Antifungal

A study of ancient literature indicates that diabetes was fairly well known and well conceived as an entity in India. Plant-based drugs have been used against various diseases since a long time. The nature has provided abundant plant wealth for all the living creatures, which possess medicinal virtues. The essential values of some plants have long been published, but a large number of them have remained unexplored to date. Therefore, there is a necessity to explore their uses and to conduct Pharmacognostic and pharmacological studies to ascertain their therapeutic properties. In fact, nowadays, diabetes is a global problem. Tridax procumbens, is a weed extensively used in traditional medicine as anticoagulant, antifungal and insect repellent. Water extract of leaf and flower contained more proteins when compared to its methanolic counterpart. The same was observed in case of total free phenol present wherein among the methanolic extracts, leaf showed good result when compared to flower. Hydroxyl free radical scavenging assay is an assay to determine the antioxidant property of the sample.

The present review highlights human vagina as a valuable route of drug delivery due to its large permeation area, rich vascularization, avoidance of first pass metabolism and relatively low enzymatic activity designed for achieving both local and systemic applications. Vagina is the best route used for administration of drugs like antifungal, contraceptives steroids, peptides and antifungal drugs. The rate and extent of drug absorption through vaginal route may fluctuate depending upon vaginal physiology, age of patients, stage of menstrual cycle, pathological conditions, and formulation factors. This route offers the ease of convenience, good blood supply, absence of GIT and hepatic first pass metabolism and permeability to large molecular weight drugs. Several drawbacks like personal hygiene, gender specificity, cultural sensitivity and local irritation need to be considered while the designing the vaginal formulation. Thus, purpose of this study is to provide the summary of advances undergone in the field of vaginal drug delivery currently available in the market and challenges associated with systemic delivery of drug via vaginal route. This review also highlights the benefits of vaginal route as drug delivery.

Butea monosperma and Butea superba belonging to the family, Fabaceae are most exploited medicinal plants by different tribal groups of Jharkhand. They are commonly found in the hills and jungles of Jharkhand and are used against arthritis, osteoarthritis, diarrhoea, dysentery, snakebite, male sexual debilities, sunstroke, leucorrhoea, anthelmintic and filariasis. Ethanolic exacts of the barks and flowers of both the plants did not exhibit significant antibacterial and antifungal activities. Phytochemical analyses revealed a total of 14 bioactive compounds from the barks and flowers of B. monosperma and B. superba.  Successful management of several diseases among the ethnic groups of Jharkhand, is indicative of presence of curative drugs without toxicity and side effects, and it could further the isolation and purification of active compounds contained in them.

1,4-Benzothiazine derivatives having variable antifungal activity against four species of fungus such as Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur  were selected to develop 2D and 3DQSAR models. The best 2DQSAR model was selected, having correlation coefficient r2 (0.8747) and cross validated squared correlation coefficient q2 (0.7145) with external predictive ability of pred_r2 (0.9658). 2DQSAR parameters are Quadrople1, SssCH2count, XA Average hydrophobicity, X Amost hydrophilic area and Polar surface area excluding P and S contributed in the model. The best 3DQSAR model having the correlation coefficient r2= 0.8635 was selected for further study. The model was further validated by means of crossed squared correlation coefficient q2 =0.7614 and pred_r2 =0.6654, which show that the model has good predictive ability and was developed by Forward SW-MLR. From QSAR model it concluded that the bulky substitution is require at para and meta position of Phenyl ring and less bulky substitution at ortho position of phenyl ring for antifungal activity.

Plants use multiple defense mechanisms in order to prevent entering of phytopathogenic microorganisms. In many plant species one of the most efficient responses to combat attacking microbes is the rapid synthesis of antimicrobial low molecular weight phytoalexins, for example, stilbenes produced by several plants may be a useful lead structure for the chemical synthesis of antimicrobials. In this study, a series of novel 2, 4, 5-trimethoxy stilbene derivatives have been synthesized via the Wittig reaction. The starting material 2, 4, 5- trimethoxy benzaldehyde (asaronaldehyde) was obtained from β-asarone of sweet flag oil. The key intermediate 2, 4, 5-trimethoxybenzyltriphenyl phosphonium chloride was prepared for the first time from the corresponding benzyl chloride. All the trans-stilbenes were characterized by HRMS, 1H and 13C NMR spectral analysis and tested in vitro for their fungicidal activity against two plant pathogenic fungi viz., Phytophthora capsici and Sclerotium rolfsii.

Synthesis of coumarin based random copolyester was prepared by the reaction of biscoumarin monomer 1 and anthroquinone3 with azeloyl chloride through interfacial polycondensation technique by using phase transfer catalyst. The chemical structure of the copolyester was investigated by Fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. Disc diffusion method was employed to investigate the antifungal activity of the synthesized copolyester.

A new class of heterocyclic compounds 1,3,4-thiadiazolo[3,2-a]-s-triazine have been synthesized as schiff’s base of 1,3,4- thiadiazole mix with ammonium acetate and various aromatic aldehyde treated in MW irradiation at 480 W. Reaction is based on microwave mediate multi-component reaction (MCRs). The structures of these compounds have been elucidated by spectral (IR, NMR & Mass) analysis. The title compounds were then evaluated for their in-vitro microbial activity against 2 gram –Ve bacteria (E.coli, K. pneumoniae), 2 gram +Ve bacteria (S.aerues, B.subtilis) and 1 fungal specie (A.niger). The some newly synthesized compounds have shown promising antimicrobial activity.

A series of [6-(p-substituted aminophenyl)-4-(p-substituted phenyl)—6H-1,3 thiazin-yl]-acetamides were synthesized via Claisen-Schmidt condensation. The titled compounds were characterized by IR, NMR analysis. The synthesized compounds were screened for their antibacterial and antifungal activity disc diffusion method. Among the synthesized compounds, T-2 was found to have a strong antibacterial and antifungal activity. Compounds T-1, T-3, T-4 and T-5 were found to have promising antimicrobial activity.

Nails are the hard and durable epidermal appendages structurally horny in nature. Nail plate is responsible for the penetration of the drug across it. There are number of formulations with antifungal agents viz. gels, creams and oral antifungals for the treatment of transungual infections. Among these entire nail lacquers is a new concept in treating nail infections. These nail lacquers are effective as monotherapy in treatment of superficial, distal and subungual diseases. The main purpose of topical nail preparations is to protect the nail plate and enhance beauty of nails. The medicated lacquer preparations are generally used in fungal diseases. Use of this system avoids oral toxicity of anti fungal drugs. The main challenge associated with developing nail lacquers for the treatment of nail disorders is to deliver the active concentration to the site of infection which is often under nail. Penetration of topical antifungal through the nail plate requires a vehicle that is specially formulated for transungual delivery. In this article we have tried to emphasize on need to develop nail lacquer for a promising antifungal treatment. This field could be explored for the treatment of Psoriasis24 and Onychomycosis.24

  The present study aimed at evaluating the in vitro antimicrobial activity of various extracts of the stem bark of Bauhinia variegata Linn. In the current study, the petroleum ether, chloroform, ethyl acetate, ethanol and aqueous extract of stem bark of B. variegata L. was tested against standard bacterial and fungal cultures. The test was performed by agar well diffusion method on nutrient agar media and Sabouraud’s dextrose media for bacterial and fungal cultures respectively. Among the solvent extracts, ethanolic extract was effective against all the tested bacteria and fungi. Ethanolic extract exhibited maximum inhibitory activity against Klebsiella. And the least activity was observed for Staphylococus aureus. For fungi ethanolic extract was more effective against Aspergillus fumigates. Key words: Antibacterial, Antifungal, Bauhinia variegata L.