Journal of Advanced Biomedical Sciences
مجله علوم زیست پزشکی پیشرفته
JABS
Medical Sciences
http://jabs.fums.ac.ir
1
admin
2228-5105
2783-1523
8
7
14
8888
13
en
jalali
1397
9
1
gregorian
2018
12
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8
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online
1
fulltext
fa
ارزیابی بیولوژیکی بخشهای هتروسیکل تعدادی از مشتقات جدید آزولها بهعنوان عوامل بالقوه ضد باکتری و ضد قارچ
Biological Evaluation of Heterocycle Moiety of Some Novel azoles Derivatives as Antibacterial and Antifungal potential Agents
بيوشيمي بالینی
Biochemistry
پژوهشي
Research
<strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">زمینه و هدف:</span></span></strong> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">هستههای آزول، بخش بسیار مهمی از داروهای ضد میکروبی، ضد درد و ضدالتهاب را تشکیل میدهند</span></span><span style="font-family:b mitra;"><span style="font-size:10.0pt;">. </span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">آزولها گروهی از ترکیبات ضد باکتری و ضد قارچ هستند که به دلیل پایین بودن سمیت و اثربخشی بالا، دارای طیف گستردهای از فعالیت میباشند.</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">امروزه</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">تلاشهای</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">فراوان</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">برای</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">توسعه داروهای</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ضد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">باکتری</span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> و ضد قارچ</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">با</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">سمیت</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">کمتر،</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">اثربخشی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">بیشتر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">و مکانیسم</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">عمل</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">جدید</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">صورت</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">گرفته</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">است. در</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">این</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مطالعه</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">تلاش شده است</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">تا اثرات</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ضد</span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> باکتریایی و ضد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">قارچی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مشتقات</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">جدید</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">آزولی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">را</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">بررسی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">کنیم</span></span><span dir="LTR"><span style="font-family:times new roman,serif;"><span style="font-size:8.0pt;">.</span></span></span><em><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"></span></span></em><br>
<strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مواد و روشها:</span></span></strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> این مطالعه بهصورت </span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">توصیفی - مقطعی انجام شد.</span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> فعالیت</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ضد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">باکتریایی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">و</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ضد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">قارچی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ترکیبات</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">طراحیشده</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">به</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ترتیب</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">بر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">روی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">سوشهای</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">استاندارد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">گرم</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">منفی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">و</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">گرم</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مثبت</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">و</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">قارچهای</span></span> <em><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">آسپرژیلوس</span></span></em> <em><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">نیجر</span></span></em><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">،</span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> <em>آسپرژیلوس فلاووس</em>، <em>کاندیدا آلبیکانز</em></span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">به</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">کمک</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">روش حداقل غلظت مهارکنندگی انجام شد.</span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"></span></span><br>
<strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">نتایج:</span></span></strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> از میان</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ترکیبات موردمطالعه، ترکیب حاوی حلقه هتروسیکل 2- متیل، 4- ایمیدازول اثر ضد باکتریایی قوی را در برابر <em>سودوموناس آئروژینوزا</em>،<em> اشرشیاکلی</em> و <em>استافیلوکوک اورئوس</em>، </span></span><em><span style="letter-spacing:.1pt;"><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">باسیلوس سابتلیس</span></span></span></em><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> به اثبات رساند، درحالیکه ترکیبات حاوی حلقه هتروسیکل ایمیدازول و بنزایمیدازول اثرات ضد قارچی در برابر <em>آسپرژیلوس نیجر</em>، <em>آسپرژیلوس فلاووس</em>، <em>کاندیدا آلبیکانز</em> نشان دادند</span></span><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">.</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">حداقل غلظت مهارکنندگی از رشد این باکتریها و قارچها از 5/12 تا 200 میلیگرم بر میلیلیتر متغیر است.</span></span><br>
<strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;">نتیجهگیری:</span></span></strong><span style="font-family:b nazanin;"><span style="font-size:10.0pt;"> نتایج حاکی از آن است که ترکیبات</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">طراحیشده حاوی حلقههای هتروسیکل 2- متیل، 4- ایمیدازول، ایمیدازول و بنزایمیدازول</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">در</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مطالعهی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">حاضر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">اثرات</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ضد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">باکتریایی و ضد قارچی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">امیدبخشی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">از</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">خود</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">نشان</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">دادند.</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">از</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">طرفی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ترکیبات</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مورد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">تست</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">دارای</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">طیف</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">اثر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مناسبی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">بودند،</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">بدینجهت</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">که</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">بر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">روی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">هر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">دو</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">سویه</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">گرم</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">مثبت</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">و</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">گرم</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">منفی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">اثر</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">ضد</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">باکتریایی</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">نشان</span></span> <span style="font-family:b nazanin;"><span style="font-size:10.0pt;">دادند</span></span><span dir="LTR"><span style="font-size:8.0pt;">.</span></span><em><span style="font-family:lotusnormal,italic;"><span style="font-size:10.0pt;"></span></span></em><br>
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<strong><em>Background & Objective:</em></strong> Azole nucleuses are very important part of antimicrobial, analgesic and anti-inflammatory drugs. The azole class of compounds is the most popular among the antibacterial and antifungal classes because of its lower toxicity, higher efficacy and a broad spectrum of activity. Today, Efforts have focused on the development of new, less toxic and more efficacious antifungal and antibacterial drugs, with the novel mechanism of action. In this study, we tried to investigate the antibacterial and antifungal effects of the new azole derivatives.<br>
<strong><em>Materials & methods:</em></strong> This research is a descriptive – cross sectional study. The antibacterial and antifungal activity of compounds was evaluated using the minimum inhibitory concentration (MIC) method on a series of gram positive and gram negative bacterial strains and <em>Aspergillus niger</em>, <em>Aspergillus flavus,</em> <em>Candida albicans</em>. The Minimum Inhibitory Concentration from the growth of this bacteria and fung ranges from 12.5 mg/ml to 200 mg/ml.<br>
<strong><em>Results:</em></strong> Among the tested compounds, 4- Nitro, 2- methyl imidazole hetrocycle-pathic compound exerted potent in vitro antibacterial activity against <em>Pseudomonas aeruginosa</em>, <em>Escherichia coli</em>, <em>Bacillus subtilis</em> and <em>Staphylococcus aureus</em> while compounds (imidazole, benzimidazole hetrocycle-pathic compound) exhibited potent in vitro antifungal activity against <em>Candida albicans</em>, <em>Aspergillus flavus</em> and <em>Aspergillus niger</em>.<br>
<strong><em>Conclusion:</em></strong> Our results indicated that the designed derivatives (4- Nitro, 2- methyl imidazole, imidazole and benzimidazole hetrocycle-pathic compounds) showed effective antibacterial and antifungal activity mainly against a series of gram positive and gram negative bacterial strains. On the other hand, the tested compounds had an appropriate spectrum effect, because they showed antibacterial effect on both positive and negative strains.<br>
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عوامل ضد باکتری, عوامل ضد قارچ, آزولها, سمیت, حداقل غلظت مهارکنندگی رشد
Antibacterial Agents, Antifungal Agents, Azoles, Toxicity, Minimum Inhibitory Concentration
1106
1115
http://jabs.fums.ac.ir/browse.php?a_code=A-10-1719-2&slc_lang=fa&sid=1
abozar
roeintan
ابوذر
روئین تن
abroeintan@gmail.com
100319475328460019024
100319475328460019024
Yes
Department of Chemistry, Faculty of Science, University of Imam Hossein, Tehran, Iran
دانشگاه افسری و تربیت پاسداری امام حسین (ع)، تهران، ایران