In Vitro Evaluation of Biological Activities and Phytochemical Analysis of Different Solvent Extracts of Punica granatum L. (Pomegranate) Peels.

Antimicrobial resistance is a public health concern resulting in high rates of morbidity and mortality worldwide. Furthermore, a high incidence of food poisoning diseases besides harmful implications of applying synthetic food additives in food preservation necessitates fabrication of safe food preservatives. Additionally, damaging effects of free radicals on human health has been reported to be involved in the incidence of serious diseases, including cancer, diabetes and cardiovascular diseases; hence, finding safe sources of antioxidants is vital. Therefore, the present study was carried out to assess the antibacterial, antiradical and carcinopreventive efficacy of different solvent extracts of pomegranate peels. Agar disk diffusion assay revealed that Staphylococcus aureus, MRSA, E. coli and S. typhimurium were highly susceptible to methanolic fraction of Punica granatum L. peels recording inhibition zones of 23.7, 21.8, 15.6 and 14.7 mm respectively. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the methanolic fraction of Punica granatum L. peels against S. aureus were 0.125 and 0.250 mg/mL, respectively. In addition, the pomegranate acetonic and methanolic fractions revealed an impressive antiradical efficiency against DPPH (2,2-diphenyl-1-picrylhydrazyl) radical recording radical scavenging activity percentages of 86.9 and 79.4%, respectively. In this regard, the acetonic fraction of pomegranate peels revealed the highest anti-proliferative efficiency after 48 h incubation against MCF7 cancer cells recording IC50 of 8.15 µg/mL, while the methanolic extract was highly selective against transformed cancer cells compared to normal cell line recording selectivity index of 5.93. GC-MS results demonstrated that 5-Hydroxymethylfurfural was the main active component of methanolic and acetonic extracts of pomegranate peels recording relative percentages of 37.55 and 28.84% respectively. The study recommends application of pomegranate peel extracts in the biofabrication of safe food preservatives, antioxidants and carcinopreventive agents.

Anti-saprolegnia potency of some plant extracts against Saprolegnia diclina, the causative agent of saprolengiasis.

Saprolegnosis of fresh water fishes caused by Saprolegnia diclina often results in serious economic losses to fish hatcheries. Despite the proven efficiency of malachite green as a potential fungicide in prevention and control of fish saprolegnosis, there is a strong debate about its safety aspects in use since it was documented to be responsible for many carcinogenic and teratogenic attributes. Bioactivity of four ethanolic plant extracts were assessed to attain a natural alternative to the traditional fungicide currently used in saprolegnosis control. Ethanolic extracts of Punica granatum and Thymus vulgaris exhibited a potential efficacy in suppressing mycelial growth of S. diclina at concentration of 0.5 mg/ml while extracts of Nigella sativa and Zingiber officinales were not effective respectively. The extract of pomegranate showed the highest antifungal potency with minimum inhibitory concentration (MIC) of 200 ppm while thyme extract was less effective and recorded MIC of 400 ppm against S. diclina. The acute fish toxicity of the plant extracts indicated the low toxicity of P. granatum and T. vulgaris extracts as no fish mortalities were detected at aquaria containing 200, 400 and 800 ppm of plant extracts respectively. Considering the low toxicity of these plant extracts, it may be concluded that 200 and 400 ppm of pomegranate and thyme extracts which suppressed the mycelial growth of the S. diclina could be safely used for saprolegniasis control. Both of pomegranate and thyme extracts which proved to possess a potential antifungal activity can be considered as a natural alternative fungicides to control saprolegniasis avoiding carcinogenic malachite green application.

In vitro anticandidal potency of Syzygium aromaticum (clove) extracts against vaginal candidiasis.

BACKGROUND: Candida vaginitis is a global health hazard that increases morbidity among women of childbearing age. Recent studies have revealed a high incidence of drug-resistant Candida strains. Additionally, treating Candida vulvovaginitis during pregnancy is challenging as antifungal therapy is associated with fetal abnormalities. Hence, it is important to develop novel therapeutic strategies to treat vulvovaginal candidiasis. METHODS: In this study, we used the disc diffusion method to evaluate the anticandidal activity of different Syzygium aromaticum extracts (methanol, ethyl acetate, n-hexane, and diethyl ether) against C. albicans, C. glabrata, and C. tropicalis. Furthermore, gas chromatography-mass spectrometry (GC-MS) analysis of different S. aromaticum extracts was performed to determine active components exhibiting anticandidal activity. Cytotoxicity of different clove extracts against the HUH7 cell line was evaluated. RESULTS: The ethyl acetate extract exhibited the highest antifungal activity against C. albicans, C. glabrata, and C. tropicalis with inhibition zone diameters of 20.9, 14.9, and 30.7 mm, respectively. The minimum inhibitory concentration of the S. aromaticum ethyl acetate extract was 250 µg/disc against C. tropicalis, and 500 µg/disc against C. albicans and C. glabrata, while the minimum fungicidal concentration was 0.5 mg/disc against C. tropicalis and 1 mg/disc against the C. albicans and C. glabrata. GC-MS analysis of the ethyl acetate extract revealed the main bioactive compound as eugenol (58.88%), followed by eugenyl acetate (23.86%), trans-caryophyllene (14.44%), and α-humulene (1.88%). The cytotoxicity assay indicated that the diethyl ether extract demonstrated the lowest toxicological effect against the HUH7 cell line, with a relative IC50 of 62.43 µg/ml; the methanolic extract demonstrated a higher toxicity (IC50, 24.17 µg/ml). CONCLUSION: As the S. aromaticum extract exhibited high antifungal activity at low concentrations, it can be a potential source of natural antifungal drugs.

Decolorization and biotransformation pathway of textile dye by Cylindrocephalum aurelium.

Due to environmental concern, the research to date has tended to focus on how textile dye removal can be carried out in a greener manner. Therefore, this study aims to evaluate the decolorization and biotransformation pathway of Mordant Orange-1 (MO-1) by Cylindrocephalum aurelium RY06 (C. aurelium RY06). Decolorization study was conducted in a batch experiment including the investigation of the effects of physio-chemical parameters. Enzymatic activity of C. aurelium RY06 during the decolorization was also investigated. Moreover, transformation and biodegradation of MO-1 by C. aurelium RY06 were observed using the gas chromatography-mass spectrometry. Manganese peroxidase, lignin peroxidase, laccase, 1,2-dioxygenase, and 2,3-dioxygenase enzymes were detected during the decolorization. In general, the present work concluded that the MO-1 was successfully degraded by C. aurelium RY06 and transformed to be maleic acid and to be isophtalic acid.

Synthesis of novel benzopyran-connected pyrimidine and pyrazole derivatives via a green method using Cu(ii)-tyrosinase enzyme catalyst as potential larvicidal, antifeedant activities.

A series of benzopyran-connected pyrimidine (1a-g) and benzopyran-connected pyrazole (2a-i) derivatives were synthesized via Biginelli reaction using a green chemistry approach. Cu(ii)-tyrosinase was used as a catalyst in the synthesis of compounds 1a-g and 2a-ivia the Biginelli reaction. The as-synthesized compounds were characterized by IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analysis. The as-synthesized compounds were screened for larvicidal and antifeedant activities. The larvicidal activity was evaluated using the mosquito species Culex quinquefasciatus, and the antifeedant activity was evaluated using the fishes of Oreochromis mossambicus. The compounds 2a-i demonstrated lethal effects, killing 50% of second instar mosquito larvae when their LD50 values were 44.17, 34.96, 45.29, 45.28, 75.96, and 28.99 µg mL-1, respectively. Molecular docking studies were used for analysis based on the binding ability of an odorant binding protein (OBP) of Culex quinquefasciatus with compound 2h (binding energy = -6.12 kcal mol-1) and compound 1g (binding energy = -5.79 kcal mol-1). Therefore, the proposed target compounds were synthesized via a green method using Cu(ii)-enzyme as a catalyst to give high yield (94%). In biological screening, benzopyran-connected pyrazole (2h) was highly active compared with benzopyran-connected pyrimidine (1a-g) series in terms of larivicidal activity.