The hepatoprotective activity of the different extracts of Ficus sycomorus L. (FS) against N nitrosodiethylamine (NDEA) and CCl4-induced hepatocarcinogenesis (HCC) in rats has been investigated for the first time. Histological observations of liver tissues demonstrated that, both wood (FSWE) and leaf extracts (FSLE) possess significant hepatoprotective activity and stem bark extract (FSBE) shows moderate activity while fruit extract (FSFE) is not significantly effective.

A new iridoid glycoside; 6-O-β-D-xylopyranoside-shanzhiside methyl ester (1) along with six known compounds; shanzhiside methyl ester (2), lamalbid (3), geniposidic acid (4), theveside (5), verbascoside (6) and arenarioside (7) were isolated from the roots of Lantana montevidensis. The structures of the compounds were determined through 1D and 2D NMR spectroscopic data analysis, HRESIMS, electronic circular dichorism and UPLC-UV/MS method. The total extract, chloroformic (F1) and aqueous (F2) fractions together with the isolated compounds were tested for their antimicrobial, antiprotozoal, antiplasmodial, anti-inflammatory, monoamine oxidase inhibition and cell viability activities in addition to free radical scavenging activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The phenylpropanoid compounds (6 and 7) resulted in a potent antioxidant activity. Total methanolic extract together with the aqueous fraction (F2) showed decrease in reactive oxidative stress with 57 and 66%, respectively, while the chloroformic fraction (F1), together with the total methanolic extract, showed a decrease in iNOS with IC50 values 5 and 30 μg/mL, respectively. Compounds 1, 2, 3, 6, and 7 showed inhibition in the reactive oxidative stress with values 50, 60, 57, 63, and 52%, respectively. Both F1 and F2 fractions demonstrated measurable inhibition of MCF-7 breast cancer cell growth, with IC50 value 0.3 mg/mL. Compounds 2 and 7 showed mild monoamine oxidase inhibition. None of the tested compounds showed antimicrobial, antiplasmodial or antiprotozoal activity.

A new iridoid glycoside; 6-O-β-D-xylopyranoside-shanzhiside methyl ester (1) along with six known compounds; shanzhiside methyl ester (2), lamalbid (3), geniposidic acid (4), theveside (5), verbascoside (6) and arenarioside (7) were isolated from the roots of Lantana montevidensis. The structures of the compounds were determined through 1D and 2D NMR spectroscopic data analysis, HRESIMS, electronic circular dichorism and UPLC-UV/MS method. The total extract, chloroformic (F1) and aqueous (F2) fractions together with the isolated compounds were tested for their antimicrobial, antiprotozoal, antiplasmodial, anti-inflammatory, monoamine oxidase inhibition and cell viability activities in addition to free radical scavenging activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The phenylpropanoid compounds (6 and 7) resulted in a potent antioxidant activity. Total methanolic extract together with the aqueous fraction (F2) showed decrease in reactive oxidative stress with 57 and 66%, respectively, while the chloroformic fraction (F1), together with the total methanolic extract, showed a decrease in iNOS with IC50 values 5 and 30 μg/mL, respectively. Compounds 1, 2, 3, 6, and 7 showed inhibition in the reactive oxidative stress with values 50, 60, 57, 63, and 52%, respectively. Both F1 and F2 fractions demonstrated measurable inhibition of MCF-7 breast cancer cell growth, with IC50 value 0.3 mg/mL. Compounds 2 and 7 showed mild monoamine oxidase inhibition. None of the tested compounds showed antimicrobial, antiplasmodial or antiprotozoal activity.

A new iridoid glycoside; 6-O-β-D-xylopyranoside-shanzhiside methyl ester (1) along with six known compounds; shanzhiside methyl ester (2), lamalbid (3), geniposidic acid (4), theveside (5), verbascoside (6) and arenarioside (7) were isolated from the roots of Lantana montevidensis. The structures of the compounds were determined through 1D and 2D NMR spectroscopic data analysis, HRESIMS, electronic circular dichorism and UPLC-UV/MS method. The total extract, chloroformic (F1) and aqueous (F2) fractions together with the isolated compounds were tested for their antimicrobial, antiprotozoal, antiplasmodial, anti-inflammatory, monoamine oxidase inhibition and cell viability activities in addition to free radical scavenging activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The phenylpropanoid compounds (6 and 7) resulted in a potent antioxidant activity. Total methanolic extract together with the aqueous fraction (F2) showed decrease in reactive oxidative stress with 57 and 66%, respectively, while the chloroformic fraction (F1), together with the total methanolic extract, showed a decrease in iNOS with IC50 values 5 and 30 μg/mL, respectively. Compounds 1, 2, 3, 6, and 7 showed inhibition in the reactive oxidative stress with values 50, 60, 57, 63, and 52%, respectively. Both F1 and F2 fractions demonstrated measurable inhibition of MCF-7 breast cancer cell growth, with IC50 value 0.3 mg/mL. Compounds 2 and 7 showed mild monoamine oxidase inhibition. None of the tested compounds showed antimicrobial, antiplasmodial or antiprotozoal activity.

Background: Sitagliptin (SITA), is an oral anti-diabetic drug of dipeptidyl peptidase-4 (DPP-4) inhibitor class used as a monotherapy or in association with metformin to treat type II Diabetes Mellitus. Methods: Two new, sensitive and precise spectrofluorimetric methods have been developed for the determination of SITA in tablets and spiked human urine samples. SITA has a native fluorescence that was enhanced by 2 folds after addition of β-cyclodextrin (method A). The fluoregenic product was measured at 296 nm after excitation at 267 nm. In addition, SITA was derivatized by 7-chloro-4- nitrobenzofurazon (NBD-Cl) to a highly sensitive fluoregenic product was measured at 532 nm after excitation at 466 nm (method B). Results: The fluorescence intensities were directly proportional to the concentration over the range 0.35-10 µg mL-1 and 0.1-3 µg mL-1 for method A and B, respectively. The %RSD for inter-day and intra-day precisions was in a range of 0.160-0.915% and the accuracy results were in the range of 96.28% -100.03%. Conclusion: Successful applications of the developed methods, for drug determination in pharmaceutical tablet and spiked human urine samples, were performed with high accuracy and precision.

Background: Sitagliptin (SITA), is an oral anti-diabetic drug of dipeptidyl peptidase-4 (DPP-4) inhibitor class used as a monotherapy or in association with metformin to treat type II Diabetes Mellitus. Methods: Two new, sensitive and precise spectrofluorimetric methods have been developed for the determination of SITA in tablets and spiked human urine samples. SITA has a native fluorescence that was enhanced by 2 folds after addition of β-cyclodextrin (method A). The fluoregenic product was measured at 296 nm after excitation at 267 nm. In addition, SITA was derivatized by 7-chloro-4- nitrobenzofurazon (NBD-Cl) to a highly sensitive fluoregenic product was measured at 532 nm after excitation at 466 nm (method B). Results: The fluorescence intensities were directly proportional to the concentration over the range 0.35-10 µg mL-1 and 0.1-3 µg mL-1 for method A and B, respectively. The %RSD for inter-day and intra-day precisions was in a range of 0.160-0.915% and the accuracy results were in the range of 96.28% -100.03%. Conclusion: Successful applications of the developed methods, for drug determination in pharmaceutical tablet and spiked human urine samples, were performed with high accuracy and precision.

Coadministration of tamoxifen citrate (TMC) and medroxyprogesterone acetate (MPA) is preferred to increase the response rate and the percentage recovery in patients with endometrial carcinoma. Administration of TMC and MPA and their combination affects estrogen and progestin receptor concentrations in advanced endometrium carcinoma by affecting 17β-hydroxyl steroid dehydrogenase activity and serum hormone concentrations. A sensitive, accurate and robust thin-layer chromatography method has been established for simultaneous analysis of TMC and MPA. Method development was carried out on silica gel F254 using butanol–acetic acid–water (6:0.5:0.5, v/v/v) as mobile phase. Densitometric scanning was carried out at 241nm for simultaneous detection of TMC and MPA. Retardation factor (Rf) values for TMC and MPA were 0.21 and 0.85, respectively. The method was validated according to ICH guidelines. Regression plots revealed linear relationships in the concentration range of 50–500 and 25–250 ng/band for TMC and MPA, successively. Accuracy was ≥99.60 and 98.72% for TMC and MPA, respectively. Forced degradation studies using UV photodegradation was applied on MPA after exposure to UV light for different times and applying a kinetic study for calculating the degradation rate constant (k) and half-life time (t1/2).

Coadministration of tamoxifen citrate (TMC) and medroxyprogesterone acetate (MPA) is preferred to increase the response rate and the percentage recovery in patients with endometrial carcinoma. Administration of TMC and MPA and their combination affects estrogen and progestin receptor concentrations in advanced endometrium carcinoma by affecting 17β-hydroxyl steroid dehydrogenase activity and serum hormone concentrations. A sensitive, accurate and robust thin-layer chromatography method has been established for simultaneous analysis of TMC and MPA. Method development was carried out on silica gel F254 using butanol–acetic acid–water (6:0.5:0.5, v/v/v) as mobile phase. Densitometric scanning was carried out at 241nm for simultaneous detection of TMC and MPA. Retardation factor (Rf) values for TMC and MPA were 0.21 and 0.85, respectively. The method was validated according to ICH guidelines. Regression plots revealed linear relationships in the concentration range of 50–500 and 25–250 ng/band for TMC and MPA, successively. Accuracy was ≥99.60 and 98.72% for TMC and MPA, respectively. Forced degradation studies using UV photodegradation was applied on MPA after exposure to UV light for different times and applying a kinetic study for calculating the degradation rate constant (k) and half-life time (t1/2).

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