Iranian Journal of Pharmaceutical Sciences

In recent years, the potential of marine natural products as anticancer agents, specifically for breast cancer, has been examined. The sea cucumber (Holothuroidea: Echinodermata) is known to contain triterpene glycosides, which have shown anticancer or cytotoxic activity. In this research, molecular docking of selected sea cucumber bioactive compounds was conducted on five receptor targets that play an important role in breast cancer: estrogen receptor alpha (ER-α), fibroblast growth factor receptor 1 (FGFR1), vascular endothelial growth factor receptor 2 (VEGFR2), progesterone receptor (PR), and insulin-like growth factor 1 receptor (IGFR1). The purpose of this was to observe the interaction between active compounds and the active site of breast cancer receptor targets. Holothurin A gave the lowest binding energy (-7.1 kcal/mol) and was involved in a hydrogen bond with amino acid His-516 when superposition towards to E4D cocrystal was present. Holothurin A also had a similar posing with raloxifene, in which the hydrogen bond with His-516 with a RMSD value of 3.3 Å was observed with superposition towards to the positive control raloxifene. The analysis and visualization results of 24-dehidroechinoside that was superposed on E4D cocrystal, BMI cocrystal, and positive control raloxifene showed that 24-dehidroechinoside had a hydrophobic interaction with amino-acid residue Leu-346, a strong hydrogen bond to Gln-977, as well as a hydrogen bond to Thr-347 in a distance of 3.7 Å, and a hydrophobic interaction with amino-acid residue Ala-350. The most potent in silico anti-breast cancer compounds in sea cucumbers are holothurin A and 24-dehidroechinoside. Holothurin A is active as an antibreast cancer agent by inhibiting ER-α, while 24-dehidroechinoside inhibits both ER-α and IGFR1.

Nuclear factor erythroid 2-related factor 2 (Nrf2) is one of the transcription factors involved in providing endogenous antioxidants. Black seed oil (BSO), suspected have antioxidant effects that can be used to modulate the expression and levels of Nrf2. The study aims to determine the effect of BSO as adjuvant therapy on levels of Nrf2 to the patients with metabolic syndrome risk.The research used analytical observational with cohort design. Samples study consisted of 62 patients at risk with metabolic syndrome risk at Jetis I Public Health Center, Bantul District, from September to December 2016. Eligible subjects were divided into two groups, (1) BSO group, patients get BSO with a dose of 3 mL/day and standard therapy for 20 days. (2) Control group, patients got placebo and standard therapy during the intervention for 20 days. Levels of Nrf2 were estimates using enzyme-linked immunosorbent assay (ELISA) method. The mean values ± SD between groups were tested with independent t-test with significance of p=<0.05 (95%). The results showed that Nrf2 in group 1 was 0,866 ± 0,11 ng/ml and the group 2 was 0,864 ± 0,15 ng/mL (p=0,94). There were no significant difference in the both groups (p>0.05).In conclusion, adjuvant therapy of BSO doses 3 mL/day for 20 days could not increase levels of Nrf2 in the patients with metabolic syndrome risk based on type treatment and demographic characteristic at Jetis I Public Health Center, Bantul District.

The purpose of this study is Acamprosate Calcium synthesis of 3-Aminopropane-1-sulfonic acid (Homotaurine) and validation of assay test in the delayed-release tablets by HPLC without organic solvents. The
assay method by HPLC was found to be linear in the concentration range of 50 to 200 μg/mL. Successful separation was achieved by isocratic elution on a Phenomenex® C18 column (250 mm × 4.6 mm, 5μm).The mobile phase was triethylammonium phosphate buffer pH: 4.0 (100%) at the flow rate of 1 mL/min using UV detection at 210 nm, column oven temperature 25ºC and injection volume 20

Common techniques for the treatment of Hepatocellular carcinoma (HCC) have not been successful, and thus the design and discovery of new compounds with better anti-cancer function are needed. Snake venom is among the most important compounds used by researchers to the treatment of various cancers. This study was designed to evaluate the toxicity effect of Persian Gulf snake venom (Enhydrina schistosa) on hepatocytes and mitochondria isolated from HCC rats model. HCC has been induced in rats with diethylnitrosamine (DEN) and 2-acetylaminofluorene (2-AAF). Then rat hepatocytes were isolated with collagen perfusion technique. The results showed that E. schistosa (5, 10, 20 and 40 μg/ml) increases the level of reactive oxygen species (ROS) generation, collapse in mitochondrial membrane potential (MMP), swelling in mitochondria, and cytochrome c release only in hepatocytes and mitochondria isolated from the HCC group. These results proposed that E.schistosa could be considered as a promising complementary therapeutic agent for the treatment of HCC.

Skin burns are common skin injuries that can result from exposure to various sources of heat by which, depending on the cause, different degrees of burns are generated. In restoration of superficial burns by reepithelialization, the skin is rebuilt, but the skin color is different than the healthy tissue. Keratinocytes represent the major cells of the epidermis. These cells are sourced from ectoderm and are continuously being formed from the basal level. The main task of these cells is to make the protein keratin. During differentiation, keratinocytes move toward the superficial layers of the epidermis and generate more keratin. These cells are colorless, but by manipulating melanocytes (the melanocyte cells produce pigment in the skin), one can control the darkness degree of the skin. Keratinocytes, in particular, produce chemical signals which, in turn, are responsible for regulating the distribution and amount of melanin pigment in melanocytes. In this study, using an aluminum stamp weighing 85 grams, at a temperature of 80 ◦C, superficial burns, of 2nd degree, were generated on six rabbits. The rabbits were divided into two groups; a control group and the second one in which a chitosan (CHI) gel was used as a dressing.
After treatment, histopathology tests and the TEM results confirmed that, in the CHI treatment group, the restoration led to acceptable results. It was shown that if the repair was performed with a CHI based gel, the keratinocyte appeared with their original structure after restoration, but if the treatment was done without the CHI dressing, the number of these cells increased, more stimulation of melanocytes occurred and, ultimately, it led to an unwanted color change of the burnt area.

The purpose of present research work is to develop gastro retentive formulation for Moxifloxacin using various release retardants. Moxifloxacin, that is a novel synthetic fluoro quinolone, is an iantibacterial agent. Floating tablets of Moxifloxacin. HCl were prepared using variable amounts of HPMCK4M, HPMCK15M and HPMCK100M with effervescent mixtures by direct compression technique. Totally 9 formulations were designed, prepared and are evaluated for various pharmacopoeial tests like uniformity of weight, thickness,Hardness, friability, floating lag time, Total floating time. Drug release profiles of formulation trails subjected to kinetic modeling. Parameters like correlation coefficient(r), slope (b), intercept (a) were determined. The results reveal that floating lag time decreases with decreased viscosity of polymer composites. According to SUPAC guidelines formulation (F4) containing 12.5% HPMCK15M was found to be most identical formulation (similarity factor f2= 70.997, dissimilarity factor f1= 6.007 to marketed product (AVELOX). Trail F4 drug release found to be first order kinetics, Non-Fickian Diffusion Anomalous Transport. (n= 1.065).

Breast engorgement is a common problem during breastfeeding that can lead to early discontinuation of breastfeeding. Commiphora Mukul (C. Mukul) is a medicinal plant with analgesic and anti-inflammatory
compounds. The present study was conducted to determine the effect of C. Mukul on improving breast engorgement in breastfeeding women. This study was a double-blind, randomized, and placebo-controlled trial conducted with 100 breastfeeding women, whose symptoms of breast engorgement were randomly allocated to C. Mukul cream group or placebo. Both groups were to rub one fingertip of cream on each breast after nursing 8 times a day for 2 days. The breast engorgement symptoms )severity index = erythema + tension + pain erew assessed by the validated breast engorgement checklist. The severity of breast engorgement before the intervention was not significantly different between the two drug and placebo groups (breast erythema (P=0.78),tension (P=0.85) and pain (P=0.06)), but two days after the intervention, 60% of women in the drug group and 22 % of them in the placebo group scored zero in breast engorgement checklist, though there was a significant difference between the groups (P<0.001). No side effects were observed or reported in either group. According to the findings, Commiphora Mukul cream can improve breast engorgement.

Epilepsy is a highly debilitating disorder by unpredictable seizures associated with emotional disturbance.One potential treatment for seizure and depression is dietary therapy. So, this study evaluated effects of daily oral administration of sesame and flaxseed oils in depression and seizure. Twenty-one adult male mice were divided into the following groups: control (normal saline recipient, 1ml/kg( , sesame and flaxseed oils groups (8ml/kg bodyweight, for 21 days). At the 22nd day, locomotor activity and depressive - like behavior were assessed by open field and tail suspension tests. Also in 23rd day, animals received a subcutaneous injection of strychnine for induction of seizure. The seizure latency and death time were recorded through observation of animal behavior immediately after injection of strychnine. There were no significant differences in locomotor activity among control, sesame and flaxeed groups. But it has been shown a significant increase in latency to immobility (p=0.027) and decrease in total immobility (p=0.001) in flaxseed oil group compared to control group. Also sesame oil group showed a significant reduction in the duration of total immobility (p=0.027) and its latency to immobility wasn’t significant. There were no significant differences in latency to seizure and death time in flaxseed oil groups compared to the control group. The subchronic consumption of sesame oil significantly increased the death time than the control group (p=0.04) but the latency to seizure was not significant. The results reveal that sesame and flaxseed may be considered as a food adjuvant for attenuating emotional problems in epilepsy.