• Journal of Microbiology and Biotechnology
• /
• v.26 no.12
• /
• pp.2036-2042
• /
• 2016

We evaluated the potentials of 10 isothiocyanates (ITCs) from cruciferous vegetables and radish root hydrolysate for inhibiting the growth of oral pathogens, with an emphasis on assessing any structure-function relationship. Structural differences in ITCs impacted their antimicrobial activities against oral pathogens differently. The indolyl ITC (indol-3-carbinol) was the most potent inhibitor of the growth of oral pathogens, followed by aromatic ITCs (benzyl ITC (BITC) and phenylethyl ITC (PEITC)) and aliphatic ITCs (erucin, iberin, and sulforaphene). Sulforaphene, which is similar in structure, but has one double bond, showed higher antimicrobial activity than sulforaphane. Erucin, which has a thiol group, showed higher antimicrobial activity than sulforaphane, which has a sulfinyl group. BITC and iberin with a short chain exhibited higher antimicrobial potential than PEITC and sulforaphane with a longer chain, respectively. ITCs have strong antimicrobial activities and may be useful in the prevention and management of dental caries.

• Advances in Traditional Medicine
• /
• v.6 no.2
• /
• pp.69-78
• /
• 2006

The isoflavonoids comprise a group of phyto-oestrogens that have useful biological activities including oestrogenic, antioxidant and anticancer. As dietary components for humans, they are bioavailable from leguminous vegetables (such as genistein from soybean), and have been well-documented to have numerous health benefits. A wide range of epidemiological studies in humans and limited studies in animals have identified isoflavonoids as potential chemopreventive agents against hormone-dependent cancers. Therefore, an attempt has been made through this review to summarise the information in the mechanisms aspect of isoflavonoid phyto-oestrogens in inhibiting cancer in vitro and in vivo in the models of human cancers.

• Bulletin of the Korean Chemical Society
• /
• v.30 no.1
• /
• pp.83-91
• /
• 2009

To develop new anticancer agents, 3-allylthio-6-aminopyridazine derivatives were synthesized from maleic anhydrides or phthalic anhydrides by formation of a pyridazine nucleus, dichlorination, allylthiolation and amination. The pyridazine nuclei were obtained by condensing a hydrazine monohydrate with maleic anhydride. An allylthio group as a pharmacologically active group was introduced into one side of a pyridazine ring. Arylalkylamines with benzene or pyridine moieties or heterocycloalkylamines with heterocycle moieties such as morpholine, piperidine, or pyrrolidine were also introduced into the para-position of allylthio pyridazine. These new compounds showed antiproliferative activities against SK-Hep-1 human liver cancer cells in MTT assays. These compounds are thus promising candidates for chemotherapy of hepatocellular carcinomas. Two compounds, 20c and 22a, showed higher potencies for inhibiting growth of hepatocellular carcinoma cells than did K6 ($ID_50$=1.08 mM). This suggests the potential anticancer activity of these two compounds.

• Bulletin of the Korean Chemical Society
• /
• v.34 no.5
• /
• pp.1487-1493
• /
• 2013

Based on the finding that the 2-aminobenzamido group of MS-275 plays a crucial role in inhibiting HDACs through chelation of zinc existing at the active site of HDAC enzymes, novel N-(2-hydroxyphenyl)arylsulfonamide derivatives were synthesized for their potential ability to inhibit HDACs and evaluated for anticancer activity against human breast cancer cell line (MCF-7). Although the synthesized arylsulfonamides have failed to significantly inhibit total HDACs activity, phenyl carbamate-linked arylsulfonamide 10 and benzyl thiocarbamate-linked arylsulfonamide 15 exhibited good anticancer activities, which were only 4.3- and 3.6-fold lower anticancer activities, respectively, than MS-275 that is undergoing phase II clinical trials. These results suggest that these compounds may act as a selective HDAC inhibitor and probably N-(2-hydroxyphenyl) sulfamoyl group may play an important role in interacting with HDAC enzymes through chelation of zinc ion.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.25 no.2
• /
• pp.306-310
• /
• 2011

Elastic fibers are found in the skin, lungs, arteries, veins and other structures. Elastases destroy the elastic fibers and cause the emphysema and pulmonary hypertension. Oxidative stress is needed for these pathologic changes. Accordingly, present study was designed to investigate the effect of Albizziae Cortex extracts (ACE) on elastase activity and anti-oxidative effects of ACE. The in vitro inhibitory effects on elastase and di(phenyl)-(2,4,6-trinitrophenyl)iminoazanium (DPPH) and nitric oxide (NO) free radical scavenging activities of ACE were measured. The elastase activity was significantly inhibited by ACE. DPPH and NO free radicals were significantly scavenged as well. ACE showed the elastase-inhibiting effects and anti-oxidative activities in vitro. These results suggest that ACE may have potential roles in the treatment of pulmonary emphysema and pulmonary hypertension.

• Journal of Microbiology and Biotechnology
• /
• v.29 no.10
• /
• pp.1603-1606
• /
• 2019

Sortase A (SrtA), a type of transpeptidase responsible for anchoring surface proteins to the peptidoglycan cell wall, is important in the virulence of gram-positive bacteria. Three compounds were isolated from marine-derived Streptomyces sp. MBTH32 using various chromatography techniques. The structures of these compounds were determined based on spectroscopic data and comparisons with previously reported data. Among the metabolites tested, lumichrome showed strong inhibitory activity against Staphylococcus aureus SrtA without affecting cell viability. The results of cell clumping activity assessment suggest the potential for using this compound to treat S. aureus infection by inhibiting SrtA activity.

• Food Science and Biotechnology
• /
• v.17 no.2
• /
• pp.434-437
• /
• 2008

The aim of this study was to investigate whether Monascus-fermented soybean extracts (MFSE) containing natural estrogen-like compounds such as isoflavones and mevinolins has potential effects on human osteoblast-like SaOS2 cells using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and alkaline phophatase (ALP) assaies. MFSE exerted biphasic dose-dependent effect; stimulating osteoblastic activity at low concentrations and inhibiting SaOS2 cells viability at high concentrations. At $10^{-8}-10^{-4}\;mg/mL$, MFSE is not only non-cytotoxic but also induced comparatively high ALP activity on SaOS2 cells. ALP activity (%) significantly increased (220.1%, p<0.05) when SaOS2 cells were treated with MFSE at a concentration of $10^{-5}\;mg/mL$, whereas slowly increased (185.6%, p<0.05) in unfermented soybean extracts (UFSE) at $10^{-3}\;mg/mL$. The potentially greater ALP activity of MFSE compared to the UFSE might partially be caused by its mevinolin, which was derived from the soybean during Monascus-fermentation. Our findings indicate that supplementation of MFSE may accelerate the speed of intracellular ALP synthesis by the bone cells when provided at optimal dosages.

• Parasites, Hosts and Diseases
• /
• v.56 no.5
• /
• pp.491-494
• /
• 2018

Multipurpose contact lens disinfecting solutions (MPDS) are widely used to cleanse and disinfect microorganisms. However, disinfection efficacy of these MPDS against Acanthamoeba cyst remain insufficient. 2, 6-dichlorobenzonitrile (DCB), a cellulose synthesis inhibitor, is capable of increasing the amoebical effect against Acanthamoeba by inhibiting its encystation. In this study, we investigated the possibility of DCB as a disinfecting agent to improve the amoebicidal activity of MPDS against Acanthamoeba cyst. Eight commercial MPDS (from a to h) were assessed, all of which displayed insufficient amoebicidal activity against the mature cysts. Solution e, f, and h showed strong amoebicidal effect on the immature cysts. Amoebicidal efficacy against mature cysts remained inadequate even when the 8 MPDS were combined with $100{\mu}M$ DCB. However, 4 kinds of MPDS (solution d, e, f, and h) including $100{\mu}M$ DCB demonstrated strong amoebicidal activity against the immature cysts. The amoebicidal activity of solution d was increased by addition of DCB. Cytotoxicity was absent in human corneal epithelial cells treated with either DCB or mixture of DCB with MPDS. These results suggested that DCB can enhance the amoebicical activity of MPDS against Acanthamoeba immature cyst in vitro.

• The Journal of Internal Korean Medicine
• /
• v.26 no.3
• /
• pp.543-550
• /
• 2005

This study was designed to identify the effects of Reynoutria Japonica on antibacterial activity aganist Bordetella pertussis ATCC 9797 which is cause of whooping cough. The ethanol- and water-extracts of more than 80 oriental herbal medicine were Investigated by Kirby -Bauer method to determine their inhibitory effects on growth of B. pertussis ATCC 9797 in vitro. For that Reynoutria Japonica was selected. The ethanol-soluble extract of Reynoutria Japonica showed relatively high antivacterial activity against B. pertussis ATCC 9797. However, the water-soluble extract of Reynoutria Japonica showed no antibacterial activity. The ethanolic extract was further fractionated with organic solvents such as hexane, chloroform, and ethyl acetate, in that order. Among the fraction tested, the chloroform fraction showed the highest antibacterial activity when the ethanol-soluble extract of Reynoutria Japonica minial inhibitory concentration(MIC) was $25{\mu}g/m{\ell}l$. Results support a role far Reynoutria Japonica in inhibiting the cell growth of B. pertussis ATCC 9797, but further experimentation is required.

• Korean Journal of Pharmacognosy
• /
• v.34 no.2 s.133
• /
• pp.161-165
• /
• 2003

Ethanol extract from Thesium chinense Tunczaninov (TCTE) was tested for breast cancer chemopreventive activity by measuring 7,12-dimethylbenz[a]anthracene (DMBA) - induced cytochrome P450 1A1 activity, induction of quinone reductase and glutathione S-transferase, and glutathione level. TCTE significantly inhibited cytochrome P45O 1A1 activity at the concentration of 90 and 150 mg/ml. TCTE induced quinone reductase activity in a dose-dependent manner in a concentration range of 3-150 mg/ml. In addition glutathione S-transferase activity and glutathione level were increased with TCTE in cultured murine hepatoma Hepa1c1c7 cells. These results suggest that TCTE has breast cancer chemopreventive potential by inhibiting cytochrome P45O 1A1 activity, inducing quinone reductase and glutathione S-transferase activities, and increasing GSH level.