Ischemic stroke is one of the leading causes of mortality and morbidity in the world and effective neuroprotectants are yet to be developed. Recent studies have demonstrated excellent neuroprotective effects of a bivalent enkephalin opioid agonist, biphalin in multiple stroke models.The purpose of this study is to evaluate novel multifunctional enkephalin-fentanyl opioid agonists, LYS436, LYS739 and LYS416 for their neuroprotective potential using in vitro and in vivo ischemic stroke models and to compare the effect to that of biphalin.In general, all non-selective opioid agonists significantly decreased neuronal cell death and levels of reactive oxygen species in primary neurons subjescted to hypoxia-aglycemia/re-oxygenation or NMDA neurotoxicity. Fluorinated enkephalin-fentanyl conjugate, LYS739 showed enhanced neuroprotection in both in vitro models compared to biphalin. Based on further in vitro screening and comparative studies to biphalin, LYS739 was selected as a lead for in vivo experimentation. A mouse middle cerebral artery occlusion (MCAO) stroke model was utilized to study biphalin and the lead analog, LYS739. Both agonists significantly decreased brain infarct and edema ratios compared to saline treated group. Neurological impairment after stroke was statistically significantly improved in terms of neurological score and locomotor activities with LYS739 and biphalin treatment. Importantly, LYS739 and biphalin demonstrated better neuroprotection compared to fentanyl, and this effect was reversed by non-selective opioid antagonist naltrexone.In summary, the results of this study suggest that the multifunctional fluorinated enkephalin analog, LYS739 can be considered as a potential lead for ischemic stroke research and may provide advantages given the multimeric peptide-opiate structure.
Introduction: Inflammation is a major cause of arthritis. Since the conventional medicines used for the treatment of this disease have many side effects, herbal remedies can be proved to be effective in this case. So, the present study was aimed at investigating the quantitative detection of phytochemicals, screening of in vivo anti-inflammatory and the possible anti-arthritic activities of the crude methanol extracts of a traditional medicinal plant Macropanax dispermus leaves (MDML) and stem barks (MDMS). Methods: Quantitative screening of phytochemical constituents was analyzed by standard procedures. The in vivo anti-inflammatory activity was conducted on Swiss albino mice by using carrageenan and formalin-induced paw edema tests, and xylene-induced ear edema test. The possible anti-arthritic activity was done by evaluating the in vitro inhibition of bovine serum albumin (BSA) denaturation. Results: The current research showed that MDML contained a considerable amount of flavonoids and alkaloids, and MDMS contained a considerable amount of phenols. MDMS (200, 400 mg/kg) was observed to be an effective and significant (P < 0.001) peripheral anti-inflammatory agent in carrageenan and formalin-induced paw edema tests, whereas MDML (400 mg/kg) was observed to have an effective and significant (P < 0.001) neurogenic anti-inflammatory effect in xylene-induced ear edema test as compared to the negative control group. MDMS was observed to be an effective anti-arthritic agent as compared to that of the negative control group. All those effects were dose and concentration-dependent.Conclusion: The present research proved that MDML and MDMS were effective medications for the treatment of inflammation and arthritis.
Hylocereus polyrhizus (Red dragon) fruit, a Cactaceae plant with traditional and medicinal uses, is found in America and South Asia. These fruits have diversified bioactive components, which make them both therapeutically and nutritionally important. This review focuses on the various aspects of this potential plant. This literature review looked at the nutritional information, botanical description, traditional medical use, nutritional values, medicinal uses, chemical compounds, and pharmacological activities of H. polyrhizus. To evaluate the required resources, Scopus, PubMed, Science Direct, Cochrane electronic databases, and Google Scholar search engines were searched (for example, Hylocereus polyrhizus OR dragon fruit, red pitaya OR pitaya, pharmacological AND phytochemical, nutritional AND ethnomedicinal). Prominent bioactive elements in this plant included phenolic compounds such as α-amyrin (15.87%) and β-amyrin (13.90%). H. polyrhizus also contains antioxidant, cardioprotective, anti-inflammatory, antifungal, antibacterial, hypolipidemic, antiviral, thrombolytic, antiplasmodial, anticancer, hepatoprotective, and antidiabetic activities. Because of its colouring pigments, carbohydrates, proteins, and fat substitution properties, the fruit is commonly used in culinary and grooming. An improved understanding of H. polyrhizus, according to this study, could pave the way for the discovery of new, beneficial chemicals with therapeutic potential.
Background: Exercise promotes cardioprotective benefits for the adult heart; however, the exercise-induced molecular and microstructural remodeling processes have yet to be fully characterized. This study sought to define the spatial interactions between molecular and microstructural remodeling that are induced by exercise and might result in cardiac protection by evaluating regional correlations of expressed cardiac CITED4, a transcriptional co-regulator previously shown to increase in hearts with exercise, and myocardial architecture mapping with diffusion tensor cardiac MRI (DT-CMR). Methods: In the first cohort, male wild-type C57BL/6J mice were housed with or without free access to a running wheel. In the second cohort, CITED4 cardiomyocyte specific knockout (KO) mice were generated along with control littermates (fl/fl mice) and the methods were repeated. After 8-weeks of voluntary wheel running, the mice were euthanized and their hearts were excised, scanned at 14.1 T MRI, and sectioned. RNA Fluorescent in situ hybridization (RNA-FISH) was used to detect CITED4 and all slides were counterstained with DAPI. All experiments were performed under approval of the IACUC of the Massachusetts General Hospital. Results: The exercised group of cohort 1 showed a significant increase in CITED4 expression and microstructural DT-CMR markers in the lateral wall of the left ventricle (p<0.05 for all). In particular, myofiber orientation, evaluated as helicity (helix angle transmurality), was significantly increased within the exercised group (p<0.05), indicating beneficial changes in the myocardial microstructure. Cohort 2 demonstrated that CITED4 was required for these changes to take place, as the CITED4 knock out exercise group did not replicate the same structural changes seen in cohort 1, while the fl/fl control mice reproduced the expected changes in tissue microstructure following exercise. Conclusion: Exercise induces a regional increase in CITED4 expression that coincides with microstructural remodeling. In addition, we have demonstrated that CITED4 is required for these beneficial exercise-induced microstructural changes to occur.
The present study was undertaken to investigate some organic phytochemicals, fatty acids, toxic metals and evaluate lipidemic and antidiabetic activity of a herbal medicine and its one constituent Syzygium cumini seed.Antidiabetic and lipidemic activity of this medicine and seed extract was studied on streptozotocin induced type 2 diabetic model rats.From chemical investigation carbohydrates and steroids were present in both samples.Alkaloid was present in herbal medicine sample only.Arsenic was found to be 0.05 ppm which was less than the tolerance level.Other toxic metals Lead, Copper, Cadmium and Manganese were absent in herbal medicine (HM-01).Myristic, palmotelic, palmitic, linoleic, oleic, stearic and arachidic acids were found in both samples.The rats were divided into 4 groups (n = 6 in each group): a) Water control b) Glibenclamide c) PESE d) HM-01.The parameters measured were: serum glucose and serum lipid profile.Oral consumption of HM-01 and PESE for 22 days caused significant (plasma glucose in mmol/L, Mean ± SD; 8.57± 1.09 vs 5.67 ± 0.45; and 8.91 ± 0.9 vs 5.56 ± 0.7 respectively, on the 1 st day vs 22 nd day; **p < 0.005) reduction of fasting serum glucose level.HM-01 and PESE treated groups decreased total cholesterol level by 25% and 23%; triglyceride by 24% and 28%; LDL cholesterol by 34% and 35%; and increased HDL cholesterol by 14% and 22% respectively.The herbal medicine and its constituent Syzygium cumini seed powder possess antidiabetic properties in type 2 diabetic model rats. INTRODUCTION:According to WHO, about 2.8% of the world population and 6% of the people of Bangladesh are suffering from diabetes mellitus.Diabetes mellitus (DM) is one of the most prevalent and devastating chronic noncommunicable diseases having serious health, economic and social consequences (IDF, 2006).
Swietenia mahagoni is a tropical ever-green hardwood timber species of Meliaceace family. In recent years increasing number of Bangladeshi people are using the Mahagoni seeds for the management of diabetes. The aim of the investigation was to evaluate the antidiabetic activity of Sm-SEF7 fraction of seeds from the plant Swietenia mahagoniinstreptozocin induced diabetic rats. Diabetes was induced by a single dose of intraperitoneal injection of streptozocin (90 mg/kg) in Long-Evans rats. Glibenclamide (5 mg/kg) was used as a standard antidiabetic agent. The result indicated that after oral ingestion of Swietenia mahagoni for 21 days in diabetic rat, a significant plasma glucose lowering effect (plasma glucose in mmol/l, Mean ± SD; 8.81 ± 1.22 vs. 3.57 ± 3.38, on the 1st day vs. 22nddays,p = .002) was improved. It also enhanced insulin releasing activity (plasma insulin in ng/ml, Mean ± SD: group 1 vs. group 3, 0.54 ± 0.13 vs. 0.93 ± 0.19; p=0.001) was significantly higher in the Sm-SEF7 treated type 2 rats (group 3) than in water treated control group (group 1). But there was no change in lipid level after 21 days fraction feeding on type 2 model rats. The results indicated that, nontoxic Sm-SEF7 fraction of Swietenia mahagoni seed possesses antidiabetic properties in type 2 diabetic model rats. It seems to act as an insulonomimetic and/or insulin sensitizing agent.
Cynodon dactylon (Poacae) is a well known traditional plant used as a folk remedy in treatment of many symptoms and diseases like cramps, measles, tumors, wounds, warts, fever and rheumatic affections. In this study, the antimicrobial activity of the plant crude extract from three different extraction (hot and cold aqueous extraction, methanol extraction) was investigated against some of the gram positive bacteria (Staphylococcus epidermidis, Bacillus cereus) and gram negative bacteria (Escherichia coli, Pseudomonas aeroginosa, Salmonella typhi, Shigella dysenteriae) using disc diffusion method. Amoxicillin was taken as positive control. The diameter of the clear zone of inhibition surrounding the disc was measured. The aqueous extract of Cynodon dactylon had antimicrobial activity against all the test organisms indicating broad spectrum activity of the extract for both gram positive and gram negative bacteria. No clear zone formed with methanol extract. It can be concluded that aqueous extract of whole plant of Cynodon dactylon may be considered as an antibacterial agent and can be used to source antibiotic substances for possible treatment of bacterial infections. Keywords: Cynodon dactylon, antimicrobial, aqueous extract, disc diffusion
Objective: This study aims to uncover the anti-diarrheal, antioxidant, thrombolytic, and anthelmintic activities of methanol extract of A. solanacea (ASME) and its soluble n-hexane fraction in methanol (ASNH).Materials and Methods: The phytochemical assessment of this plant was performed by using the standard method. The anti-diarrheal property was screened by castor oil induced diarrhea in Swiss albino mice and plant extract was administered into mice by oral gavage. The antioxidant property was being investigated by two different in vitro methods such as ferric reducing effect assay and superoxide scavenging activity assay. The thrombolytic activity was evaluated by in vitro clot lysis procedure, and the anthelmintic study was carried out on earthworm Pheretima posthuma.Results: In castor-oil induced diarrhea, ASME and ASNH induced a significant decrease (**P
