed in Xenopus oocytes. TNBS neutralizes the positively charged amino-groups of peptide N-terminal and lysine residues. External application of TNBS at 10 mM for 5 min irreversibly shifted the curves for currents at the end of the pulse and tail currents of HERG to a more negative potential and decreased the maximal amplitude of the $I_{tail}$ curve $(I_{tail,max})$. TNBS had little effect on either the activated current-voltage relationship or the reversal potential of HERG current, indicating that TNBS did not change ion selectivity properties. TNBS shifted the time constant curves of both activation and deactivation of the HERG current to a more hyperpolarized potential; TNBS's effect was greater on channel opening than channel closing. External $H^+$ is known to inhibit HERG current by shifting $V_{1/2}$ to the right and decreasing $I_{tail,max}$. TNBS enhanced the blockade of external $H^+$ by exaggerating the effect of $H^+$ on $I_{tail,max}$, not on $V_{1/2}$. Our data provide evidence for the presence of essential amino-groups that are associated with the normal functioning of the HERG channel and evidence that these groups modify the blocking effect of external $H^+$ on the current.