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1.
Anal Bioanal Chem ; 415(18): 4221-4232, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36002744

RESUMO

Humic acid-based carbon dots (HACDs) have excellent properties and are widely used in environmental detection, bioimaging, and optoelectronic materials. Herein, we investigated the structure-activity relationship between the morphology and optical properties of HACDs, and reported on a novel strategy for metronidazole (MNZ) and ornidazole (ONZ) sensing in multiple real samples. It was found that the average particle size decreased from 3.28 to 2.44 nm, optimal emission wavelength was blue-shifted from 500 to 440 nm, and the quantum yield (QY) improved from 5 to 23% with the temperature increasing from 110 to 400 °C. Under the oxidation of hydrogen peroxide (H2O2) and potassium permanganate (KMnO4), the UV-vis spectra of HACD aqueous solution showed time-dependent behavior, and the fluorescence emission of HACDs achieved spectrally tunable multi-color luminescence in the temporal dimension. The surface of HACDs contained a large number of hydroxyl (-OH) and carboxyl (-COOH) fluorophores, resulting in excellent pH sensing. Meanwhile, the synthesized HACDs revealed sensitive response to MNZ and ONZ with the limit of detection (LOD) of 60 nM and 50 nM in aqueous solutions, which had also been successfully applied in various actual samples such as lake water, honey, eggs, and milk with satisfactory results because of the inner filter effect (IFE). Our research is advantageous to enhance the potential applications of HACDs in advanced analytical systems.


Assuntos
Pontos Quânticos , Substâncias Húmicas , Pontos Quânticos/química , Carbono/química , Ornidazol/química , Metronidazol/química , Temperatura , Oxirredução , Concentração de Íons de Hidrogênio
2.
Wiad Lek ; 76(6): 1347-1358, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37463367

RESUMO

OBJECTIVE: The aim: To investigate the effect of application sorbent based on ornidazole with nanosilicon in experiment and clinic. PATIENTS AND METHODS: Materials and methods: In order to study the effectiveness of the Ornidasil application sorbent for the treatment of purulent wounds, we conducted an experimental study in rats. Also, we studied the effectiveness of the Ornidasil in the clinic for the treatment of patients with diabetic foot syndrome and to prevent the suppuration of postoperative wounds in patients with purulent peritonitis in toxic and terminal stages. RESULTS: Results: The formation of active substance complexes with hydroxylated matrices is due to hydrogen bonds between the oxygen atom of the silanol group of the silica surface and the hydrogen atom of the alcohol group of the ornidazole molecule. This promotes the gradual release of ornidazole from the surface of such a matrix into the wound exudate. Thus, on day 13, 9 experimental rats of group I healed completely, 11 rats had a small wound surface, complete healing occurred on day 15. We also investigated the effectiveness Ornidasil in the clinic. In the comparison group, postoperative wound suppuration occurred in 6 patients (31.6%), and in the main group - in 3 patients (12.5%). CONCLUSION: Conclusions: A study of the effectiveness Ornidasil in the complex treatment of Diabetic foot syndrome showed that in the experimental groups, wound healing occurred 1.6 -1.9 times faster. The use of polyurethane wound protector in combination with Ornidasil reduced the suppuration of postoperative wounds in patients of the main group by 2.5 times relative to patients in the comparison group.


Assuntos
Anti-Infecciosos , Pé Diabético , Ornidazol , Ratos , Animais , Pé Diabético/tratamento farmacológico , Ornidazol/farmacologia , Cicatrização , Supuração , Síndrome
3.
Environ Res ; 215(Pt 2): 114262, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36100108

RESUMO

Antibiotics (tinidazole (TNZ)) in wastewater, exhibit adverse effects on humans and ecosystem. The current study was aimed to synthesize photocatalysts mrGO/BiOCl and mrGO/BiOCl/Ag. mrGO was coupled with BiOCl by hydrothermal method and Ag was deposited over it. The synthesized mrGO/BiOCl and mrGO/BiOCl/Ag were confirmed by Pzc analysis (5.5 and 4.4 for mrGO/BiOCl and mrGO/BiOCl/Ag, respectively), surface area analysis (380 m2 g-1, 227.7 m2 g-1, 220 m2 g-1 for mrGO, mrGO/BiOCl and mrGO/BiOCl/Ag respectively), elemental analysis (Ag, O, Bi, Fe), surface morphology (rough ball like sphere of mrGO/BiOCl and cubic Ag nanoparticles in mrGO/BiOCl/Ag), functional groups and band gap (Eg) determination. The Eg was determined using Kubelka-Munk equation as 3.5 and 2.8 eV for mrGO/BiOCl and mrGO/BiOCl/Ag respectively. During the adsorption study, the best experimental conditions for various operating parameters such as pH (2), contact time (5 min for mrGO/BiOCl and 10 min for mrGO/BiOCl/Ag under UV irradiation), TNZ concentration (18 µgL-1) and catalyst dosage (0.001 g) were achieved. Kinetic study revealed that both composites followed pseudo second order kinetics (R2 = 0.9979 and 0.9986, respectively). Data of rGO/BiOCl was fitted to Freundlich adsorption model (R2 = 0.9687) and rGO/BiOCl/Ag fitted to Langmuir adsorption model (R2 = 0.9994). Moreover, thermodynamic parameters confirmed that a photodegradation phenomenon was spontaneous and exothermic. The results confirmed that rGO/BiOCl and rGO/BiOCl/Ag are appropriate composites for TNZ removal from the aqueous environment with removal efficiency of 97 and 24%, respectively.


Assuntos
Nanopartículas Metálicas , Prata , Adsorção , Antibacterianos , Bismuto , Ecossistema , Grafite , Humanos , Fenômenos Magnéticos , Tinidazol , Águas Residuárias , Água
4.
Gynecol Obstet Invest ; 87(5): 316-323, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36265450

RESUMO

OBJECTIVE: The aim of this study was to investigate the effectiveness of ornidazole in inhibiting the progression of endometriosis in a rat model. DESIGN: This was an in vivo experiment, including the ornidazole group (n = 16) and a control group (n = 14). Rats were provided with free access to water containing ornidazole (1 g/L) or drinking water only for 14 days. MATERIALS AND METHODS: Surgical induction of endometriosis was performed in Sprague Dawley rats via autologous endometrial transplantation. Rats were provided with free access to water containing ornidazole (1 g/L) or drinking water only for 14 days. Once the rats were euthanized (ornidazole group, n = 16; control group, n = 14), histological signatures and the volumes of endometriosis lesions were assessed. Cells positive for the inflammatory cytokines interleukin (IL)-1ß, IL-6, and tumor necrosis factor (TNF)-α were counted. Angiogenesis was identified by assessing vascular endothelial growth factor (VEGF) and microvessel density. RESULTS: The median lesion volume was lower in the ornidazole group (20.2 mm3; range, 5.7-53.3 mm3) than in the control group (81.3 mm3; range, 32.8-122.2 mm3; p = 0.007). Median IL-1ß cell counts were 5.3 (range, 4.5-6.4) for ornidazole and 11.7 (range, 9.4-15.4) for control (p < 0.001). Mean IL-6 cell counts were 5.6 ± 1.8 for ornidazole and 11.3 ± 4.1 for control (p < 0.001). Median TNF-α cell counts were 5.7 (range, 4.5-7.2) for ornidazole and 12.1 (range, 10.0-15.9) for control (p < 0.001). Median VEGF cell counts were 8.1 (range, 6.5-11.4) for ornidazole and 18.3 (range, 14.2-21.0) for control (p = 0.001). Median microvessel density values were 11.3/HPF (range, 7.7-21.8) for ornidazole and 28.7/HPF (range, 13.1-48.2) for control (p = 0.012). LIMITATIONS: This study is a short period and small sample size experiment. In this study, multiple drug concentrations were not used. We did not use in vitro models to assess the anti-inflammatory and antiangiogenic effects of ornidazole on endometriosis, and the specific anti-inflammatory and antiangiogenic mechanisms associated with ornidazole need to be further investigated. CONCLUSION: Ornidazole restricts the growth of endometriosis in rats, possibly by exerting anti-inflammatory and antiangiogenic effects.


Assuntos
Água Potável , Endometriose , Ornidazol , Animais , Feminino , Ratos , Anti-Inflamatórios/uso terapêutico , Modelos Animais de Doenças , Endometriose/patologia , Interleucina-6 , Ornidazol/uso terapêutico , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo
5.
Allergy ; 76(3): 842-852, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-32761620

RESUMO

BACKGROUND: Little is known about the diagnostic approaches for immediate hypersensitivity reactions (IHRs) due to 5-nitroimidazole antibiotics. The aim was to evaluate the usefulness of in vivo tests and basophil activation test (BAT) for the diagnosis of IHRs due to metronidazole and ornidazole and to determine possible cross-reactivity in between. METHODS: Forty-nine patients with a clear history of IHRs due to these drugs and 20 healthy subjects who were known to tolerate these drugs were included. Skin tests (STs) and single-blind placebo-controlled drug provocation tests (SBPCDPTs) were performed with both drugs whereas BAT was applied only with the culprit drug. RESULTS: The most and least common reaction types were urticaria/angioedema (34.7%) and anaphylaxis (14.3%), respectively. SBPCDPTs were positive in 15 out of 47 patients, and only 7 had positive STs. Sensitivity, specificity, positive predictive value (PPV), and negative predictive value (NPV) of STs for metronidazole/ornidazole were 33.3%/16.6%, 94.2%/97.3%, 60%/50%, and 84.6%/88.1%, respectively. BAT was positive in 12 out of 15 patients and negative in 10 control subjects, giving a sensitivity rate of 71.4% (CI, 29.0%-96.3%) for metronidazole and 83.3% (CI, 35.8%-99.5%) for ornidazole. The optimal concentration of both drugs for BAT was determined as 5 mg/mL. No cross-reactivity among two drugs was observed according to in vivo tests. CONCLUSIONS: Our study showed that SBPCDPT and BAT are both useful diagnostic tools for IHRs due to 5-nitroimidazole antibiotics and can be used as supplementary to each other. No cross-reactivity between metronidazole and ornidazole in IHRs exists.


Assuntos
Hipersensibilidade a Drogas , Hipersensibilidade Imediata , Ornidazol , Teste de Degranulação de Basófilos , Basófilos , Hipersensibilidade a Drogas/diagnóstico , Humanos , Hipersensibilidade Imediata/induzido quimicamente , Hipersensibilidade Imediata/diagnóstico , Metronidazol/efeitos adversos , Ornidazol/efeitos adversos , Método Simples-Cego , Testes Cutâneos
6.
Mikrochim Acta ; 188(11): 372, 2021 10 08.
Artigo em Inglês | MEDLINE | ID: mdl-34625823

RESUMO

The eco-friendly synthesis of metal oxides pn junction composite with high visible light absorption and its photoelectrochemical monitoring on antibiotics is reported. The In2O3-CuO pn heterojunction composite was successfully prepared by in-situ hydrothermal decoration of CuO on the prepared In2O3 using a simple reflux method. The obtained nanorods like In2O3-CuO pn heterojunction exhibited high conductivity with excellent stability for the facilitated photoelectrochemical detection of ornidazole (ONZ) that plays a role in aquatic toxicology. The photo-stability and optical characteristics of the In2O3-CuO heterojunction composite were analyzed through photocurrent and UV-visible studies. Mechanism of ONZ signaling has been proposed with appropriate band levels derived by Mott-Schottky analysis. An optimized In2O3-CuO heterojunction detects ONZ in the range 0.05-65.3 nM with 0.0092 nM as the limit of detection at - 0.45 V (vs. Ag/AgCl) working potential. The practical applicability of the sensor device was tested in chicken meat, human urine, and lake water samples containing ONZ. The recoveries of real samples were above 95% and results obtained were compared with electrochemical methods.


Assuntos
Cobre
7.
Zhonghua Nan Ke Xue ; 26(5): 446-451, 2020 May.
Artigo em Zh | MEDLINE | ID: mdl-33354955

RESUMO

OBJECTIVE: To explore the possible mechanism of Huanshao Capsules (HSC) protecting the reproductive function in rats with ornidazole-induced asthenozoospermia (AZS). METHODS: Forty SD male rats were randomly divided into four groups of equal number, blank control, AZS model control, HSC and L-carnitine (LC) intervention. The AZS model was established in the latter three groups of rats by intragastrical administration of ornidazole at 400 mg/kg/d for 28 days, and meanwhile the animals in the HSC and LC groups were treated by gavage of HSC at 0.31 g/kg/d and LC at 100 mg/kg/d, respectively. Then, all the rats were killed for examination of the LC content, sperm concentration, sperm motility and expression of OCTN2 mRNA in the epididymis and observation of the histopathological changes in the testis tissue. RESULTS: Compared with the AZS model controls, the rats in the HSC and LC groups showed significantly increased LC content (2 880.3 vs 6 366.5 and 6 934.7 mg/L, P < 0.01), sperm concentration (ï¼»34.58 ± 10.25ï¼½ vs ï¼»46.19 ± 14.23ï¼½ and ï¼»42.25 ± 6.11ï¼½ ×106/ml, P < 0.01), sperm motility (ï¼»42.59 ± 7.54ï¼½% vs ï¼»61.34 ± 7.98ï¼½% and ï¼»61.34 ± 7.98ï¼½%, P < 0.01) and expression of OCTN2 mRNA in the epididymis (26.07% vs 27.26% and 27.15%, P < 0.01). The animals of the HSC group exhibited a higher comparability than those of the LC group to the blank controls in the morphology, arrangement and activity of spermatogenic cells. CONCLUSIONS: HSC can protect the reproductive function and improve sperm concentration and motility in the model rats with ornidazole-induced AZS, which may be associated with its abilities of up-regulating the expression of OCTN2 mRNA and increasing the LC content in the epididymis.


Assuntos
Astenozoospermia , Medicamentos de Ervas Chinesas/uso terapêutico , Ornidazol , Animais , Astenozoospermia/induzido quimicamente , Astenozoospermia/tratamento farmacológico , Cápsulas , Carnitina/metabolismo , Epididimo/efeitos dos fármacos , Epididimo/metabolismo , Masculino , Ornidazol/toxicidade , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Membro 5 da Família 22 de Carreadores de Soluto/metabolismo , Contagem de Espermatozoides , Motilidade dos Espermatozoides , Espermatozoides
8.
BMC Womens Health ; 19(1): 121, 2019 10 21.
Artigo em Inglês | MEDLINE | ID: mdl-31638955

RESUMO

BACKGROUND: Bacterial vaginosis (BV) is one of the common vaginal infections among childbearing women. The usual treatment for BV is metronidazole; hence 30% of women have recurrence within 60 to 90 days after treatment. There are some studies which assessed the effect of secnidazole on BV. The aim of this systematic review was to investigate the effectiveness of secnidazole for treatment of BV. METHODS: The Cochrane Library, MEDLINE (PubMed), Scopus, and Web of Science (all databases from inception till October 28, 2018) were searched. Primary outcomes were clinical cure rate and microbiologic cure rate and the secondary outcomes were adverse events. Data was extracted from eligible studies by two review authors individually and analyzed by RevMan 5.3. RESULTS: Our search found six trials involving 1528 participants. Treatment with 2 g secnidazole could significantly reduce the risk of BV in patients with three or less episodes of BV in the last year by OR: 7.54 (95% CI, 3.89-14.60, p < 0.00001) and in patients with four or more episodes of BV in the last year (OR: 4.74, 95% CI: 1.51-14.84, p = 0.0.008). Secnidazole (2 g) could significantly increase the microbiologic cure rate in women with 3 or less episodes of BV in the last year (OR: 7.63, 95% CI: 2.30-25.33, p = 0.0009) but not in the women with 4 or more episodes of BV in the last year (OR: 20.17, 95% CI: 1.06-382.45, p = 0.05). The clinical cure rate, microbiological effect and the therapeutic cure rate of 2 g secnidazole was significantly more than that of 1 g secnidazole. The results showed that the clinical cure rate of 2 g secnidazole was not different from the following medications: metronidazole (500 mg bid for 5 days), secnidazole plus vaginal metronidazole, 2 g single dose of oral metronidazole and 2 g secnidazole plus vaginal ornidazole. CONCLUSION: This review showed that 2 g and 1 g secnidazole were better than placebo, however, 2 g secnidazole was more effective than 1 g. Secnidazole 2 g was not different from metronidazole (500 mg bid for 5 days), or from secnidazole plus vaginal metronidazole, or 2 g single dose of oral metronidazole or from 2 g secnidazole plus vaginal ornidazole.


Assuntos
Antibacterianos/administração & dosagem , Metronidazol/análogos & derivados , Vaginose Bacteriana/tratamento farmacológico , Administração Intravaginal , Administração Oral , Adulto , Quimioterapia Combinada , Feminino , Humanos , Metronidazol/administração & dosagem , Pessoa de Meia-Idade , Recidiva , Resultado do Tratamento
9.
Adv Exp Med Biol ; 1155: 507-520, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31468427

RESUMO

Asthenospermia has been considered as one of the crucial causes of male infertility, which was closely related to epididymal dysfunction. Lots of documents have revealed that taurine palys an important role in male reproduction, including antioxidation, membrane stabilization, stimulation of sexual hormone secretion and elevation of sperm quality. The objective of this study was to expose the effect of taurine on spermatozoa quality and function in ornidazole-induced asthenospermia rats. We found that taurine treatment could obviously recover the decline of cauda epididymal sperm count, viability and motility, and the elevation of sperm abnormality in asthenospermia animals. Spermatozoa acrosin, LDH-X, SDH and CCO activities of model rats also were notably increased by taurine administration. The present data indicated that taurine could raise spermatozoa quality and function by elevating mitochondrial energy metabolism. Notably, taurine supplementation markedly raised serum GnRH, LH and T levels in asthenospermia rays, suggesting taurine rescued asthenosperm by means of stimulating hypothalamic-pituitary-testicular axis secretion. We also found that concentrations of asthenospermia epididymal carnitine, SA, α-Glu and ACP, and mRNA expression levels of MMP7 and IDO2 were significantly rised by taurine administration, indicating taurine may protect epididymal epithelium structure, improve secretion activity, and maintain intraluminal microenvironment homeostasis. Finally, the present results showed taurine effectively increased cauda epididymal SOD, GSH and γ-GT levels in model rats, reduced ROS and MDA production, suggesting epididymal antioxidant ability of asthenospermia rats could be elevated by taurine treatment. To sum up, our results indicated that taurine can promote spermatozoa quality and function in ornidazole-induced asthenospermia rats by facilitating epididymal epithelium secretion and luminal microenvironment homeostasis.


Assuntos
Astenozoospermia/tratamento farmacológico , Ornidazol/efeitos adversos , Espermatozoides/efeitos dos fármacos , Taurina/farmacologia , Animais , Astenozoospermia/induzido quimicamente , Epididimo/efeitos dos fármacos , Epididimo/fisiopatologia , Masculino , Ratos , Motilidade dos Espermatozoides , Espermatozoides/citologia
10.
Pharm Dev Technol ; 24(7): 864-873, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31046546

RESUMO

Gingivitis is a common and mild form of periodontal disease and can be described as a limited inflammation of the gingiva. This study aims to develop and characterize rapid releasing mucoadhesive fibers containing ornidazole with electrospinning process for the treatment of gingivitis. Polyvinylpyrrolidone (PVP) was chosen as a polymer and used at different concentrations of 10%, 12.5%, and 15%. Scanning electron microscopy images showed that fiber diameters increased with increasing polymer concentrations. Tensile strength and elongation at break values of fibers increased with increasing PVP amount, whereas the loading of ornidazole into the fibers decreased these parameters. The contact angle values of all fibers were found to be 0° due to the hydrophilic nature of PVP. Ornidazole was released within 5 min and diffused from all of the fibers faster than that of gel and solution formulations. Electrospun ornidazole fibers were found efficient against Porphyromonas gingivalis in antimicrobial activity studies. The results demonstrated that ornidazole loaded fibers could be a potential drug delivery system for the treatment of gingivitis.


Assuntos
Anti-Infecciosos/administração & dosagem , Nanofibras/química , Ornidazol/administração & dosagem , Povidona/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacocinética , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Mucosa Bucal/metabolismo , Ornidazol/química , Ornidazol/farmacocinética , Ovinos , Solubilidade
11.
Pharm Dev Technol ; 24(1): 118-126, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29334299

RESUMO

A bilayered mucoadhesive buccal film containing a combination of ornidazole (OD) and dexamethasone sodium phosphate (DEX) was prepared using solvent casting to treat oral ulcers. Films were systematically evaluated in vitro to obtain the optimum formulation. The therapeutic effects of these films were investigated in the rabbit oral ulcer model and the in vivo release of OD and DEX in the human oral cavity was also evaluated. The backing layer contained ethyl cellulose and an optimal mucoadhesive layer containing both OD and DEX was produced. Films from the optimum formulation were 0.427 ± 0.015 mm thick, weighed 55.89 ± 0.79 mg, and had a surface pH of 6.34 ± 0.01. The drug content of the optimum formulation approximated the theoretical value with good uniformity (2.959 ± 0.106 mg/cm2 for OD and 0.877 ± 0.031 mg/cm2 for DEX). The formulation showed favorable swelling characteristics and both drugs were released at >95% after 4 h. Moreover, the compound film had a statistically significant effect on mucosal repair and reduced ulcer inflammation without stimulating the human oral mucosa. Cmax of OD in saliva was 37.04 µg/ml and that of DEX was 9.737 µg/ml. Given promising therapeutic effects, the compound film developed here could become a local drug delivery device for treating oral ulcers.


Assuntos
Dexametasona/análogos & derivados , Mucosa Bucal/metabolismo , Úlceras Orais/tratamento farmacológico , Ornidazol/administração & dosagem , Adesividade , Administração Bucal , Adulto , Animais , Antibacterianos/administração & dosagem , Antibacterianos/farmacologia , Celulose/análogos & derivados , Celulose/química , Química Farmacêutica/métodos , Dexametasona/administração & dosagem , Dexametasona/farmacologia , Modelos Animais de Doenças , Combinação de Medicamentos , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Feminino , Glucocorticoides/administração & dosagem , Glucocorticoides/farmacologia , Humanos , Masculino , Ornidazol/farmacologia , Coelhos , Suínos , Adulto Jovem
12.
Zhonghua Nan Ke Xue ; 25(12): 1113-1117, 2019 Dec.
Artigo em Zh | MEDLINE | ID: mdl-32251564

RESUMO

OBJECTIVE: To explore the protective effect of the Chinese medicinal prescription Linggui Fang (LGF) on the reproductive system of the ornidazole-induced asthenospermia (AS) rat and its possible action mechanisms. METHODS: Forty male SD rats weighing 200-230 g were equally randomized into four groups, blank control, AS model control, LGF treatment and L-carnitine (LC) intervention. The AS models were made in the latter three groups by intragastrical administration of ornidazole at 400 mg/kg. Meanwhile, the rats in the LGF group were treated intragastrically with LGF at 17.5 g/kg, those in the LC group with LC at 100 mg/kg, and the control animals with 0.5% sodium carboxymethylcellulose (CMC-Na), all once a day for 4 successive weeks. Then, all the rats were sacrificed for examination of the semen parameters, determination of the LC content and OCTN2 mRNA expression in the epididymis and observation of the histopathological changes in the testis. RESULTS: Compared with the AS model controls, the rats in the other groups showed significantly higher percentages of progressively motile sperm and total motile sperm (P < 0.01) as well as a higher LC content in the epididymis (P < 0.01), but no statistically significant difference in sperm concentration (P > 0.05). The expression of OCTN2 mRNA was remarkably upregulated in the LGF and LC groups in comparison with that in the AS model control (P < 0.05). Compared with the rats in the blank control group, the AS model controls exhibited markedly increased morphologically abnormal seminiferous tubules, irregularly arranged, with narrowed lumens and reduced numbers of sperm and sperm cells, as well as significantly increased hollow seminiferous tubules with deficient and disorderly arranged spermatogenic cells and partial epithelial degeneration and vacuolization. Those in the LGF and LC groups, however, manifested almost normal testicular histomorphology, with basically regular arrangement of different layers of seminiferous tubules. CONCLUSIONS: ①Ornidazole induces AS in rats by reducing the LC content in the epididymis, while LGF can improve the sperm motility and testicular morphology of the rats and upregulate the expression of OCTN2 mRNA in the epididymis by increasing the LC concentration.


Assuntos
Astenozoospermia/tratamento farmacológico , Carnitina/análise , Medicamentos de Ervas Chinesas/uso terapêutico , Animais , Astenozoospermia/induzido quimicamente , Epididimo/química , Epididimo/efeitos dos fármacos , Humanos , Masculino , Ornidazol , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Membro 5 da Família 22 de Carreadores de Soluto/metabolismo , Contagem de Espermatozoides , Motilidade dos Espermatozoides , Espermatozoides , Testículo/efeitos dos fármacos , Testículo/patologia
13.
Zhonghua Nan Ke Xue ; 24(4): 297-303, 2018 Apr.
Artigo em Zh | MEDLINE | ID: mdl-30168947

RESUMO

OBJECTIVE: To study the protective effect of lipoic acid (LA) on the spermatogenic function of the male rats with oligoasthenozoospermia induced by ornidazole (ORN). METHODS: Seventy male SD rats were equally randomized into groups A (solvent control: 1 ml 0.5% CMC-Na + 1 ml olive oil), B (low-dose ORN model: 400 mg/kg ORN suspension + 1 ml olive oil), C (low-dose ORN + low-dose LA treatment: 400 mg/kg ORN + 50 mg/kg LA), D (low-dose ORN + high-dose LA treatment: 400 mg/kg ORN + 100 mg/kg LA), E (high-dose ORN model: 800 mg/kg ORN suspension + 1 ml olive oil), F (high-dose ORN + low-dose LA treatment: 800 mg/kg ORN + 50 mg/kg LA), and G (high-dose ORN + high-dose LA treatment: 800 mg/kg ORN + 100 mg/kg LA), and treated respectively for 20 successive days. Then all the rats were sacrificed and the weights of the body, testis, epididymis and seminal vesicle obtained, followed by calculation of the organ index, determination of epididymal sperm concentration and motility, and observation of the histomorphological changes in the testis and epididymis by HE staining. RESULTS: Compared with group A, group E showed significantly decreased body weight (ï¼»117.67 ± 11.53ï¼½ vs ï¼»88.11 ± 12.65ï¼½ g, P < 0.01) and indexes of the testis (ï¼»1.06 ± 0.12ï¼½ vs ï¼»0.65 ± 0.13ï¼½ %, P < 0.01) and epididymis (ï¼»0.21 ± 0.03ï¼½ vs ï¼»0.17 ± 0.01ï¼½ %, P < 0.01). In comparison with group E, group F exhibited remarkable increases in the epididymal index (ï¼»0.17 ± 0.01ï¼½ vs ï¼»0.20 ± 0.02ï¼½ %, P < 0.01), and so did group G in the body weight (ï¼»88.11 ± 12.65ï¼½ vs ï¼»102.70 ± 16.10ï¼½ g, P < 0.05) and the indexes of the testis (ï¼»0.65 ± 0.13ï¼½ vs ï¼»0.95 ± 0.06ï¼½ %, P < 0.01) and epididymis (ï¼»0.17 ± 0.01ï¼½ vs ï¼»0.19 ± 0.02ï¼½ %, P < 0.05), but no obvious difference was observed in the index of seminal vesicle among different groups. Compared with group A, group B manifested significant decreases in sperm motility (ï¼»74.12 ± 8.73ï¼½ vs ï¼»40.25 ± 6.08ï¼½ %, P < 0.01), and so did group E in sperm count (ï¼»38.59 ± 6.40ï¼½ vs ï¼»18.67 ± 4.59ï¼½ ×105/100 mg, P < 0.01) and sperm motility (ï¼»74.12 ± 8.73ï¼½ vs ï¼»27.58 ± 8.43ï¼½ %, P < 0.01). Sperm motility was significantly lower in group B than in C and D (ï¼»40.25 ± 6.08ï¼½ vs ï¼»58.13 ± 7.62ï¼½ and ï¼»76.04 ± 8.44ï¼½%, P < 0.01), and so were sperm count and motility in group E than in F and G (ï¼»18.67 ± 4.59ï¼½ vs ï¼»25.63 ± 9.66ï¼½ and ï¼»29.92 ± 4.15ï¼½ ×105/100 mg, P < 0.05 and P < 0.01; ï¼»27.58 ± 8.43ï¼½ vs ï¼»36.56 ± 11.08ï¼½ and ï¼»45.05 ± 9.59ï¼½ %, P < 0.05 and P < 0.01). There were no obvious changes in the histomorphology of the testis and epididymis in groups A, B, C and D. Compared with group A, group E showed necrotic and exfoliated spermatogenic cells with unclear layers and disorderly arrangement in the seminiferous tubules and remarkably reduced sperm count with lots of noncellular components in the epididymal cavity, while groups F and G exhibited increased sperm count in the seminiferous tubules and epididymis lumen, also with exfoliation, unclear layers and disorderly arrangement of spermatogenic cells, but significantly better than in group E. CONCLUSIONS: LA can reduce ORN-induced damage to the spermatogenetic function of rats, improve sperm quality, and protect the reproductive system.


Assuntos
Antioxidantes/farmacologia , Astenozoospermia/tratamento farmacológico , Oligospermia/tratamento farmacológico , Espermatogênese/efeitos dos fármacos , Ácido Tióctico/farmacologia , Animais , Astenozoospermia/induzido quimicamente , Peso Corporal/efeitos dos fármacos , Epididimo/anatomia & histologia , Epididimo/efeitos dos fármacos , Masculino , Oligospermia/induzido quimicamente , Ornidazol , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Glândulas Seminais/anatomia & histologia , Glândulas Seminais/efeitos dos fármacos , Túbulos Seminíferos/anatomia & histologia , Túbulos Seminíferos/efeitos dos fármacos , Contagem de Espermatozoides , Motilidade dos Espermatozoides/efeitos dos fármacos , Espermatozoides/efeitos dos fármacos , Testículo/anatomia & histologia , Testículo/efeitos dos fármacos
14.
Biochem J ; 473(23): 4413-4426, 2016 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-27647935

RESUMO

Ornidazole of the 5-nitroimidazole drug family is used to treat protozoan and anaerobic bacterial infections via a mechanism that involves preactivation by reduction of the nitro group, and production of toxic derivatives and radicals. Metronidazole, another drug family member, has been suggested to affect photosynthesis by draining electrons from the electron carrier ferredoxin, thus inhibiting NADP+ reduction and stimulating radical and peroxide production. Here we show, however, that ornidazole inhibits photosynthesis via a different mechanism. While having a minute effect on the photosynthetic electron transport and oxygen photoreduction, ornidazole hinders the activity of two Calvin cycle enzymes, triose-phosphate isomerase (TPI) and glyceraldehyde-3-phosphate dehydrogenase (GAPDH). Modeling of ornidazole's interaction with ferredoxin of the protozoan Trichomonas suggests efficient electron tunneling from the iron-sulfur cluster to the nitro group of the drug. A similar docking site of ornidazole at the plant-type ferredoxin does not exist, and the best simulated alternative does not support such efficient tunneling. Notably, TPI was inhibited by ornidazole in the dark or when electron transport was blocked by dichloromethyl diphenylurea, indicating that this inhibition was unrelated to the electron transport machinery. Although TPI and GAPDH isoenzymes are involved in glycolysis and gluconeogenesis, ornidazole's effect on respiration of photoautotrophs is moderate, thus raising its value as an efficient inhibitor of photosynthesis. The scarcity of Calvin cycle inhibitors capable of penetrating cell membranes emphasizes on the value of ornidazole for studying the regulation of this cycle.


Assuntos
Bactérias Anaeróbias/efeitos dos fármacos , Ornidazol/farmacologia , Fotossíntese/efeitos dos fármacos , Cianobactérias/efeitos dos fármacos , Ferredoxinas/metabolismo , Gliceraldeído-3-Fosfato Desidrogenase (Fosforiladora)/metabolismo , Gliceraldeído-3-Fosfato Desidrogenases/metabolismo , Glicólise , Metronidazol/farmacologia , Modelos Biológicos , Synechocystis/efeitos dos fármacos , Trichomonas/efeitos dos fármacos , Trichomonas/metabolismo , Triose-Fosfato Isomerase/metabolismo
15.
Cutan Ocul Toxicol ; 36(3): 294-296, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27780370

RESUMO

BACKGROUND: Fixed drug eruption (FDE) is a special variant of drug reaction seen on skin or mucous membrane, and typically recurs at the same location. Ornidazole-induced FDE cases have been reported extremely rare. CASE: The 48-year-old female patient was diagnosed for ornidazole-induced fixed drug reaction on the sole. The patient's history revealed that the lesion occurred for the third time in the last 6 months and she was administered ornidazole tablet 3 times by the gynecologist for genitourinary tract infection. CONCLUSION: This report presents a case of fixed drug reaction located at the sole induced by ornidazole use and a literature review.


Assuntos
Antitricômonas/efeitos adversos , Toxidermias/etiologia , Ornidazol/efeitos adversos , Antitricômonas/uso terapêutico , Toxidermias/patologia , Feminino , Humanos , Pessoa de Meia-Idade , Ornidazol/uso terapêutico , Pele/efeitos dos fármacos , Pele/patologia , Infecções Urinárias/tratamento farmacológico
16.
Zhonghua Nan Ke Xue ; 23(3): 206-211, 2017 Mar.
Artigo em Zh | MEDLINE | ID: mdl-29706039

RESUMO

OBJECTIVE: To investigate the improving effect of astaxanthin (AST) on the sperm quality of rats with ornidazole (ORN)-induced oligoasthenozoospermiaand its action mechanism. METHODS: Forty adult male SD rats were equally randomized into groups A (solvent control), B (low-dose ORN ï¼»400 mg/(kg·d)]), C (high-dose ORN ï¼»800 mg/(kg·d)]), D (low-dose ORN ï¼»400 mg/(kg·d)] + AST ï¼»20 mg/(kg·d)]), and E (high-dose ORN ï¼»800 mg/(kg·d)] + AST ï¼»20 mg/(kg·d)]), all treated intragastrically for3 weeks.After treatment, the epididymal tails ononeside was taken for determination of sperm concentration and activity, and the epididymideson the other side harvested for measurement of the activities of GSH-Px, GR, CAT and SOD and the MDA contentin the homogenate. RESULTS: Compared with group A, sperm motilityin the epididymal tail andGSH-Px and SOD activities in theepididymiswere markedly decreased while the MDAcontent significantlyincreased in group B (P<0.05), spermmotility and concentrationin the epididymal tail, testisindex, and the activities of GSH-Px, GR, CAT and SOD in the epididymis were remarkably reduced while theMDA contentsignificantly increased in group C(P<0.05). In comparison with group B, group D showed markedly increased sperm motility (ï¼»45.3±8.7ï¼½% vs ï¼»66.3±8.9ï¼½%, P<0.05) in the epididymal tail and SOD activity in the epididymis (ï¼»116.7±25.3ï¼½ U/mg prot vs ï¼»146.1±23.8ï¼½ U/mg prot, P<0.05), decreased MDA content(ï¼»1.68±0.45ï¼½ nmol/mg prot vs ï¼»1.19±0.42ï¼½ nmol/mg prot, P<0.05).Compared with group C, group Eexhibited significant increases in the weight gained (ï¼»89.0±9.5ï¼½ vs ï¼»99.9±4.1ï¼½ %, P<0.05) and sperm motility (ï¼»17.9±3.5ï¼½% vs ï¼»27.3±5.3ï¼½ %, P<0.05) but a decrease in the content of MDA (ï¼»2.03±0.30ï¼½ nmol/mg prot vs ï¼»1.52±0.41ï¼½ nmol/mg prot, P<0.05). CONCLUSIONS: AST can improve spermquality in rats with ORN-inducedoligoasthenozoospermia, which may be associated with its enhancing effect on the antioxidant capacity of the epididymis.


Assuntos
Antioxidantes/farmacologia , Astenozoospermia/prevenção & controle , Epididimo/efeitos dos fármacos , Oligospermia/prevenção & controle , Substâncias Protetoras/farmacologia , Espermatozoides/efeitos dos fármacos , Animais , Epididimo/metabolismo , Masculino , Ornidazol , Estresse Oxidativo , Radiossensibilizantes , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Contagem de Espermatozoides , Motilidade dos Espermatozoides , Espermatozoides/metabolismo , Xantofilas/farmacologia
17.
J Sep Sci ; 39(18): 3488-97, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27433792

RESUMO

Two-way and three-way calibration models were applied to ultra high performance liquid chromatography with photodiode array data with coeluted peaks in the same wavelength and time regions for the simultaneous quantitation of ciprofloxacin and ornidazole in tablets. The chromatographic data cube (tensor) was obtained by recording chromatographic spectra of the standard and sample solutions containing ciprofloxacin and ornidazole with sulfadiazine as an internal standard as a function of time and wavelength. Parallel factor analysis and trilinear partial least squares were used as three-way calibrations for the decomposition of the tensor, whereas three-way unfolded partial least squares was applied as a two-way calibration to the unfolded dataset obtained from the data array of ultra high performance liquid chromatography with photodiode array detection. The validity and ability of two-way and three-way analysis methods were tested by analyzing validation samples: synthetic mixture, interday and intraday samples, and standard addition samples. Results obtained from two-way and three-way calibrations were compared to those provided by traditional ultra high performance liquid chromatography. The proposed methods, parallel factor analysis, trilinear partial least squares, unfolded partial least squares, and traditional ultra high performance liquid chromatography were successfully applied to the quantitative estimation of the solid dosage form containing ciprofloxacin and ornidazole.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Ciprofloxacina/análise , Ornidazol/análise , Calibragem , Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia Líquida de Alta Pressão/normas , Comprimidos/análise
18.
Urologiia ; (3 Suppl 3): 91-96, 2016 08.
Artigo em Russo | MEDLINE | ID: mdl-28247621

RESUMO

The article discusses the possible etiological factors in the development of chronic bacterial prostatitis. The authors presented a comparative long-term analysis of morbidity from non-viral sexually transmitted infections (STIs) in Russia. Against the background of general decline in STIs incidence, a significant percentage of them is made up by urogenital trichomoniasis. The findings substantiated the advantages of combination therapy (ornidazole and ofloxacin) for bacterial urinary tract infections.


Assuntos
Antibacterianos/uso terapêutico , Infecções Bacterianas/terapia , Prostatite/microbiologia , Prostatite/terapia , Adulto , Doença Crônica , Quimioterapia Combinada , Humanos , Masculino , Prostatite/epidemiologia , Federação Russa , Doenças Bacterianas Sexualmente Transmissíveis/epidemiologia
19.
Arch Med Sci ; 20(1): 189-195, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38414462

RESUMO

Introduction: Timely and effective treatments of pericoronitis are very important. We aimed to evaluate the role of ornidazole in the treatment of pericoronitis, to provide insights for clinical pericoronitis treatment. Material and methods: The PubMed, Clinical trials, EMBASE, Science Direct, Cochrane Library, China National Knowledge Infrastructure (CNKI), Weipu and Wanfang databases were searched to find randomized controlled trials (RCTs) of ornidazole in the treatment of pericoronitis from the establishment of the database to March 15, 2023. Review Manager 5.3 software was used for meta-analysis. Results: A total of 16 RCTs involving 2004 patients were included. The results of the meta-analysis showed that the effective rate of ornidazole treatment was significantly higher than that of the routine treatment group (RR = 1.22, 95% CI (1.15, 1.29), p < 0.001). Ornidazole treatment was beneficial to reduce the oral bacterial density (MD = -26.13, 95% CI (-32.08, -21.51)), time to pain disappearance (MD = -0.64, 95% CI (-0.92, -0.17)) and time to disappearance of redness and swelling of the teeth crown (MD = -1.45, 95% CI (-2.43, -1.01)) compared to the routine treatment (all p = 0.05). No publication bias was found by the funnel plots and Egger test (p = 0.206). Conclusions: Ornidazole is effective in the treatment of pericoronitis, with more advantages. Still, the effects and safety of ornidazole in the treatment of pericoronitis need to be evaluated by more high-quality RCTs with larger sample sizes.

20.
Cell Biochem Biophys ; 2024 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-38886281

RESUMO

BACKGROUND: Around the world, non-small cell lung cancer (NSCLC) is the leading cause of cancer-related deaths among all cancers. Despite advancements in new therapeutic approaches over the past few decades, the five-year survival rate still remains disappointing. The lack of effective anti-angiogenic and anti-migration drugs is the biggest obstacle to the treatment of metastatic lung cancer. Therefore, there is a need to develop new and effective therapeutic compounds targeting anti-angiogenic and anti-migration pathways for the treatment of lung cancer. Ornidazole is a nitroimidazole agent widely used in the treatment of parasitic infections such as trichomonas vaginalis, amebiasis and giardiasis. This study aimed to investigate the anti-proliferative, anti-angiogenic and anti-mitotic activities of the anti-parasitic drug Ornidazole in two human lung cancer cell lines (A549, H1299). METHODS: We determined the effects of Ornidazole, on cell viability, apoptosis, migration, angiogenesis and metastatic ability against NSCLC in lung cancer cell lines. Its action on the mRNA and protein expression levels of VEGFA, VEGFR2, NRP1, Casp9, Casp3, Bax, Bcl-2, PIK3CA, AKT, MTOR, PTEN and FOX3A was assessed. Furthermore, in this study the effects on cell migration, cell viability and proliferation was evaluated through wound healing, MTT and Crystal violet assays. RESULTS: This study demonstrated that Ornidazole effectively reduces cell viability and migration ability, inhibits angiogenesis and metastatic abilities in NSCLC cells. CONCLUSIONS: In conclusion, these results may shed light on the treatment of NSCLC, and we suggest the anti-parasitic drug Ornidazole as a new agent with potential anti-angiogenic and anti-mitotic activity by interfering with the molecular pathways that trigger tumor angiogenesis and migration.

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