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.

Chemical compositions, antibacterial, antifungal and cytotoxic effects of Alhagi mannifera five extracts.

OBJECTIVES: Plants were used as medicines thousands of years ago. Conventional medicine use is increasing and many of the currently used drugs are extracted from herbal sources. In Palestinian traditional medicine, the Alhagi mannifera plant is used for the treatment of cancer. Our study aimed to extract this plant using five solvent fractions, identifying their chemical compositions, and evaluating their antimicrobial and cytotoxic effects. METHODS: The successive technique was used to extract five solvent fractions of A. mannifera. While the spectral analysis was used to characterize quantitatively and qualitatively the chemical components of these extracts. The antimicrobial activity of plant extracts was evaluated against seven microbial strains using a broth micro-dilution assay. The cytotoxic activity was assessed using a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay against cervical cancer cell line (HeLa). RESULTS: A total of 165 compounds were identified in A. mannifera different extracts. In the petroleum ether extract were found a total of 55 compounds. The major compounds were 2,5-cyclooctadien-1-ol (9.42%), 3-chloropropionic acid, heptyl ester (9.42%), carbonic acid, ethyl nonyl ester (9.42%) and chloroacetic acid. In methylene chloride extract a total of 11 compounds were found, and the major compounds were m-ainobenzenesulfonyl fluoride (14.35%), dodecane,2,6,10-trimethyl- (14.35%) and propanoic acid,2,2-dimethyl-,2-ethylexyl ester (14.35%). In chloroform extract, a total of 23 compounds were found. The major compounds were 5-ethyl-1-nonene (21.28%), and decanedioic acid, bis(2-ethylhexyl) ester (21.28%). In acetone extract were found a total of 47 compounds and the major compound was phenol,2,4-bis(1,1-dimethylethyl)- (5.22%). In methanol extract a total of 29 compounds were found and the major compounds were 3-o-methyl-d-glucose (10.79%), myo-inositol, 2-c-methyl- (10.79%), myo-inositol, 4-c-methyl- (10.79%), and scyllo-inositol,1C-methyl- (10.79%). All extracts showed antimicrobial activity. However, the petroleum ether extract showed the most potent antimicrobial effect against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumonia, MRSA, and Candida albicans with minimal inhibitory concentration (MIC) values of 1.25, 1.25, 6.25, 0.325, 6.25, and 1.56 µg/mL, respectively. De facto, chloroform extract followed by ether extract displayed potential cytotoxic activity with IC50 values of 0.2 and 1.2 mg/mL, respectively. CONCLUSIONS: A. mannifera was found to contain a variety of phytochemicals and its chloroform extract showed a potent cytotoxic effect on HeLa cancer cells. In addition, petroleum ether showed potent antimicrobial agents and these extracts look promising as drug candidates. Further in vivo investigations should be conducted to provide the basis for developing new cancer and microbial infections treatments.

Spectral characterization, antioxidant, antimicrobial, cytotoxic, and cyclooxygenase inhibitory activities of Aloysia citriodora essential oils collected from two Palestinian regions.

BACKGROUND: Aloysia citriodora Palau (AC) is commonly known as Lemon Verbena and has been utilized as a medicinal tea in folkloric medicine for the treatment of abdominal spasm, anxiety, and fever. The present investigation aimed to identify the chemical ingredients of AC essential oil (EO) collected from two different locations in Palestine and to assess their antioxidant, antimicrobial, cytotoxic, and cyclooxygenase (COX) inhibitory effects. METHODS: Gas chromatography/mass spectroscopy (GC/MS) technique was used to identify the chemical components of the hydro-distilled EO from both regions, while DPPH, MTS, and COX assays were utilized to estimate the antioxidant, cytotoxic, and COX inhibitory activities of the EOs, respectively. Moreover, a broth microdilution assay was used to assess antimicrobial potentials against seven microbial strains. RESULTS: The GC/MS technique revealed the presence of 17 compounds from the AC collected from the Umm al-Fahm region and 13 compounds from the sample from the Baqa al-Gharbiyye region, while α-citral was the major component of both EOs, representing 47.62 and 43.46%, respectively. The Baqa al-Gharbiyye AC EO exerted more potent antioxidant activity than the Umm al-Fahm EO, with IC50 values of 11.74 ± 0.18 and 35.48 ± 0.14 µg/mL, respectively, while the positive control Trolox had antioxidant IC50 values of 2.45 ± 0.01 µg/mL. Interestingly, both EOs inhibited more potential activity against Methicillin-Resistant Staphylococcus aureus (MRSA) and Proteus vulgaris than Ciprofloxacin and Ampicillin antibiotics and also showed more potent antifungal activity against Candida albicans than Fluconazole. Moreover, the Baqa al-Gharbiyye AC EO had a more potent cytotoxic effect than the Umm al-Fahm EO, with IC50 values of 84.5 ± 0.24 and 33.31 ± 0.01 µg/mL, respectively, compared with Doxorubicin, which had an IC50 dose of 22.01 ± 1.4 µg/mL. The EOs from Baqa al-Gharbiyye showed potent activity against both COX-1 and COX-2 enzymes, with IC50 of 52.93 ± 0.13 and 89.31 ± 0.21 µg/mL, respectively, while the EOs from the Umm al-Fahm region showed weaker activity against these enzymes, with IC50 of 349.99 ± 0.33 and 1326.37 ± 1.13 µg/mL, respectively. CONCLUSION: Both characterized EOs have a huge variety of chemical components. The Baqa al-Gharbiyye AC EO has more potent antioxidant and cytotoxic activities than the Umm al-Fahm EO, but both have potential antimicrobial activity against MRSA, P. vulgaris, and C. albicans. These results suggest the use of AC EOs as promising sources of active ingredients in the food, cosmetic, and pharmaceutical industries.