• 대한한방내과학회지
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• 제33권4호
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• pp.609-614
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• 2012

Drug-induced liver injury (DILI) is a common cause of acute hepatitis. Regarding the risk of DILI from herbal preparations, there are controversial issues such as exaggerated reports straying far from the truth and lack of discrimination between herbal drugs and folk remedies or food supplements. This study reported one case of a patient with DILI caused by Smilacis Chinae Radix and cured in an Oriental hospital. Smilacis Chinae Radix has been used as an anti-inflammatory, anti-microbial, detoxification and anticancer compound, as a folk remedy. This report would provide helpful information for management of DILI by folk remedies or herbal drugs.

• 약학회지
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• 제47권5호
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• pp.331-338
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• 2003

A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.

• 대한미생물학회지
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• 제22권2호
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• pp.185-193
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• 1987

Ten species of herbae, which have been used to treat cancers in Chinese medicine, were tested to investigate their mutagenicity or antimutagenicity in S. typhimurium TA97, TA98, TA100, TA1535, and TA1538. Scolopendra centipede was weakly active in reversion of the frameshift mutation in S. typhimurium TA97 strain and the base-pair substitution in TA100 and TA1535 strains. Other herbae such as Coix lachryma, Dianthus superbus, Tricanthoshse kirilowii, Eupatorium formosanum, Lithospermum erythrorhizon, Ansaema japonicum, Curcuma zedoaria, Helicteres angustifolia, and Euonymus sieboldianus did not show any of the mutagenic potential, regardless of the metabolic activation with rat hepatic microsomal fraction. Dianthus superbus, Eupatorium formosanum, and Euonymus sieboldianus exhibited suppressive activities on microbial mutagenesis of N-methyl-N'-nitrosoguanidine, a base-pair substitution mutagen, in TA1535 and TA100 tester strains. The antimutagenic activities of Dianthus superbus and Euonymus sieboldianus appeared to be dose-dependant.

• Asian Pacific Journal of Cancer Prevention
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• 제14권10호
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• pp.5855-5860
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• 2013

Phytochemicals are among the natural chemopreventive agents with most potential for delaying, blocking or reversing the initiation and promotional events of carcinogenesis. They therefore offer cancer treatment strategies to reduce cancer related death. One such promising chemopreventive agent which has attracted considerable attention is sulforaphane (SFN), which exhibits anti-cancer, anti-diabetic, and anti-microbial properties. The present study was undertaken to assess effect of SFN alone and in combination with a chemotherapeutic agent, gemcitabine, on the proliferative potential of MCF-7 cells by cell viability assay and authenticated the results by nuclear morphological examination. Further we analyzed the modulation of expression of Bcl-2 and COX-2 on treatment of these cells with SFN by RT-PCR. SFN showed cytotoxic effects on MCF-7 cells in a dose- and time-dependent manner via an apoptotic mode of cell death. In addition, a combinational treatment of SFN and gemcitabine on MCF-7 cells resulted in growth inhibition in a synergistic manner with a combination index (CI)<1. Notably, SFN was found to significantly downregulate the expression of Bcl-2, an anti-apoptotic gene, and COX-2, a gene involved in inflammation, in a time-dependent manner. These results indicate that SFN induces apoptosis and anti-inflammatory effects on MCF-7 cells via downregulation of Bcl-2 and COX-2 respectively. The combination of SFN and gemcitabine may potentiate the efficacy of gemcitabine and minimize the toxicity to normal cells. Taken together, SFN may be a potent anti-cancer agent for breast cancer treatment.

• 한국수산과학회지
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• 제57권3호
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• pp.216-226
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• 2024

This study screened the antimicrobial and anti-inflammatory activities of three extracts [1% acetic acid (HAc), distilled water (D.W.), and ethanol] from the common stalked barnacle Pollicipes mitella. Among the extracts, the 1% HAc extract showed the strongest antibacterial activity against several bacteria, but exhibited no activity against Candida albicans. To improve the degree of separation of the 1% HAc extract, solid-phase extraction was performed using a C18 cartridge with three solvents (D.W., 60A, and 100A). The 1% HAc 60A eluate showed the strongest antibacterial activity and enzyme, salt, and temperature stability, with no hemolytic activity. In addition, strong DNA-binding ability but no bacterial membrane permeability was observed. These results indicate that the P. mitella 1% HAc 60A eluate may contain antibacterial organic compounds that target intracellular components but not bacterial membranes. In addition, the 1% HAc 60A eluate exhibited potent inhibitory activity to reduce the production of inflammatory mediators (nitric oxide and prostaglandin E₂) and pro-inflammatory cytokines (tumor necrosis factor-α, interleukin (IL)-6, and IL-1β) with no cytotoxicity. Therefore, the P. mitella 1% HAc 60A eluate has anti-inflammatory activity. Collectively, our results suggest that the P. mitella 1% HAc 60A eluate can be used as a bioactive source with antibacterial and anti-inflammatory activities.

• Archives of Pharmacal Research
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• 제25권6호
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• pp.770-780
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• 2002

The airway surface liquid (ASL), often referred to as mucus, is a thin layer of fluid covering the luminal surface of the airway. The major function of mucus is to protect the lung through mucociliary clearance against foreign particles and chemicals entering the lung. The mucus is comprised of water, ions, and various kinds of macromolecules some of which possess the protective functions such as anti-microbial, anti-protease, and anti-oxidant activity. Mucus glycoproteins or mucins are mainly responsible for the viscoelastic property of mucus, which is crucial for the effective mucociliary clearance. There are at least eight mucin genes identified in the human airways, which will potentially generate various kinds of mucin molecules. At present, neither the exact structures of mucin proteins nor their regulation are understood although it seems likely that different types of mucins are involved in different functions and might also be associated with certain airway diseases. The fact that mucins are tightly associated with various macromolecules present in ASL seems to suggest that the defensive role of ASL is determined not only by these individual components but rather by a combination of these components. Collectively, mucins in ASL may be compared to aircraft carriers carrying various types of weapons in defense of airborne enemies.

• 대한의생명과학회지
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• 제17권3호
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• pp.217-223
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• 2011

${\beta}$-sitosterol glucoside exists in a variety of plants and have anti-tumor, anti-microbial, and immunomodulatory activities. Mast cells and eosinophils play important roles in a variety of inflammatory diseases, specifically asthma and atopic dermatitis. In the present study, we used lactose-${\beta}$-sitosterol (L-BS) and investigated the effect of L-BS on inflammatory responses of the human mast cell line, HMC-1 and the human eosinophilic leukemia cell line, EoL-1. In HMC-1 cells, L-BS significantly inhibited cell migration in response to stem cell factor without cytotoxicity. However, the mRNA expression of CC chemokine receptors (CCRs), including CCR1-5, were not altered after L-BS treatment in HMC-1 cells. LPS-induced IL-4 production was also suppressed by L-BS in a dose-dependent manner. In EoL-1 cells, the concentration ranging from 0.1 ${\mu}M$ to 10 ${\mu}M$ of L-BS had no cytotoxicity and had no effect on mRNA expression of major protein-mediators derived from activated eosinophils. However, 100 ${\mu}M$ of L-BS induced the apoptosis of EoL-1 cells in a time-dependent manner. This finding indicates the possibility of L-BS as a potential therapeutic molecule in inflammatory diseases and may contribute to the need to improve current therapeutic drugs.

• Advances in Traditional Medicine
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• 제1권1호
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• pp.71-81
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• 2000

High molecular weight water-insoluble chitosan alone has been previously shown to exhibit in vitro stimulatory effect on macrophages nitric oxide (NO) production. However, high molecular weight water-soluble chitosan (WSC) had no effect on NO production by itself. When WSC was used in combination with recombinant $interferon-{\gamma}\;(Rifn-{\gamma})$, there was a marked cooperative induction of NO synthesis in a dose-dependent manner. The optimal effect of WSC on NO synthesis was shown at 24 h after treatment with $rIFN-{\gamma}$. The increased production of NO from $rIFN-{\gamma}$ plus WSC-stimulated RAW 264.7 macrophages was decreased by the treatment with $N^G$ $monomethyl-_L-arginine$. The increase in NO synthesis was reflected, as an increased amounts of inducible NO synthase (iNOS) protein. Synergy between $rIFN-{\gamma}$ and WSC was mainly dependent on WSC-induced nuclear $factor-_KB$ activation. The present results indicate that WSC may provide various activities such as anti-microbial, anti-tumoral, and anti-viral. In addition, since NO has emerged as an important intracellular and intercellular regulatory molecule having functions as diverse as vasodilation, neural communication, cell growth regulation and host defense, it is tempting to hypothesize that this WSC is involved in the local control of the various fundamental processes such as cardiagra, cardiac infarction, impotence etc.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.258-269
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• 2002

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

• KSBB Journal
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• 제19권3호
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• pp.187-191
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• 2004

14종 한약재의 70% 에탄을 추출물의 Helicobacter pylori에 대한 항균활성은 황련 (Coptis japonica Makino)이 가장 뛰어 났으며, 소엽 (Perilla frutescens var. acuta KUDO), 소목 (Caesalpinia sappan L.) 및 형개 (Schizonepeta tenuifolia Briq.)의 경우에도 높은 항균활성을 나타내었다. 그러나 Helicobacter pylori의 위내 서식을 도와주는 것으로 알려진 urease 활성억제능은 연교 (Forsythiae Fructus)의 메탄올 (80%) 추출물에서 가장 높았으며, 소목 및 형개의 추출물도 높았다. 특히 연교의 경우 한약재 추출물을 넣지 않은 대조군과 비교하여 80% 이상의 활성이 억제되었다. 연교의 메탄올 추출물을 물, 에틸아세테이트 (ethyl acetate), 부탄을 순으로 분획하여 각 분획물에 대한 urease 활성억제능을 검색한 결과 에틸아세테이트 분획에서 92%의 urease 활성이 억제되었다.