• Archives of Pharmacal Research
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• 제29권1호
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• pp.26-33
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• 2006

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

• Journal of Veterinary Science
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• 제22권1호
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• pp.4.1-4.13
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• 2021

Background: Microsporum canis is a zoonotic disease that can cause dermatophytosis in animals and humans. Objectives: In clinical practice, ketoconazole (KTZ) and other imidazole drugs are commonly used to treat M. canis infection, but its molecular mechanism is not completely understood. The antifungal mechanism of KTZ needs to be studied in detail. Methods: In this study, one strain of fungi was isolated from a canine suffering with clinical dermatosis and confirmed as M. canis by morphological observation and sequencing analysis. The clinically isolated M. canis was treated with KTZ and transcriptome sequencing was performed to identify differentially expressed genes in M. canis exposed to KTZ compared with those unexposed thereto. Results: At half-inhibitory concentration (½MIC), compared with the control group, 453 genes were significantly up-regulated and 326 genes were significantly down-regulated (p < 0.05). Quantitative reverse transcription polymerase chain reaction analysis verified the transcriptome results of RNA sequencing. Gene ontology enrichment analysis and Kyoto Encyclopedia of Genes and Genomes enrichment analysis revealed that the 3 pathways of RNA polymerase, steroid biosynthesis, and ribosome biogenesis in eukaryotes are closely related to the antifungal mechanism of KTZ. Conclusions: The results indicated that KTZ may change cell membrane permeability, destroy the cell wall, and inhibit mitosis and transcriptional regulation through CYP51, SQL, ERG6, ATM, ABCB1, SC, KER33, RPA1, and RNP genes in the 3 pathways. This study provides a new theoretical basis for the effective control of M. canis infection and the effect of KTZ on fungi.

• 디지털융복합연구
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• 제13권9호
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• pp.369-375
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• 2015

본 연구는 한 대학병원에서 6 년간 (2006-2011) 다양한 임상 검체에서 분리된 진균의 빈도를 조사하여 임상검체에서 진균의 종류에 따른 연관성을 파악하여 이와 관련된 환자 관리에 필요한 정보를 제공하기 위함이다. 경상남도의 단일 대학병원 진단검사의학과 미생물검사실로 의뢰된 검체 163,530건을 대상으로 하였고 배양에서 양성으로 판정된 진균 5,378주(3.3%)에 대하여 환자의 일반적인 특징과 성별, 연령, 검체 종류를 분석하였다. 균주별 분리빈도는 Candida albicans가 41.9%로 가장 많았고, Candida glabrata (15.5%), Candida tropicalis (14.6%)가 그 다음 순서로 분리되었다. 분리건수는 2006년 526건에서 2011년이 1,145건으로 2배이상 증가하였다. 연령별로는 60대(27.0%)와 70대(26.5%)에서 가장 흔히 분리되었다. 검체별로는 소변이 44.8%로 가장 많았다. 성별에 따른 분리는 남성이 52.4%로 여성 47.6%보다 약간 높았다. 추후 전국적인 분포도를 연구하고, 항진균 융복합 약제 감수성을 분석한다면 더 유익한 자료를 제공할 것으로 사료된다.

• Advances in Traditional Medicine
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• 제3권4호
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• pp.191-195
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• 2003

Euphorbia hirta, locally called 'ara tanah' or 'susun nabi' in Malaysia is a small annual herb common to the tropical countries and belongs to the same family as the tic and tapioca. E. hirta has had a long history of usage in the treatment of various ailments. In this current study, in vitro sensitivity test of crude aqueous and ethanol extracts of leaves and barks of E. hirta was carried out against bacteria (Escherichia coli, Salmonella enteritidis, Staphylocccus aureus and Bacillus subtilis) and fungi (Microsporum canis, Aspergillus fumigatus, Candida albicans and Candida tropicalis) using the discs diffusion method. The extract-impregnated discs (20, 40 and $80\;{\mu}g/{\mu}l$), the E. hirta extracts inhibited the growth of all the bacteria tested. The growth of C. albicans was inhibited in a concentration dependent manner by the aqueous leaves and barks extracts. C. tropicalis was found to be sensitive to the aqueous leaves extracts. The results were compared to antibacterial drugs of chloramphenicol, ampicilin, penicillin G, and enrofloxacine; and to antifungal drug of ketoconazole, itraconazole and miconazole. In this current study, it can be concluded that this plant has antimicrobial activity that is as potent as the standard antimicrobial drugs against certain microorganisms.

• 한국진공학회:학술대회논문집
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• 한국진공학회 2014년도 제46회 동계 정기학술대회 초록집
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• pp.260-260
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• 2014

Dermatophytes can invade in keratinized tissues and cause dermatophytosis [1] that rank among the most widespread and common infectious diseases world-wide. Although several systemically and topically administered drugs with activities against these fungi are available, still complete eradication of some of these infections, is difficult and relapses and remissions are often observed [2,3]. In addition, some people are allergic to many of the available drugs which add complications even more. Therefore, the search for novel, selective and more effective therapy is always required and it may help the clinicians to choose the correct treatment for their patients. Non-thermal plasmas primarily generate reactive species and recently have emerged as an efficient tool for medical applications including sterilization. In this study, we evaluated the ability of non-thermal dielectric barrier discharge (DBD) plasma for the inactivation of clinical isolates of Trichophyton genera, Trichophyton mentagrophytes (T. mentagrophytes) and Trichophyton rubrum (T. rubrum), which cause infections of nails and skin and, are two of the most frequently isolated dermatophytes [4]. Our results showed that DBD plasma has considerable time dependent inactivation potential on both T. mentagrophytes and T. rubrum in-vitro. Furthermore, the mechanisms for plasma based T. mentagrophytes and T. rubrum inactivation and planning for in-vivo future studies will be discussed.

• 대한수의학회지
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• 제29권1호
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• pp.69-73
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• 1989

준임상형 유방염 이환 젖소의 유즙과 유두컵으로부터 분리된 Candida속 균의 8종 항진균성약제에 대한 감수성을 조사하였던 결과는 다음과 같다. 총 53주의 Candida속균 중 98.2%, 94.4%, 84.8%의 균주가 각각 clotrimazole, econazole, miconazole의 농도 $25{\mu}g/ml$이하에서 발육이 억제됨으로서, 이들 약제의 항균력이 타 약제에 비하여 우수하였다. 균종별로 보면 C albicans는 clotrimazole에 대한 감수성이 가장 높았으며, 기타 비교적 감수성이 높았던 약제는 5-fluorocytosine, econazole, miconazole의 순이었다. C pseudotropicalis와 C guilliermondii는 haloprogin, clotrimazole, miconazole, econazole, 5-fluorocytosine등에 높은 감수성을 나타내었으며, haloprogin의 평균 MIC가 $0.17{\sim}0.19{\mu}g/ml$로 가장 우수하였다. C krusei는 cycloheximide에 대한 감수성이 가장 높았으며, 그의 비교적 감수성이 높았던 약제는 clotrimazole, haloprogin, miconazole, econazole의 순이었다. 한편 C parapsilosis는 econazole, cycloheximide, clotrimazole등에 다소 감수성을 나타내었으나, 이들 약제의 MIC는 econazole(기하평균 MIC $7.26{\mu}g/ml$)을 제외하고는 타균종에서 보다 현저히 낮았다. 또한 C tropicalis는 전 공시약제에 대하여 감수성이 낮은 경향이었다.

• Journal of Microbiology and Biotechnology
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• 제27권4호
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• pp.685-693
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• 2017

Candidiasis involving the biofilms of Candida albicans is a threat to immunocompromised patients. Candida biofilms are intrinsically resistant to the antifungal drugs and hence novel treatment strategies are desired. The study intended to evaluate the anti-Candida activity of allyl isothiocyanate (AITC) alone and with fluconazole (FLC), particularly against the biofilms. Results revealed the concentration-dependent activity of AITC against the planktonic growth and virulence factors of C. albicans. Significant (p <0.05) inhibition of the biofilms was evident at ${\leq}1mg/ml$ concentrations of AITC. Notably, a combination of 0.004 mg/ml of FLC and 0.125 mg/ml of AITC prevented the biofilm formation. Similarly, the preformed biofilms were significantly (p <0.05) inhibited by the AITC-FLC combination. The fractional inhibitory concentration indices ranging from 0.132 to 0.312 indicated the synergistic activity of AITC and FLC against the biofilm formation and the preformed biofilms. No hemolytic activity at the biofilm inhibitory concentrations of AITC and the AITC-FLC combination suggested the absence of cytotoxic effects. The recognizable synergy between AITC and FLC offers a potential therapeutic strategy against biofilm-associated Candida infections.

• Journal of Chest Surgery
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• 제30권5호
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• pp.544-547
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• 1997

저자들은 흉막 아스페르길루스증을 치험하였다. 50세 여자가 2주 동안의 권태감, 식욕부진, 객담을 동반한 기침 및 우측 홉막성 흉통을 주소로 내원하였다. 과거력상 10여년전 폐결핵으로 약물치료를 받은 적이 있었 다. 일반 흉부 사진상 폐우상엽에 공동을 동반한 농기흉을 보였으며,흉부 전산화 단층촬영상 우측 폐에 분 획된 농기흉 및 기관지 늑막루 소견을 보이는 공동이 관찰되었다. 폐 박피술과 부분절제,그리고 흉막절제술 을 시행하였으며 술후 경과는 만족스러웠다. 흉막 아스페르길루스증은 매우 드물고 잘 치유되지 않는 질병 이나 전신적 항진균제제 투여 및 수술적 치료로 별다른 합병증 없이 좋은 결과를 얻을 수 있었으나 재발의 가능성 때문에 계속 추적 관찰 중이다.

• Journal of Microbiology and Biotechnology
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• 제19권9호
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• pp.869-872
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• 2009

The cyclic undecapeptide cyclosporin A (CyA), one of the most valuable immunosuppressive drugs, is produced nonribosomally by a multifunctional cyclosporin synthetase enzyme complex by the filamentous fungus Tolypocladium niveum. To increase CyA productivity by wild-type T. niveum (ATCC 34921), random mutagenesis was first performed using an antifungal agar-plug colony assay (APCA) selection approach. This generated a mutant strain producing more than 9-fold greater CyA than the wild-type strain. Additionally, a foreign bacterial gene, Vitreoscilla hemoglobin gene (VHb), was transformed via protoplast regeneration and its transcription was confirmed by RT-PCR in the UV-irradiated mutant cell. This led to an additional 33.5% increase of CyA production. Although most protoplast-regenerated T. niveum transformants tend to lose CyA productivity, the optimized combination of random mutagenesis and protoplast transformation described here should be an efficient strategy to generate a commercially valuable, yet metabolite low-producing, fungal species, such as CyA-producing T. niveum.

• Maxillofacial Plastic and Reconstructive Surgery
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• 제13권4호
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• pp.456-461
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• 1991

This is a case report of invasive aspergillosis of the right maxillary antrum and the left lung in a 43 year-old male patient with diabetes mellitus and liver cirrhosis. The results were as follows. 1. Invasive aspergilliosis should be considered in compromised patients who have nasal symptomatology, infraorbital swelling and pain. 2. Invasive aspergillosis is a rapidly progressive mycotic infection of the sinus which may extend to the orbit, nasal cavity and cheek. 3. Surgical intervention is particularly urgent in orbital aspergillosis in patient in whom the eyesight is still preserved. 4. Diagnosis depends upon pathological demonstration of tissue invasion by organism with the typical morphology of aspergillus species. 5. Long-term antifungal drugs should be administrated postoperatively in pathint with invasive aspergillosis.