Calotropis gigantea- A Review

Calotropis gigantea plant has a family Asclepiadaceae commonly and sub family Apocynaceae known as Madar in Hindi. It is a perennial herb with a very long history of use in traditional medicines. Calotropis gigantea is a hoary, laticiferous shrub, which is also known as “the milkweed”. Calotropis is used as a traditional medicinal plant in whole world. Calotropis gigantea plant contain chemical constituents in which cardenolides, flavonoids, terpenes, pregnanes and nonprotein amino acid and more in various concentration. The root bark contains α-amyrin, β-amyrin, taraxasterol and its ψ-isomer taraxasteryl isovalerate, taraxasteryl acetate, gigantin, giganteol, isogiganteol, β-sitosterol and wax. The rootalso shows Nootropic activity in methanolic extract. The latex, leaves, flowers and bark are used as caustic, acrid, expectorant, to removes body hairs, anthelmintics and alsoused in leprosy, ulceration, cough, scabies ring worm of the scalp, piles, explosion on the body, asthma, enlargement of spleen or liver, edema and in painful joint swellings. Also, evaluate possible anxiogenic effect, sedative action and anxiolytic potential of crude ethanolic extract of Calotropis gigantealeaf. Methanolic extract of Calotropis gigantea root used as memory increasing activity. This review gives an idea about its pharmacological activity and phytochemistry.

Evaluation of Nootropic Activity of Leaf Extract of Anacardium occidentale L.

One of the plants that have been used for enthno medicinal purposes in traditional civilization is Anacardium occidentale L. of the family Anacardiaceae is native to Brazil also found in tropical countries such as Malaysia and India commonly known as cashew. The purpose of this study is to determine the in-vitro and in-vivo cognitive effects of an ethanolic leaf extract of the herb Anacardium occidentale on albino rats. Orally the ethanolic extract was administered in two doses (100 mg/kg and 400 mg/kg). The Elevated Plus maze and Y-maze showed statistically significant improvement in the memory process. The estimation of acetylcholinesterase enzyme in rats brain also shows improvement in the memory process by reducing acetylcholinesterase activity. Disorders related to cognition are one of the major health problems and increasing day by day especially affecting the elder individual. There is no proper medication for the impairment of memory. The study reveals that the ethanolic extract of the leaf of Anacardium occidentale has dose-dependent memory-enhancing performance. Synthetic drugs have a lot of side effects, whereas drugs belongs to natural substances have least side effect compared to synthetic one, which has gained a lots of importance. These studies need to be documented effectively. Research findings were contributed to meet the future needs in general healthcare, research, and conservation of endangered species and may give a lead to the discovery of newer drugs.

Formulation and optimization of water soluble granules of Withania Somnifera

Herbal medicines have great demand in the treatment of various kinds of illness. Ayurvedic system of medicine has consisted of many herbal sources in which ashwagandha one of them which are the very popular herbal sources. Many literature surveys suggest that ashwagandha is used as an immunomodulator, tranquilizer, antioxidant, antidiabetic, and nootropic activity. Present research work explored the potential benefit of ashwagandha by designing suitable granules of its water extract. Further, it is characterized by various parameters and In-vitro drug release Keywords: Immunomodulator, Tranquilizers Ayurvedic, Ashwagandha, Granules

ATTENUATION OF STRESS INDUCED URINARY BIOCHEMICAL CHANGES AND SCOPOLAMINE-INDUCED MEMORY LOSS BY HYDROALCOHOLIC SEED EXTRACT OF CELASTRUS PANICULATUS WILLD. IN RAT MODEL

Ayurveda uses seeds of Celastrus paniculatus to treat various stress related disorders. In the present investigation, the hydroalcoholic seed extract of C. paniculatus was evaluated for anti-stress activity by forced swim stress model. Vanillylmandelic acid and ascorbic acid were selected as non-invasive biomarkers to assess the anti-stress activity. Nootropic activity in rats was evaluated by conditioned avoidance response using Cook’s pole climbing apparatus, the antioxidant potential was determined based on the ability of the extract to scavenge hydroxyl radicals. Pretreatment with the extract significantly (p < 0.05) inhibited the stress induced urinary biochemical levels. The cognition was observed to be dose dependent. The extract also produced significant dose dependent inhibition of hydroxyl radicals. The present study provides scientific support for the anti-stress, antioxidant and nootropic activities of hydroalcoholic seed extract of C. paniculatus and substantiates the traditional claims for the usage of C. paniculatus willd. in stress induced disorders.

Phytochemistry and pharmacology of Celastrus paniculatus Wild.: a nootropic drug

Objectives Celastrus paniculatus Wild is an evergreen climbing shrub. The plant is of great significance in the traditional Indian System of Medicine, such as Ayurveda, Unani, and Siddha. The seeds and their oil are extensively used to treat neurological disorders such as cognitive dysfunction, paralysis, epilepsy, insomnia, and other ailments like rheumatism, arthritis, sciatica, and leprosy. This paper aims to highlight the nootropic activity of C. paniculatus and explore its phytochemistry, traditional uses, and other pharmacological activities. Methods All available information concerning C. paniculatus has been searched in the internationally accepted scientific databases, including PubMed, ScienceDirect, Scopus, and Google Scholar. Additional knowledge was gathered from the classical Textbooks and Unani Pharmacopoeia. Results C. paniculatus is a rich source of several secondary metabolites, such as β-Dihydroagarofuranoids sesquiterpenes, alkaloids (Celastrine, Celapanin, Celapagin, and paniculatin), flavonoids, terpenoid (β-amyrin, Lupeol, Pristimerin), sterols (β-sitosterol, campesterol, stigmasterol, α-tocopherol, γ-Tocopherol), fatty acid (palmitic, stearic, oleic, linoleic, linolenic acids) and non-fatty acids (Benzoic acid, Cinnamic acid). The various study shows that the extracts and active constituent of this plant possess potent nootropic activity. Besides nootropic activity, it has also been reported for anti-Alzheimer, anticonvulsant, antidepressant, antioxidant, analgesic, anti-inflammatory, antiarthritic, gastroprotective, anti-psoriatic, wound healing, antibacterial, antimalarial, and several other properties. Conclusions Several in vitro and in vivo trials confirm the conventional use of C. paniculatus in cognitive dysfunction. However, the relations between the possible mechanisms of other activities and traditional uses of the C. paniculatus remain indistinct. Still, pharmacological studies also explored the effects of C. paniculatus, which were not recognized in ancient times, such as cytotoxic, ACE inhibitor, and antidiabetic activities. These discoveries are may be beneficial in the development of the new drug to treat various diseases. It is also confirmed that the β-dihydroagarofuranoids exhibit significant AChE inhibitory, cytotoxic, antibacterial, and insecticidal effects. This versatile medicine is truly a life elixir. Considering the therapeutic importance of the C. paniculatus and the absence of any reported clinical studies, extensive clinical trials are needed to explore its memory enhancing and other activities.

MOLECULAR DESIGN OF N-ACYL DERIVATIVES OF 2-(2-OXOPYROLIDIN-1-YL)-ACETAMIDE WITH GABA-ERGIC AND GLUTAMATERGIC ACTIVITIES

The first of the most successfully implemented nootropic drugs in medical practice is piracetam, which should be attributed to cyclic derivatives of gamma-aminobutyric acid. The production of new piracetam derivatives with high nootropic activity is a promising direction in the development of new neuroprotective drugs.The aim of the study is to predict GABA-ergic and glutamatergic activities of N-acyl derivatives of 2-(2-oxopyrolidin-1-yl)- acetamide by a molecular docking method through the energy analysis of interaction of modeled structures with GABAA and AMPA receptors with their subsequent targeted synthesis.Materials and methods. The objects of the research are new N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide and a virtual model of the GABAA receptor of the Homo sapiens organism with the identification code 6D6U and a three-dimensional model of the AMPA-receptor of the Rattus norvegicus organism with the identification code 3LSF from the RCSB PDB database. The simulated compounds were designed in the HyperChem 8.0.8 program. This program was also used to optimize geometry using the force field of molecular mechanics MM+. Molecular docking was carried out using the Molegro Virtual Docker 6.0.1 program. The preparation of N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)-acetamide was carried out by the interaction of 2-(2-oxopyrrolidin-1-yl)-acetamide with an excess of the corresponding anhydride under conditions of acid catalysis.Results. Based on the results of molecular docking, a high affinity of all simulated compounds for the binding site of GABAA and AMPA receptors can be estimated. According to the predict, the maximum GABA-ergic activity should be expected for (N-[2-(2-oxopyrrolidin-1-yl)-acetyl]-butyramide. N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide form a more stable complex with amino acid residues Arg207, Phe200, Thr202, Tyr97, Tyr157, Tyr205 and Phe65 of the GABAA receptor binding site than the GABA molecule. In terms of the minimum interaction energy, the N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)- acetamide are superior to a number of known ligands such as GABA, piracetam, anipiracetam, picamilon and pramiracetam. The tested compounds have also shown a high affinity for the binding site of the AMPA receptor. The leader compound is also the compound PirBut, as in the case of the GABAА receptor.Conclusion. Molecular modeling of the ligands interaction with the active binding site of gamma-aminobutyric acid of the GABAA receptor by molecular docking showed that all virtual N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide can exceed a number of nootropic drugs by activity. In the course of molecular design, a method for predicting a glutamatergic activity for 2-pyrrolidone derivatives has been developed. It suggests a significant nootropic activity for N-[2-(2-oxopyrrolidin-1-yl)- acetamide amides.

Biomolecular Evaluation of Lavandula stoechas L. for Nootropic Activity

Lavandula Stoechas L. is widely known for its pharmacological properties. This study was performed to identify its biomolecules, which are responsible for enhancement of memory. L. stoechas aqueous extract was first purified by liquid column chromatography. The purified fractions were analyzed for in vitro anti-cholinesterase activity. The fraction that produced the best anti-cholinesterase activity was named an active fraction of L. stoechas (AfL.s). This was then subjected to GC–MS for identifications of biomolecules present in it. GC–MS indicated the presence of phenethylamine and α-tocopherol in AfL.s. Different doses of AfL.s were orally administered (for seven days) to scopolamine-induced hyper-amnesic albino mice and then behavioral studies were performed on mice for two days. After that, animals were sacrificed and their brains were isolated to perform the biochemical assay. Results of behavioral studies indicated that AfL.s improved the inflexion ratio in mice, which indicated improvement in retention behavior. Similarly, AfL.s significantly (p < 0.001) reduced acetylcholinesterase and malondialdehyde contents of mice brain, but on the other hand, it improved the level of choline acetyltransferase, catalase, superoxide dismutase, and glutathione. It was found that that high doses of AfL.s (≥400 mg/Kg/p.o.) produced hyper-activity, hyperstimulation, ataxia, seizures, and ultimate death in mice. Its LD50 was calculated as 325 mg/Kg/p.o. The study concludes that α-tocopherol and phenethylamine (a primary amine) present in L. stoechas enhance memory in animal models.

Antidepressant and nootropic activity of aqueous extract of Bougainvillea glabra

The aim of this analysis was to assess antidepressant & nootropic capacity of Bougainvillea Glabra aqueous extract (BGAE). Forced swim test, tail suspension test, & tetrabenazine mediated catalepsy & ptosis models were used to assess BGAE's antidepressant efficacy in mice at doses of 250 & 500 mg/kg orally. Morris water maze with elevated plus maze (EPM) was used to test nootropic behaviour. Normal medications for antidepressant & nootropic function were imipramine (25 mg/kg) & piracetam (300 mg/kg), respectively. Antioxidant assays such as DPPH & TBARS were used to validate antidepressant & nootropic function. When comparison to car, pre-treatment with BGAE resulted in substantial dose-dependent decrease in immobility time in both FST & TST. (P0.005) Tetrabenazine-induced catalepsy & ptosis were both decreased dramatically. Furthermore, in MWM & EPM, BGAE demonstrated dose-dependent cognitive enhancing behaviour. In DPPH assay, BGAE had IC50 of 17.39 g/ ml, & in TBARS assay, it had IC50 of 398.71 gm/ ml. BGAE has antidepressant & nootropic activities that are equivalent to imipramine & piracetam at doses of 250 & 500 mg/kg, respectively, which may be due to its effect on neurotransmitters & antioxidant function.