Recent advances in anti-infective drug discovery最新文献

Introduction: Dandruff and Seborrheic Dermatitis (SD) are similar skin conditions with different degrees ofseverity. Since the current therapies cannot remove dandruff efficiently, herbal extracts with better effectiveness and fewer side effects are used in the pharmaceutical and cosmetic industries. Due to the adverse effects of chemical drugs, the use of natural products and traditional medicine has significantly increased over the past few decades. Therefore, in this review, we reported the herbs used as anti-dandruff agents in traditional medicine worldwide.

Methods: The review was conducted on the literature available on the medicinal utility of certain plants as anti-dandruff agents using PubMed and Google Scholar and the following search terms: Dandruff and plants or medicinal plant and dandruff treatment, and essential oil and dandruff.

Results: Since the current therapies cannotefficiently remove dandruff, herbal extracts with better effectiveness and fewer side effects are used in the pharmaceutical and cosmetic industries. Nowadays, there are numerous different types of herbal antidandruff shampoos. They are effective and safe without the side effects of chemical agents. Recently, herbal medicine has attracted a great deal of scientific attention. Clinical evidence on the therapeutic effects of herbal products has resulted in the study of far more herbs for their therapeutic roles.

Conclusion: Herbal therapy plays a significant role in the development of favorable therapeutics, either alone or in combination with conventional antibiotics. However, the major challenges in this regard include finding compounds with satisfactorily lower MICs, low toxicity, and high bioavailability for effective and safe use in humans and animals.

Introduction: Metallo-β-lactamases (MBLs) play a major role in the resistance of Pseudomonas aeruginosa to carbapenems. We investigated the antibiotic susceptibility patterns and frequency of MBLs genes (bla_IMP and bla_SPM) in carbapenem-resistant P. aeruginosa clinical isolates in Sari, Iran.

Materials and methods: The isolates were identified using standard microbiological tests, and their antibiotic susceptibility pattern was determined by the disk agar diffusion method according CLSI criteria. Phenotypic identification of MBL-producing strains assessed by the combined disk test (CDT). Then, polymerase chain reaction (PCR) was used to detect the presence of bla_IMP and bla_SPM genes.

Results: The highest and lowest levels of antibiotic resistance were observed against gentamicin (40%) and piperacillin-tazobactam (13%), respectively. Besides, 40 isolates (40%) had the multi-drug resistant (MDR) phenotype, while 5 (12.5%) MDR isolates were resistant to all antibiotics tested. The results of the CDT showed that among 43 carbapenem non-susceptible clinical isolates of P. aeruginosa, 33 (76.74%) isolates were MBL-producing strains. Also, the frequency of the bla_IMP gene among 43 carbapenem non susceptible isolates was determined to be 6.97%, while none of these isolates carried the bla_SPM gene.

Conclusion: Due to the high prevalence of carbapenem-resistant and MDR P. aeruginosa in this study, routine antibiotic susceptibility testing and phenotypic identification of carbapenemase production by this bacterium are necessary for the proper selection of antibiotics.

Background: Acute gastroenteritis is a common infectious disease with a high rate of morbidity and mortality in children below five years of age. Appropriate empirical treatment is therefore vital for reducing the incidence of the disease.

Objective: This study aimed at determining the trends in the empirical treatment of hospitalized children with acute gastroenteritis.

Methods: The study involved the data analysis of 88 medical folders of children who were diagnosed with gastroenteritis from January to February 2020 (a period of gastroenteritis yearly outbreak) in Mile 4 Hospital Abakaliki, Ebonyi State, Nigeria. Socio-demographic data and administered antibiotics data were collected.

Results: Out of the 88 children, a total of 54 (61%) children were males, while 34 (39%) were females. The ages of the children ranged between 1-51 months, while the mean age was seen at 14 months. About 58 (66%) were diagnosed with acute gastroenteritis alone, with children aged 7-12 months recording higher numbers [25 (28%)]. Severe dehydration was seen as the most common morbidity of children with acute gastroenteritis. The guardians/parents of these children stayed at home for an average of 3 days (1-6 days) before visiting the hospital. The children were treated for an average of 5 days (2-9 days) in the hospital. The most singly used antibiotics was ciprofloxacin [31 (35%)] followed by a combination of ciprofloxacin and ceftriaxone [21 (24%)]. About 12 (14%) of the children were treated using a single dose of the antimalarial drug while 10 (11%) were treated in double combination therapy. The lowest duration in hospitalization (4 days) was seen in the use of a single dose regimen, while the highest hospitalization time (6 days) was seen in the use of a triple dose regimen.

Conclusion: The best empirical treatment of acute gastroenteritis may involve the use of ciprofloxacin alone and its combination with ceftriaxone. The severity of gastroenteritis may also be exacerbated with malaria.

Background: The prevalence and scope of dermatological illness differ from region to region. Based upon type and severity, the conditions may vary from superficial to deep systemic skin infections. Niacinamide, an amide analog of vitamin B3 which was conventionally utilized as a food supplement, is now explored for the management of skin disorders. Being a powerhouse on its own, it is not stored inside the body naturally and has to be acquired from external sources. Areas Covered: This review is an attempt to disclose the physiology, pharmacology, and highlight the dermatological potentials of niacinamide, discussing its pharmacological mechanisms, varied commercially available treatments, and novel approaches, i.e., in research and patented formulations.

Results: Niacinamide has been verified in treating almost every skin disorder, viz. aging, hyperpigmentation, acne, psoriasis, pruritus, dermatitis, fungal infections, epidermal melasma, non-melanoma skin cancer, etc. It has been reported to possess numerous properties, for instance, anti-inflammatory, antimicrobial, antioxidant, antipruritic, and anticancer, which makes it an ideal ingredient for varied dermal therapies. Long term use of niacinamide, regardless of the skin type, paves the way for new skin cells, making skin healthier, brighter, and hydrated.

Conclusion: Niacinamide possesses a variety of positive characteristics in the field of dermatology. Novel approaches are warranted over current treatments which could bypass the above shortcomings and form an effective and stable system. Hence, niacinamide has the potential to become an individual and a productive component with wide future scope.

The authors wish to add words "Research Scholar" and "Research Supervisor" to their affiliations [1]. The original article can be found online at https://doi.org/10.2174/1574891X15999201110212725 The corrected affiliation is: 1Department of Pharmaceutics, Rayat-Bahra College of Pharmacy, Hoshiarpur, Punjab 146001, India; 2Faculty of Pharma-ceutical Sciences, Department of Pharmaceutics, PCTE Group of Institutes, Ludhiana, Punjab 142021, India; 3Research Scholar, I.K. Gujral Punjab Technical University, Jalandhar-Punjab 144601, India; 4Research Supervisor, I.K. Gujral Punjab Technical University, Jalandhar-Punjab 144601, India.

Background: Trichomonas vaginalis (TV), Mycoplasma genitalium (MG) and Ureaplasma urealyticum (UU) are common sexually transmitted infections (STIs) that are diagnosed in infertile couples (cps). In cases with their simultaneous presence in a patient (mixed STI, MSTIs), treatment is complicated by the different sensitivity of microorganisms to antibacterial drugs. Moreover, in cases of complicated infections, the empirical treatment should be started before obtaining the results of drug susceptibilities.

Objective: The objective of the current study is to find the effective and well-tolerated combination of drugs for the empirical antibacterial treatment of mixed STIs presented by TV, MG and UU in infertile couples. We also aimed to establish the influence of mixed STIs on semen quality.

Methods: Our prospective study included 154 infertile couples (308 patients) with confirmed symptomatic MSTIs in one of the couples caused by the simultaneous presence of TV, MG and UU. All couples were randomized on three groups for empirical treatment: Group 1 (n=49 cps, 98 pts) who were treated by initial prescribing of anti-trichomoniasis drug Secnidazole, 2.0 g po followed by Azythromycin 500 mg on day 1 continuing by 250 mg on days 2-7; Group 2 (n=52 cps, 104 pts: Secnidazole, 2.0 g po followed by Josamycin 1000 mg bid for 12 days); Group 3 (n=53 cps, 106 pts: Secnidazole, 2.0 g po followed by Moxifloxacin 400 mg once daily for 12 days). The endpoints were clinical and microbiological cure rates as well as the frequency of side-effects in analyzed groups. We determined the basic parameters of the spermogram and Deoxyribonucleic acid (DNA) fragmentation levels in 59 patients with MSTIs before and at the 3rd, 6th and 9th month after pathogens eradication comparing them with results in 63 healthy sperm donors.

Results: After the treatment, clinical cure rates in analyzed groups were 82.6% (Group 1) vs. 96.1% (Group 2) vs. 92.3% (Group 3). Microbiological cure rates (UU+MG) were 73.9% vs. 97.1% vs. 84.5% correspondingly (p<0.05). TV microbiological cure rates were 97.8% vs. 98.0% vs. 96.1% (p>0.05). Side-effects were registered in 28.6% vs. 12.5% vs. 18.9% cases correspondingly (p<0.05). In MSTIs patients, we registered the increasing DNA fragmentation rates, leucocytes count and decreasing semen volume, motility, vitality, sperm concentration, total spermatozoa number and number of spermatozoa with normal morphology. At the 6th month after complete pathogens eradication, these parameters approached normal values.

Conclusion: At the present time, the combination of Secnidazole+Josamycin can be considered the most effective and well-tolerated for the empirical treatment in patients with MSTIs presented by TV, MG and UU. Complete eradication of these MSTIs in males improves their semen parameters.

Background: In the past few centuries, a widespread increase in antimicrobial resistance has been observed among Klebsiella species. The antibiotic- resistant strains of the genus Klebsiella are becoming a serious threat in clinical settings due to their involvement in severe invasive and non-invasive infections. The emergence of resistance among these strains is associated with their strong enzymatic activity against several broad-spectrum antibiotics. These enzymes include beta-lactamases, extended-spectrum beta-lactamases (ESBL), AmpC beta-lactamases, and carbapenemases. These resistance enzymes are capable of hydrolyzing various broad-spectrum drugs like extended-spectrum cephalosporin and carbapenems.

Objective: The present study was conducted to determine the emerging resistance among Klebsiella strains by identifying the production of carbapenemase enzyme phenotypically and the frequency of the NDM resistance gene by a polymerase chain reaction.

Methods: In this study, 236 Gram-negative isolates from different clinical laboratories were identified. Out of which, 125 isolates were found as Klebsiella species by using standard microbiological techniques. Minimum inhibitory concentrations (MIC) were determined using eight representative antibiotics by the Macro broth dilution method. Phenotypic detection of carbapenemase producing Klebsiella species was performed by Modified Hodge Test. Phenotypic findings were then checked and compared with genotypic results obtained by using the Polymerase chain reaction (PCR) for the detection of resistance genes responsible for the production of carbapenemase.

Results: In this study, carbapenemase production was found only in 6 (5%) Klebsiella isolates by using the phenotypic method; however, 3 isolates out of 125 were screened positive for the gene NDM-1.

Conclusion: Since we are considering carbapenems as the last therapeutic option for treating infections, mainly caused by Gram-negative isolates, the prevailing resistance against this drug is widely disseminating. It is better to evaluate the antibiotic susceptibility, phenotypic screening as well genotypic screening (where possible) for implementing strict antibiotic control policies in health care settings, hospitals, laboratories, etc.

Background: Dermatological disorders are cutaneous infirmities which are frequently occurring and increasing at an alarming rate. These range from mild itching/redness (dermatitis) to fatal skin cancers and has posed a major health concern. Azadirachta indica A. Juss (commonly known as neem), a member of Meliaceae family, is an Indian medicinal plant which has been known for its health promoting effects since ancient times.

Objective: The review highlights the traditional practices, pharmacological aspects, and formulatory approach of neem for the treatment of dermatological disorders. Further, recent patents and novel delivery systems (developed and in pipeline) improving skin delivery and therapeutic profile of neem are discussed.

Results: Neem is a traditional medicinal plant that has been employed for the prevention and treatment of numerous ailments covering systemic and topical disorders. Scientific studies have validated the traditional claims of neem and attributed these health benefits to the presence of more than 300 structurally diverse and complex compounds. It possesses anti-inflammatory, antibacterial, analgesic, antiviral, antifungal, immunomodulatory and antioxidant activities which substantiate its use as skin therapy. Various novel formulations and associated patents that improved the permeability of neem based products across skin could be found in literature.

Conclusion: Critical appraisal of available literature revealed that neem possesses anti-microbial, anti-inflammatory, antioxidant and antiseptic properties. Thus it has the potential to be developed as a single effective therapy for the management of multimodal skin disorders. Further, pharmaceutical tailoring of neem by implication of novel carriers could enhance its penetrability across skin.