Antidiabetic, antioxidant, and anti-obesity effects of phenylthio-ethyl benzoate derivatives, and molecular docking study regarding α-amylase enzyme.

In addition to their wide therapeutic application, benzoates and benzoic acid derivatives are the most commonly utilized food preservatives. The purpose of this study was to estimate the antioxidant, anti-diabetic, and anti-obesity activities of four 2-(phenylthio)-ethyl benzoate derivatives utilizing standard biomedical assays. The results revealed that the 2a compound has potent antidiabetic activity through the inhibition of α-amylase and α-glycosidase with IC50 doses of 3.57 ± 1.08 and 10.09 ± 0.70 µg/ml, respectively, compared with the positive control acarbose (IC50 = 6.47 and 44.79 µg/ml), respectively. In addition, by utilizing the ß-carotene linoleic acid and DPPH methods, the 2a compound showed the highest antioxidant activity compared with positive controls. Moreover, the 2a compound showed potential anti-lipase activity with an IC50 dose of 107.95 ± 1.88 µg/ml compared to orlistat (IC50 = 25.01 ± 0.78 µg/ml). A molecular docking study was used to understand the interactions between four derivatives of (2-(phenylthio)-ethyl benzoate with α-amylase binding pocket. The present study concludes that the 2a compound could be exploited for further antidiabetic, antioxidant, and anti-obesity preclinical and clinical tests and design suitable pharmaceutical forms to treat these global health problems.

Isolation, identification, and antimycotic activity of plumbagin from Plumbago europaea L. roots, leaves and stems.

Plumbago europaea L. is a plant utilized in Palestinian ethnomedicine for the treatment of various dermatological diseases. The current investigation was designed to isolate plumbagin from P. europaea leaves, roots and for the first time from the stems. Moreover, it aimed to evaluate the antimycotic activity against three human fungal pathogens causing dermatophytosis, also against an animal fungal pathogen. The qualitative analysis of plumbagin from the leaves, stems, and roots was conducted using HPLC and spectrophotometer techniques, while the structure of plumbagin was established utilizing Proton and Carbon-13 Nuclear Magnetic Resonance (NMR) and Infrared (IR) techniques. The entire plant constituents were determined by GC-MS. Moreover, the antimycotic activity against Ascosphaera apis, Microsporum canis, Trichophyton rubrum, and Trichophyton mentagrophytes was assessed utilizing the poison food technique method. The percentage of plumbagin recorded in the leaves, stems, and roots was found to be 0.51±0.001%, 0.16±0.001%, and 1.65±0.015%, respectively. The GC-MS examination declared the presence of 59 molecules in the plant extract. The plant extract and pure plumbagin exhibited complete inhibition against all tested dermatophytes at 6.0mg/mL for the extracts and 0.2mg/mL for plumbagin. P. europaea root is the best source of plumbagin and the plant extract could represent a potential drug candidate for the treatment of dermatophytosis infections. Further studies required to design suitable dosage forms from the natural P. europaea root extracts or plumbagin alone, to be utilized for the treatment of dermatological and veterinary ailments.

Biological Properties and Bioactive Components of Mentha spicata L. Essential Oil: Focus on Potential Benefits in the Treatment of Obesity, Alzheimer's Disease, Dermatophytosis, and Drug-Resistant Infections.

In the present study, the medicinal aromatic plant Mentha spicata has been investigated as a source of essential oil (EO) and pharmaceuticals. The quantity and composition of EO from M. spicata cultivated in Palestine were analyzed seasonally over a three-year period. A significantly higher EO content was produced in summer and fall months (2.54-2.79%). Chemical analysis of EO revealed 31 compounds with oxygenated monoterpenes (90%) as the most abundant components followed by sesquiterpene and monoterpene hydrocarbons (6 and 3%, respectively). M spicata can be characterized as a carvone chemotype (65%). EO and carvone have shown strong inhibitory activities against the principal enzymes associated with Alzheimer's disease (AD) and overweight diseases (cholinesterase and porcine pancreatic lipase) and also shown strong antidermatophytic activity against Microsporum canis, Trichophyton rubrum, T. mentagrophytes, and Epidermophyton floccosum. The pancreatic lipase inhibition and the synergism showed the potential activity of M. spicata EO and carvone and that their combinations with standard drugs can be useful for the treatment of obesity and overweight. The results also demonstrated that, in addition to their significant inhibitory activity against biofilm formation of methicillin-resistant Staphylococcus aureus (MRSA), M. spicata EO and carvone had a strong inhibitory effect on metabolic activity and biomass of the preformed biofilm. The current study supports the utilization of M. spicata EO as a traditional medicine and opens perceptions to find more potent substances in the EO for the management of obesity, AD, and dermatophytosis and for combating drug-resistant bacterial infections.

Rapid, cost-effective and organic solvent-free production of biologically active essential oil from Mediterranean wild Origanum syriacum.

BACKGROUND: Origanum syriacum (O. syriacum) is a very popular edible and medicinal plant in the East Mediterranean countries. The aims of the current study were to use microwave-ultrasonic assisted hydrodistillation (MUAHD) method to produce essential oils (EOs) from wild O. syriacum samples collected from four different geographical areas in The West Bank using water as a solvent, determine the phytochemical profile using GC-MS analysis and assess their antioxidant and antibacterial potential. METHODS: Essential oils were produced using MUAHD method. Gas chromatography coupled with mass spectrometer detector (GC-MS) was employed for phytochemical analysis. In vitro antibacterial and antioxidant potentials were carried out. RESULTS: Differences in the EOs yield among the four Origanum samples were observed. GC-MS analysis of EOs revealed terpenes as the major constituents; monoterpenes (22-56%) and oxygenated monoterpenes (28-57%). Thymol, α-terpinene and carvacrol represent the bulk of all phytochemicals detected by GC-MS analysis. γ-Terpinene-rich EOs, exhibited the highest antioxidant capacity. Thymol-rich EOs were found to be most effective against Staphylococcus aureus and Methicillin-Resistant Staphylococcus aureus (MRSA) (MIC 390 µg/mL). Alpha-terpinene-rich chemotype EOs exhibited the highest inhibitory effect of Pseudomonas aeruginosa (MIC of 1560 µg/mL). Interestingly, γ-terpinene-rich EO showed promising antibacterial properties against Enterococcus faecium (MIC 97 µg/mL) and a powerful anti-oxidant effect (91.45% ±2.30). CONCLUSION: The current study supports the use of MUAHD as a time-saving, cost-effective, environment-friendly method for production of high quality O. syriacum EO for potential use as a natural complementary treatment and in the prevention of bacterial infections as well as oxidation by free radicals without compromising the quantity.

The effect of inhalation of Citrus sinensis flowers and Mentha spicata leave essential oils on lung function and exercise performance: a quasi-experimental uncontrolled before-and-after study.

BACKGROUND: Recently, there has been an increased interest in the effects of essential oils on athletic performances and other physiological effects. This study aimed to assess the effects of Citrus sinensis flower and Mentha spicata leaves essential oils inhalation in two different groups of athlete male students on their exercise performance and lung function. METHODS: Twenty physical education students volunteered to participate in the study. The subjects were randomly assigned into two groups: Mentha spicata and Citrus sinensis (ten participants each). One group was nebulized by Citrus sinensis flower oil and the other by Mentha spicata leaves oil in a concentration of (0.02 ml/kg of body mass) which was mixed with 2 ml of normal saline for 5 min before a 1500 m running tests. Lung function tests were measured using a spirometer for each student pre and post nebulization giving the same running distance pre and post oils inhalation. RESULTS: A lung function tests showed an improvement on the lung status for the students after inhaling of the oils. Interestingly, there was a significant increase in Forced Expiratory Volume in the first second and Forced Vital Capacity after inhalation for the both oils. Moreover significant reductions in the means of the running time were observed among these two groups. The normal spirometry results were 50 %, while after inhalation with M. spicata oil the ratio were 60 %. CONCLUSION: Our findings support the effectiveness of M. spicata and C. sinensis essential oils on the exercise performance and respiratory function parameters. However, our conclusion and generalisability of our results should be interpreted with caution due to small sample size and lack of control groups, randomization or masking. We recommend further investigations to explain the mechanism of actions for these two essential oils on exercise performance and respiratory parameters. TRIAL REGISTRATION: ISRCTN10133422, Registered: May 3, 2016.