minocycline is more potent than tetracycline and doxycycline in inhibiting mmp-9 in vitro

نویسندگان

mina modheji ahvaz jundishapur university of medical sciences, ahvaz, ir iran

samaneh olapour department of pharmacology and toxicology, school of pharmacy, ahvaz jundishapur university of medical sciences, ahvaz, ir iran

mohammad javad khodayar department of pharmacology and toxicology, school of pharmacy, ahvaz jundishapur university of medical sciences, ahvaz, ir iran

ali jalili cellular and molecular research center, kurdistan university of medical sciences, sanandaj, ir iran

چکیده

conclusions our results suggest that tetracyclines dose-dependently inhibit mmp-9 activity, and among the common clinical tetracyclines, minocycline provides the most potent inhibition of excess mmp-9 activity and its consequences. materials and methods an mmp-9-rich culture medium of u-937 cells was used as the source of the enzyme. serial dilutions of 5, 20, 100, 200, and 500 µm of each drug were placed in zymography incubation buffer. gelatin zymography was run, and densitometry of the bands was performed using image j software. the resulting data were used to draw dose-response curves using graphpad prism software. results our results showed that tetracyclines inhibited mmp-9 activity with ic50 values of 40.0, 10.7, and 608.0 µm for tetracycline, minocycline, and doxycycline, respectively. minocycline showed the highest potency in mmp-9 inhibition (p < 0.0001), while tetracycline was found to be more potent than doxycycline in mmp-9 inhibition based on the zymography experiments (p < 0.0001). background tetracyclines are antimicrobial agents that possess anti-inflammatory and matrix metalloproteinase (mmp) inhibitory effects. tetracycline, doxycycline, and minocycline have shown different potencies in inhibiting various mmps. mmps are a conserved family of zinc-dependent endopeptidases, which are involved in various physiologic and pathologic conditions. mmp-9 is among the most important proteases involved in the development of cardiovascular disease, cancer, and inflammatory disease objectives considering the central role of mmp-9 in the above-mentioned diseases and the variable inhibitory potentials of routine tetracyclines, including tetracycline, doxycycline, and minocycline, this study measured the inhibitory effect of these routine tetracycline agents on mmp-9 activity obtained from u-937 cell cultures using the zymography method.

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Comparative susceptibility of anaerobic bacteria to minocycline, doxycycline, and tetracycline.

The comparative susceptibility of 622 recent clinical isolates of anaerobic bacteria to minocycline, doxycycline, and tetracycline was determined by an agar-dilution technique. In addition to Bacteroides fragilis, a variety of other anaerobic bacteria was resistant to achievable blood concentrations of tetracycline (55% inhibited by 6.25 mug/ml) and doxycycline (58% inhibited by 2.5 mug/ml). In...

متن کامل

Nilotinib Is More Potent than Imatinib for Treating Plexiform Neurofibroma In Vitro and In Vivo

Plexiform neurofibromas (PNFs) are benign nerve sheath tumors mostly associated with neurofibromatosis type 1. They often extend through multiple layers of tissue and therefore cannot be treated satisfactorily by surgery. Nilotinib is a tyrosine kinase inhibitor used to treat leukemia, with advantages over the prototype imatinib in terms of potency and selectivity towards BCR-ABL, and the DDR, ...

متن کامل

Relation between lipophilicity and pharmacological behavior of minocycline, doxycycline, tetracycline, and oxytetracycline in dogs.

Four tetracyclines were studied in dogs to determine the relation between their lipophilicity and various other pharmacological characteristics. Lipid solubility correlated inversely with the mean concentration of drug in arterial plasma and renal uptake and excretion, and directly with the biliary concentration gradient (level in bile/level of free drug in serum). Only the more lipophilic cong...

متن کامل

PI3K and mTOR inhibitor, NVP-BEZ235, is more toxic than X-rays in prostate cancer cells

Background: Radiotherapy and adjuvant androgen deprivation therapy have historically been the first treatment choices for prostate cancer but treatment resistance often limits the capacity to effectively manage the disease. Therefore, alternative therapeutic approaches are needed. Here, the efficacies of radiotherapy and targeting the pro-survival cell signaling components epidermal growth fact...

متن کامل

Minocycline, a tetracycline derivative, is neuroprotective against excitotoxicity by inhibiting activation and proliferation of microglia.

Minocycline, a semisynthetic tetracycline derivative, protects brain against global and focal ischemia in rodents. We examined whether minocycline reduces excitotoxicity in primary neuronal cultures. Minocycline (0.02 microm) significantly increased neuronal survival in mixed spinal cord (SC) cultures treated with 500 microm glutamate or 100 microm kainate for 24 hr. Treatment with these excito...

متن کامل

Suppression of MMP-9 by doxycycline in brain arteriovenous malformations

BACKGROUND The primary aim of this study is to demonstrate the feasibility of utilizing doxycycline to suppress matrix metalloproteinase-9 (MMP-9) in brain arteriovenous malformations (AVMs). METHODS Ex-vivo treatment of AVM tissues: Intact AVM tissues were treated with doxycycline for 48 hours. Active and total MMP-9 in the medium were measured. Pilot trial: AVM patients received either doxy...

متن کامل

منابع من

با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید


عنوان ژورنال:
jundishapur journal of natural pharmaceutical products

جلد ۱۱، شماره ۲، صفحات ۰-۰

کلمات کلیدی
[ ' t e t r a c y c l i n e s ' , ' m a t r i x m e t a l l o p r o t e i n a s e ' , 9 , ' z y m o g r a p h y ' , ' i c 5 0 ' ]

میزبانی شده توسط پلتفرم ابری doprax.com

copyright © 2015-2023