Iranian Journal of Pharmaceutical Sciences

Natural medicine products usually consist of two to five kinds of plants that have synergistic biological activity. The responsible constituents for the therapeutic activity in plants often involve diverse chemical components. The combination of ethanol extracts of Annona squamosa L. (EEAS) and Persea americana M. (EEPA) has been shown to have antihyperlipidemic activity. To ensure the correctness and consistency of the EEAS and EEPAs combination as the antihyperlipidemic treatments, it is necessary to characterize the plant’s secondary metabolites. This study aimed to obtain the profiles of the secondary metabolites of Annona squamosa L. and Persea americana M. using the TLC-densitometry technique. Extract samples were applied to TLC plates and screened using densitometry at 254 nm. The obtained chromatogram peak was measured at the wavelength range of 200–700 nm to obtain the maximum wavelength of each peak. The results showed that EEAS had 5 peaks with rf values of 0.00, 0.61, 0.67, 0.73, and 0.87. The TLC-densitometry analysis results of EEPA showed eight peaks with rf values of 0.00, 0.11, 0.19, 0.49, 0.56, 0.71, 0.77, and 0.90. The extract chromatograms spectra showed that 2–3 peaks at the wavelength range of 300-350 nm. Chromatogram TLC-densitometry profile data on EEAS and EEPA can be used as the indicators in the raw material combinations standardization process of EEAS and EEPA as natural medicine products to treat antihyperlipidemic.

Nowadays medicinal plants have been considered as the complementary medicine in cancer treatment by researchers. Some plants possess chemical compounds which are able to inhibit the growth of cancer cells or even eliminate them through apoptosis or necrosis. In current study anticancer effect of Tilia dasystyla and Polygonatum orientale Desf extracts on AGS and SKOV-3 cancer cell lines were investigated. The cytotoxic effect of Tilia dasystyla and Polygonatum orientale Desf extracts on AGS and SKOV-3 has not been reported so far. Cancer cell lines were treated with different concentrations (100-5000 μg/ml) of T. dasystyla and P. orientale Desf methanol extracts for 24, 48, 72 hours. Cell viability of AGS and SKOV-3 cancer cells were evaluated by MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide) method. Results of the study indicate that, extracts of T. dasystyla and P. orientale Desf showed cytotoxic effect on AGS and SKOV-3 cancer cell lines. The lowest IC50 value of AGS and SKOV-3 cell lines was about 1.02 ± 0.01 mg /ml and 1.14 ± 0.17 mg / ml respectively. T. dasystyla and P. orientale Desf extracts showed cytotoxic effect on AGS and SKOV-3 cancer cell lines in time- and dose-dependent manner. Full potential of the extracts, as an option for cancer treatment, is yet to be determined by further studies on animal models and subsequent trials.

A series of new class of quinoline analogues were synthesized from isatin through two steps in good yields. All compounds were further evaluated for their anticancer activity against triple-negative breast cancer cell line (MDA-MB-231) using MTT assay and antibacterial activity against Gram-positive bacteria (Staphylococcus aureus 6538p and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) using agar well diffusion method. All synthesized compounds were confirmed by spectral characterization viz FT-IR, MS, 1H-NMR, and 13C-NMR. Results indicated that in vitro anticancer evaluation, IC50 values of all target compounds were in the range of 11.50-37.99 μM and compound 4h showed better promising anti-breast cancer activity among all synthesized derivatives. In vitro antibacterial evaluation, compounds 4d, 4f, 4h, and 4j showed moderate antibacterial activity among all derivatives. Molecular docking analysis demonstrated good interaction of compound 4h with the active site residue of Human Carbonic Anhydrase I, Protein Kinase A, and Kinesin Spindle Protein (KSP).

The present study was aimed to evaluate the antibacterial potential of ethanol, methanol, acetone, and aqueous extracts of some bryophytes common in Armenia (Mnium spinosum (Voit) Schwaegr, Brachythecium salebrosum (Web. et Mohr) B.S.G., Thuidiumrecognitum (Hedw) Lindb and Dicranum scoparium (Hedw). Antibacterial activity was determined using agar-well diffusion method against five bacterial species (Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Salmonella enterica, and S. typhimirium). The results showed that the bryophytes D. scoparium and B. salebrosum possessed high antibacterial activity in methanol extracts, whereas M. spinosum has high antibacterial activity in acetone extract. Antibacterial activity against S. aureus was comparably weaker. Ethanol extract of T. recognitum had greater antibacterial activity than the extract of M. spinosum. Of all those tested for antibacterial activity bryophytes in vitro extracts of D. scoparium have yielded the most promising results. Antibacterial activity might be caused by a high content of flavonoids in bryophytes determined. Thus, the studied bryophytes might be used to develop new antibacterial agents.

Breast cancer is the most common malignancy among American women and the second leading cause of cancer death after the lung cancer. For this reason, trying to find new drugs for the treatment of this disease is essential. The aim of the present study was to evaluate the cytotoxic effects of three cinnamic acid derivatives isolated from Allium ampeloprasum var. Persicum including Caffeoyl tyramine, Feruloyl tyramine, and Persicoimidate on two breast cancer cell lines, MCF-7 and BT-474. Evaluation the cytotoxic effects of mentioned purified compounds against MCF-7 and BT-474 cells was performed using MTT assay and their IC50 was determined. Finally, flow cytometery analysis on MCF-7 cells was performed and used to determine the cell death mechanism of investigated compounds. The results exhibited that the cytotoxic effects of all three compounds against breast cancer cell lines was concentration-dependent. The IC50 of Caffeoyl tyramine, Feruloyl tyramine, and Persicoimidate was determined to be as 73, 56, and 40 μg/ml for MCF-7 and 100, 54, and 37 μg/ml for BT-474 cells, respectively. So, Perscicoimidate showed the most potent cytotoxic effects against two breast cancer cells. Finally, flow cytometery analysis showed that Persicoimidate caused approximately 48% of apoptosis in concentration of 40 μg/ml. According to the tyrosine kinase inhibitory activity of cinnamic acid derivatives, these compounds has the potential of being cancer drug candidates for complementary studies on breast tumors with highly expression of EGF receptor. However, evaluation of anticancer effects of these compounds against other breast cancer cell lines is suggested.

This study was planned to formulate, characterize, and evaluate to establish the bioavailability of gastroretentive mucoadhesive dosage of atenolol in human subjects with possible in-vitro-in-vivo correlation. In this investigation gastroretentive mucoadhesive dosage of Atenolol was formulated using HPMCK4M, chitosan and Isabgul husk by wet granulation technique. The prepared tablets were subjected to physical evaluation, in-vitro drug release, and in-vivo X-ray studies, followed by the pharmacokinetic study in human volunteers. All the prepared tablets showed physicochemical properties within the limits and good in-vitro mucoadhesion. Formulation F2 was selected based on the in-vitro characteristics and in-vivo radiographic studies by replacing part of the drug by adding barium sulphate. From the radiographic studies it was found that the F2 could be successfully retained in stomach for more than 6 hours. Pharmacokinetic studies showed a significant improvement in AUC0-14; 6414.93 ± 58.221 ng.h/mL (p < 0.05) when compared to reference AUC0-14; 4752.18 ± 76.759 ng.h/mL in healthy human volunteers with good in vitro-in vivo correlation. Based on in-vitro characteristics and in-vivo radiographic studies, F2 was selected as optimized gastroretentive mucoadhesive dosage form with improved bioavailability for better patient compliance and disease management.

Centella asiatica L. (C.asiatica) is a plant with a hypotensive effect. Since this effect has several mechanism(s), therefore in the current study we investigated the effects of hydroalcoholic extract of C.asiatica on cardiovascular parameters in acute hypertensive rats. Animals were divided into four groups; 1) control, 2) Angiotensin II (AngII) that received (50 ng/kg) intravenously (i.v.), 3 and 4) two groups of C.asiatica extract (CA100, and CA200 mg/kg). In treated groups, 30 min after injection of the extract, AngII was injected. Cardiovascular parameters were recorded by the power lab system after the cannulation of the femoral artery. The maximum changes (Δ) of systolic blood pressure (SBP), mean arterial pressure (MAP), and heart rate (HR) were calculated and used for statistical analysis. In the AngII group, ΔSBP and ΔMAP significantly increased compared to the control group. The HR also decreased compared to the control group but it was not significant. In CA100+AngII group ΔSBP and ΔMAP significantly decreased compared to the AngII. The use of these doses of CA with AngІІ compared to AngІІ alone had a significant effect on the HR. In CA200+AngII group ΔSBP and ΔMAP significantly decreased compared to the AngII. The change of HR in this dose was not significant to the AngII. In a recent study, we concluded that C.asiatica decreased the cardiovascular responses in hypertensive rats received AngII. Also between two doses of C.asiatica did not observe any significant difference. Therefore, one of the most important hypotensive mechanism(s) of the considered plant can be the effect on Renin-angiotensin system.

Drug-drug interactions (DDIs) result from the simultaneous consumption of two or more drugs that alter the patient’s response to the initial drug. The treatment regimen in patients with kidney disease is very diverse and may be associated with several diseases that increases the risk of DDIs. This study was carried out to investigate the DDIs incidence in patients with chronic kidney disease (CKD) in the nephrology ward. This descriptiveanalytical study was performed in a 4-month period in 2017. The patients’ information, such as age, sex, list of drugs during hospitalization, and kidney disease stage were recorded from patients’ medical records. Drug-drug interactions were extracted using LexiComp Online. In this study 48.55% of patients were male, 51.45% were female, and 53.2% of patients were in stage 5 of kidney disease. There was a significant correlation between the incidence of drug-drug interactions with stage 5 of disease (P=0.02). The highest number of interactions was categorized as type C and interaction between atorvastatin and pantoprazole was the most frequent interaction. The maximum range of prescription drugs was between 6 and 10 items by 49.7% of patients. There was a significant correlation between the incidence of drug-drug interactions and the number of prescribed drugs (P=0.03). Drug-drug interactions are common in patients with chronic kidney disease. Based on the results, the number of prescribed drugs and the stage of the disease are effective in drug-drug interactions incidence. It is possible to reduce drug complications and to increase the life span of patients by recognizing drug-drug interactions.