Cardiovascular and Hematological Agents in Medicinal Chemistry最新文献

Background: Chronotherapeutics, the drug delivery based on circadian rhythm, is recently gaining much attention worldwide. Various diseases like asthma, hypertension, and arthritis show the circadian variation that demands time scheduled drug release for effective drug action. Therefore, the pulsatile drug delivery system has been designed to confer preprogrammed drug delivery.

Objective: In the present study, a '3 Cap' pulsatile drug delivery system has been developed, optimized, and characterized in order to achieve the floating and pulsatile release of ramipril.

Methods: An optimal response surface design was employed to investigate the effect of isopropanol: formaldehyde vapors for varying time on drug release from the capsules. '3 Cap' pulsatile drug delivery system was evaluated in terms of floating time, density, the effect of gastric flow rate, and type of dissolution apparatus on drug release.

Results: Independent variables exhibited a significant effect on the drug release of the prepared formulations. Results showed that time between the release of fractions of dose increased with an increase in formaldehyde: isopropanol ratio and duration of exposure to formaldehyde vapors with no effect of gastric flow rate.

Conclusion: The results of the designed system revealed that an optimum exposure of 1:2 of isopropanol: formaldehyde vapors for sixty minutes resulted in the desired release of second pulse of dose after a predetermined lag time of 5 hours as desired. '3Cap' system was successful in achieving floating and pulsed release of hypertensive drug opening a 'new lease of life' to the existing drug molecule.

Introduction: Acute porphyrias cause life-threatening attacks of neurovisceral non-specific symptoms, so this condition mimics many acute medical and psychiatric diseases. The disease is very misdiagnosed, probably due to its low incidence and non-pathognomonic symptoms, this delays the effective treatment onset. Early diagnosis and treatment highly improve the prognosis and can prevent the development of neuropathic manifestations.

Methods: We assembled a systematic review, following the PRISMA guidelines and using Pubmed as our database. Our aim was to show some peculiarities among patients that present neurological manifestations in acute porphyria attack. We obtained the patients' age, sex, clinical presentation, eurological manifestations and porphyria type of 16 patients. We also evaluated the time between symptoms onset and neurological manifestations. The average age was 28,4 ± 11,1; 50% of patients were male.

Results: AIP was the most prevalent porphyria type. The average time between symptoms onset and neurological manifestations was of 9,53 ± 11,6 days. Abdominal pain; nausea and vomiting and psychiatric manifestations were the most common symptoms preceding neurological attacks. Seizures and consciousness disturbance were the most prevalent findings within an attack. We also presenting a case to illustrate how difficult this diagnosis can be.

Aims: The study aimed to evaluate the antihyperlipidemic and antioxidant activities of Matricaria pubescens.

Background: Matricaria pubescens (Desf.) Shultz belongs to Asteraceae family and it is commonly used traditionally for handling diabetes mellitus.

Objective: The objective of this study was to assess the antioxidant activity of Matricaria pubescens (Desf.) Shultz and its effect on lipid and lipoprotein profile in normal and streptozotocin-induced diabetic rats.

Methods: The effect of repeated (7 days of treatment) oral administration of the aqueous extracts of aerial part of Matricaria pubescens (MPAE) at a dose of 40 mg/kg on lipid and lipoprotein profile was examined in normal and streptozotocin-induced diabetic rats. Furthermore, a preliminary phytochemical screening and the quantification of phenolic, flavonoid and tannin contents as well as the antioxidant activity using two methods (FRAP and ABTS) were carried out.

Results: MPAE demonstrated a potent antidyslipidemic effect in diabetic rats by reducing serum levels of triglycerides, total cholesterol and Low-Density Lipoprotein (LDL). In addition, the results showed that the extract is rich in several phytochemical compounds and revealed an important antioxidant activity.

Conclusion: In summary, this study proved that Matricaria pubescens (Desf.) Shultz. has a favorable effect on diabetic dyslipidemia.

Background: Diabetic Cardiomyopathy (DCM) has an adverse effect on health and occurs with or without concurrent vascular disease. Although several pathological mechanisms have been implicated in DCM, oxidative stress is widely thought to be the foremost cause for DCM pathogenesis.

Objective: In this review, we focused on the role of bioactive compounds from different sources such as plant and marine products in cardiomyopathy.

Results: Natural Products (NPs) and their constituents were traditionally considered implausible as therapeutic agents. In the last few decades, studies on the use of NPs in the pharmaceutical field have reduced due to problems such as the requirement of compatibility of conventional NP extract libraries with high-throughput selection. The characteristics of NP structures such as high chemical variety, biochemical specificity, and other molecular properties that make them favorable as direct structures for drug synthesis and that distinguish them from combinatorial and synthetic compound libraries have been documented since ancient times.

Conclusion: Consequently, the aim of this review was to provide an overview on the recent progress and development of bioactive compounds in DCM and to focus on the cellular mechanisms underlying cardiomyocyte dysfunction in their therapeutic targets.

Stevia rebaudiana of the Asteraceae family is a perennial shrub. It is a sweetener herb also known as sweet weed, sweet leaf, sweet herbs and honey leaf, native to Argentina, Brazil and Paraguay. The leaves of stevia are sweeter than sucrose with zero calories. Steviol, a diterpenoid glycoside derivative identified from this plant, is sweeter than sucrose and is safe when used as a sweetening agent. Diabetic and obese people with hyperglycemia who are in a condition to follow a strict diet can use stevioside as an alternative sweetener. In addition to its hypoglycemic property, the plant also exhibits antibacterial, anti-inflammatory, hypotensive, antiseptic, diuretic, anti-fertility and cardiotonic properties. It has also been documented to show good effects on treating skin diseases such as dermatitis, acne, eczema etc. The leaves of stevia with enriched phytoconstituents could be an alternative natural sweetener for children, adults and old age persons who have a craze to drink beverages and eat sweetened food products in their habitual life.

Background: This study determined the effect of Biochanin A (BCA) on isoproterenol (ISO) induced Myocardial Infarction (MI) in male Wistar rats.

Methods: Animals (weighing 150-180 g) were divided into four groups, with six animals in each group and pretreated with BCA (10mg/kg Body Weight [BW]) and ɑ-tocopherol (60mg/kg BW) for 30 days; and ISO (20mg/kg BW) was administrated subcutaneously on the 31st and 32nd day.

Results: ISO-induced MI rats demonstrated the significant elevation of serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, lactate dehydrogenase, creatine kinase-MB and cardiac troponin; however, concomitant pretreatment with BCA protected the rats from cardiotoxicity caused by ISO. Activities of antioxidant enzymes, such as superoxide dismutase, catalase, glutathione peroxidase, glutathione-S-transferase and glutathione reductase significantly reduced in the heart with ISO-induced MI. Pretreatment with BCA produced a marked reversal of these antioxidant enzymes related to MI-induced by ISO.

Conclusion: In conclusion, this study suggested that BCA exerts cardioprotective effects through modulating lipid peroxidation, enhancing antioxidants, and detoxifying enzyme systems.