Neurite outgrowth properties of calotropis procera: In search for a neuroprotectant

In view of the well-documented medicinal properties of Calotropis procera [CP], the present study was designed to evaluate the neuroprotective effect of the extract. We have prepared a methanolic extract of Calotropis procera and screen varying concentration of CP [20, 30, 40, 50 and 70microg/ml] for the stimulatory potency on neurite outgrowth. The stimulatory effect of CP on neurite outgrowth was assessed in primary hippocampal neurons. Neurite lengths were measured using optika provison analysis software. Neuritogenesis was further analyzed by immunostaining by using specific neuronal marker beta III-tubulin. The data show that neurite outgrowth from hippocampal neurons were significantly enhanced in the presence of CP [40microg/ml]. The most stimulatory neurite outgrowth effects were appeared after 48hrs incubation of neurons with CP [40microg/ml]. These data confirm that CP extract could promote invitro hippocampal neurite outgrowth in a dose-dependent manner. Our results indicate that CP can be used as a healthy dietary supplement for the cognitive functions of the brain

Vitex negundo induces an anticonvulsant effect by inhibiting voltage gated sodium channels in murine Neuro 2A cell line

Vitex negundo [Vn] extract is famous for the treatment of neurological diseases such as migraine and epilepsy. These neurological diseases have been associated with abnormally increased influx of sodium ions into the neurons. Drugs that inhibit voltage gated sodium channels can be used as potent anti-epileptics. Till now, the effects of Vn on sodium channels have not been investigated. Therefore, we have investigated the effects of methalonic fraction of Vn extract in Murine Neuro 2A cell line. Cells were cultured in a defined medium with or without the Vn extract [100 microg/ml]. Sodium currents were recorded using whole-cell patch clamp method. The data show that methanolic extract of Vn inhibited sodium currents in a dose dependent manner [IC50 =161microg/ml]. Vn [100 microg/ml] shifted the steady-state inactivation curve to the left or towards the hyper polarization state. However, Vn did not show any effects on outward rectifying potassium currents. Moreover, Vn [100 microg/ml] significantly reduced the sustained repetitive [48 +/- 4.8%, P<0.01] firing from neonatal hippocampal neurons at 12 DIV. Hence, our data suggested that inhibition of sodium channels by Vn may exert pharmacological effects in reducing pain and convulsions

Neuroprotective capabilities of Vitex negundo in primary hippocampal neurons

Vitex negundu [Vn] is a well-known aromatic shrub commonly used as a traditional folk medicine famous for its potential pharmacological and biological activities. Several chemical compounds are extracted and identified from the different parts of the Vn such as leaves, root, seeds and flowers. Number of researches reported the herb as antimicrobial, anti-androgenic, anti-osteoporotic, and anti-tumour, anti-cancer, anti-inflammatory, anti-oxidant, anti-hyperglycemic and hepatoprotective. The effects of Vn on neurite outgrowth have not been identified till now. Therefore present study was designed to investigate the neurite outgrowth effects of Vn extract in hippocampal neurons. Neurons from P0 mice were isolated and cultured in defined medium containing the different concentrations of Vn [20, 30, 40, 50, 100, 150 and 200 microg/ml] for 48 hrs. The presence of the neurites was confirmed by using betaIII-tubulin antibody which specifically labels only the neurites. Morphometric analysis was done by using Optika Pro-Vision software. The data show that Vn at 30 and 40 microg/ml significantly increased the mean average length of the longest neurite whereas at 150 and 200 microg/ml it significantly decreased the mean average length of the 10 longest neurite in hippocampal neurons. Nevertheless Vn did not show any significant effects on the sum of all the neurite lengths at any concentrations tested. Taken together the result shows that methanolic extract of Vn has potential to produce long neurites at 30 and 40 microg/ml and therefore can be act as a neuroprotective agent in the future drug development

Some novel piperidine analogues having strong alpha glucosidase inhibition

The idea of this study is based on the marvelous fact of nojirimycin and deoxy nojirimycin, naturally occurring from piperidine class and having their role as alpha glucosidase inhibitors. In the present work some hydroxyl piperidine analogues have been synthesized and analysed for their hypoglycemic effect through glucosidase inhibition owing to the structural resemblance with nojirimycin. The activity was done by spectral absorbance analysis using acarbose as standard. Two analogues [I and IV] were found to pose excellent activity having 87.4 and 54.7% inhibition respectively, hence strengthening the idea of studying piperidine analogiues as glucosidase inhibitors due to structural similarity with nojirimycin

Immunomodulatory activity and chemical characterization of fixed oils obtained from different parts of Oxytropis glabra DC

Oxytropis glabra DC. is a plant with enormous therapeutic vitality. In the present study a comparison of lipophilic profiling of different parts of O. glabra has been carried out by using gas chromatography-mass spectrometry. A total of 32 compounds have been identified from this plant, amongst which 31 have been identified for the first time. These compounds have been further confirmed from their Van den Dool and Kratz [I] Indices. Out of these 32 compounds, 18 have been identified from flower [80.94%], 15 from fruit [85.36%], 11 from leaves [66.35%] and 11 from root [45.96%]. The major class of metabolite identified from different parts is fatty acid. Hydrocarbons have also been detected in flower and fruit but not in root and leaves. The extracts were screened for their immunomodulatory activity on whole blood cells. The root oil was found to be moderately active [IC50 32.3 micro g/ml]. At present only limited data is available on the phytochemical composition of O. glabra

Synthesis, characterization and SAR of novel bezimidazole derivatives as nematicidal agents

Six novel analogues were prepared by reacting benzimidazole molecules [BM and CMB] propiophenone andbenzoyl chlorides respectively. The structures of newly synthesized compounds were determined with the help of spectroscopic techniques. The compounds were subjected to in-vitro screening for their activity against nematodes. It was observed that the benzimidazole [BM] derivatives possessed more nematicidal activity as compared to that of cyanomethyl-benzimidazole [CMB] for Meloidogyne incognita. Among them, the propiophenone substituted benzimidazole derivative B3 was found to be the most active compound and can be further studied as lead molecule for development of anthelmintic drugs

Synthesis, characterization and evaluation of antioxidant potential of 2, 6-diphenylpiperidine-4-one compounds and their novel imine derivatives

In search of potent molecules having antioxidant activity the present work was designed to synthesize 2, 6diphenylpiperidine-4-one compounds [1a and 1b] and their imine derivatives [2a, 2b, 3a, and 3b]. Compounds 1a and 1b were synthesized by Mannich condensation reaction. The method was found to be simple, convenient with high yield and products were easily separated. Compounds 1a and 1b serves as an intermediate for the preparation of highly functionalized novel imine derivatives. Oxime [2a, 2b] and carbothioamide [3a, 3b] derivatives of 1a and 1b compounds were produced by condensation reaction with hydroxyl amine hydrochloride and thiosemicarbazide respectively. These compounds were characterized by IR, EI-mass and 1HNMR spectroscopy. The antioxidant activity of compounds was analyzed by 1, 1- dipheny1-2-picrylhydrazyl [DPPH] assay method. It was found that substituted aryl derivatives containing phenol and methoxy groups [1b, 2b and 3b] showed better antioxidant activity [IC50 values rang from 1.844.53[micro]g/ml] than unsubstituted aryl derivative [1a, 2a and 3a] [IC50 rang from 6.46-11.13[micro]g/ml]. Compound 1b exhibited excellent antioxidant activity [IC50 1.84 +/- 0.15[micro]g/ml] comparable to standard ascorbic acid [IC501.65 +/- 0.16[micro]g/ml]