INTRODUCTION:The polyol pathway is responsible for the metabolism of almost one-third of the total glucose in people with chronic diabetes. Moreover, it causes complications in organs that rely on aldose reductase (AR) as an enzyme. The purpose of this research was to examine the in vitro and in vivo effects of a flavonoid-rich ethyl acetate fraction of a methanolic extract of Ficus carica Lam. leaves (FCEA) on the aldose reductase gene AKR1B1. The complicated relation of AR for target confirmation and analysis of the flavonoids of FCEA, quercetin, kaempferol, and chrysin was explored by building a flavonoid-protein complex network utilizing GeneCards®, String, and Cytoscape Networking. METHODS:The examination of ADMET was carried out after docking on the active sites of AR. By the binding and scoring abilities, the analysis was carried out. The ADMET characteristics demonstrated that these flavonoids had excellent solubility, absorption, and oral bioavailability, and the results demonstrate that they have potential. An additional in-vivo investigation was conducted on rats using a model induced by streptozotocin (STZ). Hence, upon induction, the rats' sciatic nerves were removed and prepared for an RT-PCR analysis of the AKR1B1 gene. RESULT:Compared to the diabetic normal group and the metformin group, rats treated with FCEA had lower levels of messenger RNA and AKR1B1 gene expression. CONCLUSION:This proves that FCEA has effectively blocked AR. It is highly likely to suggest FCEA as a potent aldose reductase inhibitor, as it considerably reduces the mRNA level of AKR1B1 gene expression in the sciatic nerve of sick rats, according to a combined bioinformatics prediction and RT-PCR analysis.
Background: Neuropathy can be induced in rats by peripheral injuries, depending on compression of complete or a section of sciatic nerve and chemically by Streptozotocin (STZ). Materials and Methods: In the present study neuropathic pain were induced in rats by two methods, chronic constriction injury (surgical model) and STZ (40mg/kg/i.p.) induced diabetes (drug induced model). In both the models, behavioural as well as markers of oxidative stress were studied. Behavioural parameters were tested using vonfrey hair and Randall Selitto analgesiometer whereas biochemical parameter includes glycosylated haemoglobin and markers of oxidative stress. The study was further supported by histopathology of sciatic nerve. Flavonoid rich extract of Allium cepa Lam. leaves was administered at three different doses viz. 25, 50 and 100mg/kg/p.o to the rats with neuropathic pain. Both the models of neuropathic pain showed significant alteration in behavioural as well as oxidative stress parameters. Results: Treatment of Allium cepa leaves extract showed dose dependent improvement in behavioural and biochemical parameters towards normal (p value <0.001, <0.05 and <0.01). The altered histopathological changes in sciatic nerve were also significantly improved as compared to rats with neuropathic pain. Conclusion: The neuroprotective effects of the Allium cepa leaves extract is a virtue of its strong antioxidant activity.
Background: Flavonoids, a group of polyphenols responsible for protective role against many diseased conditions, provide antioxidant activity which is the reason for their medicinal properties. Tactile allodynia is a behavioral biomarker of neuropathy that is well estimated by von Frey filaments and Randall–Selitto test. Objective: Ficus carica Lam. leaves were studied for the conformation of flavonoids in ethyl acetate fraction of methanolic extract (FCEA) using GC-HRMS for the identification of flavonoids. It was analyzed for antioxidant activity by in vitro free radical scavenging activity, performed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) followed by blood glucose-level estimation, evaluation of neuropathic pain, and kidney and liver function tests in diabetic rats. Materials and Methods: The shade-dried leaves of F. carica Lam. were extracted with methanol and after that fractionated using ethyl acetate (FCEA). The characterization of FCEA was established using GC-HRMS. In vitro free radical scavenging activity was performed using DPPH assay. Diabetes was induced using streptozotocin (40 mg/kg/intraperitoneally), and effects of FCEA were studied on blood glucose level, neuropathy markers, and liver and kidney functions of diabetic rats. Results: GC-HRMS results highlighted the presence of quercetin, kaempferol, and chrysin in FCEA with free radical scavenging activity of 78.35% and IC50 value of 5.508 μM. FCEA reduces glucose levels and also shows protective effects in case of diabetic neuropathy as it increases the threshold of withdrawal latency in tactile allodynia and also decreases the serum glutamic-oxaloacetic transaminase, serum glutamic-pyruvic transaminase, blood urea nitrogen, and creatinine levels. Conclusion: The protective effects of FCEA against diabetic neuropathy, hepatoprotective and nephroprotective effects might be due to strong antioxidant property of important flavonoids present which is confirmed in the study.
Flavonols aglycones are well established in plant extracts with omnipresence of common flavonols like kaempferol, quercetin and myricetin. Quercetin has been reported for various pharmacological activities with major ones in the field of inflammation, cancer, arthritis, diabetes and its complications. Leaves of plants selected for this study viz. Allium cepa L., Ficus carica L. and Ziziphus mauritiana L. reported to have antioxidant, anticancer, hypoglycemic activities. It is hypothetised thisactivities are due to flavonoids present in these plants. Hence the ethylacetate fraction of methanolic extract of these leaves was obtained as it provides flavanoid rich fraction and the samples were prepared and HPTLC analysis was performed against standard quercetin and their quantitative analysis was performed, the solvent system toluene: ethyl acetate: formic acid (9: 1: 0.5) was selected. It was observed that these plants shows presence of quercetin where A. cepa has highest concentration with F. carica and Z. mauritiana having quercetin in declining order. The calibration curve was linear in the range of 0.1 to 0.7 μg for quercetin. Further a correlation coefficient of 0.999 indicates good linearity between concentration and area. Thus, it was proved that the plants used in the study has presence of quercetin which is possibly the reason having the pharmacological uses.
Objective: Antioxidant potential has protective effects in diabetic neuropathy (DN); hence, the present study was designed with an objective to quantify quercetin from shade-dried leaves of Allium cepa Lam. and to study its effects on streptozotocin (STZ)-induced chronic DN. Materials and Methods: The shade-dried leaves of A. cepa Lam. were extracted with methanol and then fractionated using ethyl acetate (ACEA). The quantification of quercetin in ACEA was evaluated by high-performance thin layer chromatography (HPTLC). The STZ (40 mg/kg) was administered to Sprague-Dawley rats (180-250 g) maintained at normal housing conditions. The STZ was administered once a day for 3 consecutive days. The elevation in blood glucose was monitored for 3 weeks periodically using flavin adenine dinucleotide-glucose dehydrogenase method by Contour TS glucometer. Rats showing blood glucose above 250 mg/dl were selected for the study. Animals were divided into eight groups. ACEA (25, 50, and 100 mg/kg), quercetin (40 mg/kg), metformin (120 mg/kg), and gabapentin (100 mg/kg) were given orally once a day for 2 weeks. The blood glucose level was again measured at the end of treatment to assess DN. Thermal hyperalgesia, cold allodynia, motor incoordination, and neurotoxicity were studied initially and at the end of 2-week treatment. Biochemical parameters were also evaluated after 2-week drug treatment. Results: The quercetin present in ACEA was 4.82% by HPTLC. All the ACEA treatment reduces blood glucose level at the end of the 2-week study and shows a significant neuroprotective effect in STZ-induced DN in the above experimental models. Conclusion: The quercetin present in ACEA proved protective effect in STZ-induced DN.
The aim of current review was to elaborate the osmotic drug delivery system for controlled release of drugs. The oral route is the most common and most acceptable route of drug administration. For treatment of chronic diseases repeated dose administration is required, the osmotic drug delivery system serve as a tool for control release of drugs in these condition and avoid the repeated administration. The present review illustrates the basics of osmotic drug delivery system, types with special focus on controlled porosity osmotic pump, mechanism of osmosis, ideal drug candidate, formulation techniques, various osmotic agents, pore formers, coating materials and marketed preparation based on osmotic drug delivery system. These parameters may be helpful in designing of dosage for modification in release of various drugs having problem in conventional form.
INTRODUCTION Diabetes mellitus is a wide spread disorder, which has long been in the history of medicine [1]. Report of ethnobotany suggested that about 800 medicinal plants possess antidiabetic potential [2] and the bioactive compounds such as glycosides, alkaloids, terpenoids, carotenoids and flavonoids are effective drugs both in preclinical and clinical studies [3-4]. It has been estimated that, about 1.3 % of the world population suffer from this disease. But, most of the hypoglycemic agents and hypolipidemics used in allopathic practice to treat diabetes mellitus and hyperlipidemia are reported to have side
In the present study, we investigated the effects o f n-butanolic fraction of methanolic extract of lea ves of Ziziphus mauritiana, Lam (BZM 10, 25 and 50 mg/kg) on learni ng and memory in mice using Elevated Plus Maze, Pas sive avoidance Paradigm and Object recognition test. Pir acetam was used as standard drug. The acute toxicit y study shows no mortality up to BZM 2000 mg/kg. Decrease i n the transfer latency reported with the treatment of BZM on the elevated plus maze after 24 hrs. and on day-7 a nd it expressed as inflexion ratio (IR). Significan t increase in step down latency was observed on passive avoidance para digm. The object recognition test report increase i n Recognition Index (RI) indicates its nootropic effe ct. No neurotoxicity observed with all dosage using rota-rod method. BZM 25 mg/kg also antagonises the amnesia pby scopolamine and hence indicates involvem ent of central cholinergic mechanism in its effect. Hence, the present study proved nootropic effect of n-but anolic fraction of methanolic extract of leaves of Ziziphus mauriti ana.