Combined vaginal administration of nystatin, diiodohydroxyquin, and benzalkonium chloride versus oral metronidazole for the treatment of bacterial vaginosis.

OBJECTIVE: To compare combined vaginal administration of nystatin, diiodohydroxyquin, and benzalkonium chloride versus oral metronidazole for the treatment of bacterial vaginosis (BV). METHODS: A randomized controlled trial was conducted among women diagnosed with BV using the Amsel criteria (n=90) at a university hospital in Khon Kaen, Thailand, between June 27, 2017, and April 30, 2018. The oral metronidazole group (n=44) received 400 mg of metronidazole, administered three times per day. The combined vaginal tablet group (n=46) received a vaginal suppository once daily, which comprised nystatin (100 000 U), diiodohydroxyquin (100 mg), and benzalkonium chloride (7 mg). Treatment was administered for 7 days in both groups. Follow-up visits at 14 and 42 days assessed treatment outcomes and adverse effects. RESULTS: Remission of BV occurred among 41 (93%) women in the oral metronidazole group and 39 (85%) women in the combined vaginal tablet group. The adjusted relative risk was 0.92 (95% confidence interval 0.80-1.06). The rate of nausea and/or vomiting was significantly higher in the oral metronidazole group than that in the combined vaginal tablet group. CONCLUSION: Treatment efficacy of the combined vaginal tablet versus oral metronidazole was equivalent. CLINICAL TRIAL REGISTRATION: TCTR20170627001 (www.clinicaltrials.in.th).

Identification and Characterization of the Human Cytosolic Sulfotransferases Mediating the Sulfation of Clioquinol and Iodoquinol.

OBJECTIVE: The aim of the current study was to identify the human cytosolic sulfotransferases (SULTs) that are capable of sulfating clioquinol and iodoquinol, and to verify the presence of clioquinol/ iodoquinol-sulfating activity in human organ homogenates and cultured cells. METHOD: An established sulfotransferase assay was employed to analyze clioquinol/iodoquinolsulfating activity of thirteen known human SULTs, as well as cytosols of human kidney, liver, lung, and small intestine. Metabolic labeling with [35S]sulfate in the presence of different concentrations of clioquinol/iodoquinol was performed using cultured HepG2 human hepatoma cells and Caco-2 human colon carcinoma cells. RESULTS: A systematic analysis revealed that six of the thirteen known human SULTs, SULT1A1 SULT1A2, SULTA3, SULT1B1, SULT1C4, and SULT1E1 showed considerable clioquinol/ iodoquinol-sulfating activity. Kinetic parameters of the sulfation of clioquinol and iodoquinol by three SULTs, SULT1A1, SULT1A3, and SULT1C4, that showed the strongest clioquinol/iodoquinolsulfating activity were determined. Moreover, clioquinol/iodoquinol-sulfating activity was detected in the cytosol fractions of human liver, lung, kidney, and small intestine. Cultured HepG2 and Caco-2 cells were shown to be capable of sulfating clioquinol/iodoquinol under metabolic conditions. CONCLUSION: Collectively, these results provided a molecular basis underling the metabolism of clioquinol and iodoquinol through sulfation.

A small organic compound enhances the religation reaction of human topoisomerase I and identifies crucial elements for the religation mechanism.

The different steps of the human Top1 (topoisomerase I) catalytic cycle have been analysed in the presence of a pentacyclic-diquinoid synthetic compound. The experiments indicate that it efficiently inhibits the cleavage step of the enzyme reaction, fitting well into the catalytic site. Surprisingly the compound, when incubated with the binary topoisomerase-DNA cleaved complex, helps the enzyme to remove itself from the cleaved DNA and close the DNA gap, increasing the religation rate. The compound also induces the religation of the stalled enzyme-CPT (camptothecin)-DNA ternary complex. Analysis of the molecule docked over the binary complex, together with its chemical properties, suggests that the religation enhancement is due to the presence on the compound of two oxygen atoms that act as hydrogen acceptors. This property facilitates the deprotonation of the 5' DNA end, suggesting that this is the limiting step in the topoisomerase religation mechanism.

Antimicrobial activity of iodoquinol 1%-hydrocortisone acetate 2% gel against ciclopirox and clotrimazole.

Commercially available topical formulations consisting of iodoquinol 1%-hydrocortisone acetate 2%, ciclopirox 0.77%, and clotrimazole 1%-betamethasone dipropionate 0.5% were assessed for their antimicrobial activity against cultures of Micrococcus luteus, Propionibacterium acnes, methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa, Corynebacterium aquaticum, Trichophyton mentagrophytes, Malassezia furfur, Microsporum canis, Candida albicans, Trichophyton rubrum, or Epidermophyton floccosum. At 1 and 5 minutes following inoculation into suspensions of each product, aliquots were removed, serially diluted, and plated onto appropriate agar to determine the log reduction in colony-forming units (CFUs) for each organism. Iodoquinol 1% produced the broadest and greatest antimicrobial activity as measured by a 3-log reduction of CFU, active against all microbes tested following incubation times of 1 or 5 minutes, except M luteus. By contrast, ciclopirox 0.77% and clotrimazole 1% showed activity against P aeruginosa and T rubrum, with ciclopirox also killing M luteus, P acnes, M canis, C albicans, and E floccosum at 5 minutes. Iodoquinol 1%-hydrocortisone acetate 2% also was the only product that showed effective antibacterial reduction of MRSA at 1 minute.

Eradication of amebiasis in a large institution for adults with mental retardation in Taiwan.

OBJECTIVE: Investigation of a program to eradicate amebiasis using consecutive intensive mass screenings followed by medication in a large institute for adults with mental retardation in Taiwan. DESIGN: Prospective cohort study, with 3 years of follow-up. SETTING: A large, 450-bed institution for adults with mental retardation located in southern Taiwan. PARTICIPANTS: All 443 adults with mental retardation in the institution, who have various motor and/or mental handicaps, were included in this study. INTERVENTIONS: A total of 7 consecutive intensive mass screenings for amebiasis for all residents (performed in March, August and November 2001, March and August 2002, January 2003, and May 2004). Infected patients were treated using the standard protocol of the Center for Disease Control of Taiwan. RESULTS: Enzyme immunoassay testing was used for the amebiasis screening, with the rapid detection of the specific antigen for Entamoeba histolytica in human fecal specimens confirmed by microscopic examination. The serial prevalence and cumulative incidence were then calculated. The prevalence of amebic infection declined in serial screenings, but new infections and reinfections were detected in 5 of 6 follow-up screenings. The prevalence was 10.8% at the beginning of the program and then gradually reduced, falling to 6.3%, 3.6%, 2.7%, 3.4%, and 2.2%. Finally, no more positive cases were identified in the last screening (May 2004). The cumulative incidence rate stabilized at around 40% by the fifth screening. Of the 179 infected patients, 120 had primary infections, with 59 cases of multiple amebic infections. CONCLUSIONS: Active surveillance with intensive mass screening is an effective method of identifying asymptomatic and latent cases of amebiasis in areas where it is endemic, such as an institution for adults with mental retardation.

Effects of oral administration of zinc and diiodohydroxyquinolein on plasma zinc levels of uremic patients.

Patients with chronic renal failure often have low plasma zinc (Zn) levels. Some factors that may account for abnormal Zn metabolism in these patients are low dietary Zn intake, a specific Zn transport defect, or absence of intestinal Zn ligand. In this study Zn supplementation and a Zn-chelating drug, diiodohydroxyquinolein (DQ), were used to assess the effects of Zn intake and Zn transporters on Zn plasma levels in patients with chronic renal failure. To meet this objective, 20 uremic patients were randomly assigned to one of the following groups of treatment: group 1 received placebo; group 2 Zn sulfate (100 mg/day p.o.), group 3 DQ (80 mg/day p.o.), and group 4 received Zn sulfate plus DQ at the same dosages as in groups 2 and 3. The Zn plasma levels were measured in venous samples, before and after 1 and 2 weeks of treatment, by atomic absorption spectrophotometry. The Zn plasma levels increased in group 2 patients from 8 +/- 0.2 to 10 +/- 0.4 and 11 +/- 0.9 mumol/l by the end of the 1st and 2nd weeks of treatment, respectively. In group 4 patients, the Zn plasma levels increased even more: from 9 +/- 0.1 to 14 +/- 1.6 and 13 +/- 2.1 mumol/l respectively. The plasma Zn concentration of group 1 and 3 patients remained at basal levels. These results show that DQ, when given along with Zn sulfate supplements, causes a greater increase in plasma Zn levels than that caused by either drug given alone.

Tratamiento simplificado de la amebiasis intestinal con diyodohidroxiquinoleína en niños / A simplified treatment of intestinal amebiasis in children with diiodohydroxyquinolein

Se trataron con diyodohidroxiquinoleina 53 niños de ambos sexos, en edad comprendida entre cinco y 17 años, atendidos en la consulta externa del servicio de parasitología del Instituto Nacional de Pediatía, en los cuales se diagnosticó amebiasis intestinal no invasiva en fase clínica y por exámenes de laboratorio (CPS) Faust). El fármaco se administró a razón de 30 mg/kg/dpia 10 días. Hubo curación en el 98.1% sólo dos pacientes refirieron efectos advrsos atribuidos al medicamento, uno presentó diarrea y otro náusea. Los resultados obtenidos permiten recomendar el uso de diyodohidroxiquinoleína en el tratamiento de la amebiasis intestinal no invasiva en niños con un esquema más corto que el convencional, que disminuye la presentación de efectos adversos y abatimiento del costo

Bio-antimutagenic effect of L-cysteine on diiodohydroxyquinoline-induced micronuclei in Swiss mice.

The mutagenic potential of diiodohydroxyquinoline (DIHQ), a common anti-amebic drug, was tested using the in vivo micronucleus test in Swiss mice following oral administration. It was found to be mutagenic in a dose-dependent manner. Using the same model system, the bio-antimutagenic effect of the sulfhydryl compound L-cysteine against DIHQ was established.

[Treatment of pityriasis alba with a combination of coal tar, diiodohydroxyquinolin and hydrocortisone]. / Tratammiento de la pityriasis alba con la asociación de alquitrán de hulla, diyodohidroxiquinoleina e hidrocortisona.

Pityriasis Alba, a dermatosis whose significance is basically cosmetic, is extremely common and so benign that the majority of patients-dark skinned children and young people do not consult a physician. Nevertheless due to its high incidence and chronicity a large number of patients eventually seek relief. The various treatments currently employed based on a mistaken concept of its etiology are ineffective, though the dermatosis disappears spontaneously after some time. The use of cream containing 2% coal tar., 1% diiodohydroxyquinolin and 0.5% hydrocortisone applied 3 times a day for one month on 29 patients in a double blind trial compared with on the contralateral region, proved to have acceptable results, with a highly significant difference compared with the placebo (P less than 0,0005).