Author: Javanshir, Shahrzad ; Seif, Farhad ; Dey, Sanjay Kumar ; Kamal Abdelbasset, Walid ; Farasati Far, Bahareh ; Bokov, Dmitry ; Setia Budi, Hendrik ; Pazoki-Toroudi, Hamidreza ; Widjaja, Gunawan

COVID-19 patients have shown overexpressed serum levels of several pro-inflammatory cytokines, leading to a high mortality rate due to numerous complications. Also, previous studies demonstrated that the metronidazole (MTZ) administration reduced pro-inflammatory cytokines and improved the treatment outcomes for inflammatory disorders. However, the effect and mechanism of action of MTZ on cytokines have not been studied yet. Thus, the current study aimed to identify anti-cytokine therapeutics for the treatment of COVID-19 patients with cytokine storm. The interaction of MTZ with key cytokines was investigated using molecular docking studies. MTZ-analogues, and its structurally similar FDA-approved drugs were also virtually screened against interleukin-12 (IL-12). Moreover, their mechanism of inhibition regarding IL-12 binding to IL-12 receptor was investigated by measuring the change in volume and area. IL-12-metronidazole complex is found to be more stable than all other cytokines under study. Our study also revealed that the active sites of IL-12 are inhibited from binding to its target, IL-12 receptor, by modifying the position of the methyl and hydroxyl functional groups in MTZ. Three MTZ analogues, metronidazole phosphate, metronidazole benzoate, 1-[1-(2-Hydroxyethyl)-5-nitroimidazol-2-yl]-N-methylmethanimine-oxide, and two FDA-approved drugs acyclovir (ACV), and tetrahydrobiopterin (THB) were also found to prevent binding of IL-12 to IL-12 receptor similar to MTZ by changing the surface and volume of IL-12 upon IL-12-drug/ligand complex formation. According to the RMSD results, after 100 ns MD simulations of human IL-12-MTZ/ACV/THB drug complexes, it was also observed that each complex was swinging within a few Å compared to their corresponding docking poses, indicating that the docking poses were reliable. The current study demonstrates that three FDA-approved drugs, namely, metronidazole, acyclovir and tetrahydrobiopterin, are potential repurposable treatment options for overexpressed serum cytokines found in COVID-19 patients. Similar approach is also useful to develop therapeutics against other human disorders.Communicated by Ramaswamy H. Sarma.

01 Nov 2012·Rheumatology InternationalQ4 · MEDICINE

Efficacy comparisons of the intraarticular steroidal agents in the patients with knee osteoarthritis

Q4 · MEDICINE

Article

Author: Sami Sökücü ; Kahraman Öztürk ; Akif Albayrak ; Umut Yavuz

Osteoarthritis is a chronic disease that causes serious pain and limitations in activities. Intraarticular corticosteroid injections combined with pharmacological treatment and physiotherapy have been used for years to control the local inflammation and relieve pain in the patients with osteoarthritis. There are several animal experiments which suggested that the intraarticular corticosteroid injections impair cartilage protein synthesis. However, there are no serious evidences suggesting the increase of cartilage impairment. The aim of our study was to compare the efficacy of placebo and intraarticular corticosteroid agents in the patients with symptomatic knee osteoarthritis. One hundred and twenty patients with painful knee osteoarthritis were included in the prospective, randomized, controlled study. The patients were randomized into four groups. Each group consisted of thirty patients. Intraarticular single dose of methylprednisolone acetate (40 mg, 1 ml), Betametazone disodium phosphate (3 mg, 1 ml), Triamsinolon acetonate (40 mg, 1 ml), and serum physiological (0.09% NaCl, 1 ml) were administrated to the groups, respectively. The patients were evaluated by Visual Analog Scale (0-10 cm [VAS]) for the pain severity, and by Lequesne Functional Index for functional state before treatment, and at the 1st, 3rd, 6th, and 12th weeks. Our results showed that single doses of three agents provided symptomatic and functional relief and their effects reduced at the 12th week. However, methylprednisolone acetate was a statistically more effective analgesic as compared to the other agents until the sixth week.

01 Oct 1997·The American Journal of SurgeryQ3 · MEDICINE

Preventing infection of the incision after appendectomy by using metronidazole preoperatively to infiltrate tissues at the incision

Q3 · MEDICINE

Article

Author: Wang Shubing ; Zhang Litian

METHODSFrom January 1991 to July 1995, 260 patients with acute appendicitis were operated on. After excluding 21 patients, the remaining 239 cases were randomly divided into two groups. Group A was given the treatment and group B was the control group. Precisely 0.915 g metronidazole disodium phosphate injection (Tongzhen Pharmaceutical Co., Shan Xi Province, P. R. China) or 25% metronidazole glucose solution was added to 100 mL 0.9% normal saline. After anesthetizing the patients in group A, 60 to 80 mL of the solution was injected into the subcutaneous tissue and muscle. The control group B was given intravenous injection of metronidazole disodium phosphate and cephazolin postoperatively.RESULTSIn the 119 cases in group A, the rate of incision infection was 0.8%. By contrast, the rate of infection among the 120 cases in group B was 11.6%. The statistical analysis (chi square) was significant, with P < 0.001 showing that preincisional or intraincisional infiltration with metronidazole was effective.

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Anaerobic bacterial infection	CN	-	-

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