PASS assisted prediction and pharmacological evaluation of novel nicotinic analogs for nootropic activity in mice

Khurana, Navneet; Ishar, M. P. S.; Gajbhiye, Asmita; Goel, Rajesh Kumar

doi:10.1016/j.ejphar.2011.04.048

Cited by 97 publications

(68 citation statements)

References 37 publications

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“…The TL test is a neutral behavioral model which is being used to evaluate learning and memory in animals [18,19,25]. TL test principle is based on the supposition that mice prefer the closed arms over the open arms [26].…”

Section: Discussionmentioning

confidence: 99%

“…Deficit in cholinergic system may lead to the cognitive impairments symptoms observed in AD [29]. Sco is a well-known nonselective muscarinic receptor blocker that induces deterioration of learning and memory process in animals [18,19]. Sco-induced amnesia model is an interoceptive behavioral model which is widely cited in the literature for mimicking human dementia [18,19,25,29].…”

Section: Discussionmentioning

confidence: 99%

“…The mice (n=6/group) were divided into different groups for employing Sco-induced amnesia model [18,19]. Group 1 (control group) was administered with vehicle, i.e., 0.5% CMC solution (5 mL/kg; p.o.)…”

Section: Sco-induced Amnesia Modelmentioning

confidence: 99%

“…In this test, the passive avoidance behavior of animal was evaluated using SDL method [19,20]. The stepdown paradigm apparatus consisted of a rectangular wooden box (27 cm × 27 cm × 27 cm) with inclusion of Plexiglass wall on one side, a grid floor and a lamp of 15 W illumination.…”

Section: Sdl Testmentioning

confidence: 99%

“…TL estimation was done using EPZ apparatus, that served as the significant model, to evaluate the retention of learned tasks by the animals. The procedure, method, and end point for this test were followed using the parameters as described by the earlier evaluators with few modifications [19,20] Before moving the mouse to their cages, they were kept in the maze for another 2 minutes for exploration of maze. The same procedure was repeated after 24 hrs of the treatment and retention was examined in mice.…”

Section: Tl Testmentioning

confidence: 99%

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Ameliorative Effect of Sida Cordifolia L. Against Scopolamine-Induced Cognitive Deficit Mice Model

Khurana

Sharma

Patil

et al. 2017

Asian J Pharm Clin Res

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Objective: In this study, ameliorative effect of aqueous extracts of Sida cordifolia and hydroethanolic extracts of S. cordifolia L. (AESC and EESC, respectively) was evaluated against scopolamine (Sco)-induced amnesia in mice. S. cordifolia L. is a well-know Ayurvedic plant which has been administered anciently for various nervous disorders including loss of memory. Female Swiss albino mice were used for Sco-induced amnesia model and acute toxicity study.Methods: Acute toxicity study was carried out to select safe and effective doses (50, 100 and 250 mg/kg; p.o.) of AESC and EESC for further pharmacological evaluation. The AESC and EESC at selected doses and donepezil (Dpl) (5 mg/kg; p.o.) were administered to different groups for consecutive 15 days. On 15 th day of treatment, Sco (0.4 mg/kg, intraperitoneally) was administered to different groups for induction of amnesia. Mice were subjected to transfer latency (TL) and step down latency (SDL) tests on the 16 th day to evaluate the effect of AESC and EESC on memory.Results: Sco treatment caused a significant increase in TL and decrease in SDL. The EESC significantly and dose dependently reversed the Sco-induced amnesia. The maximum effect was seen in EESC (100 mg/kg) treated group. This effect of EESC was comparable to the group treated with Dpl. The group treated with varying doses of AESC showed no significant effect on TL and SDL. Conclusion:These findings suggested the possible therapeutic potential of EESC (70%) for diseases related to memory dysfunctions like dementia in Alzheimer's disease.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Sco-induced Amnesia Modelmentioning

confidence: 99%

Section: Sdl Testmentioning

confidence: 99%

Section: Tl Testmentioning

confidence: 99%

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Ameliorative Effect of Sida Cordifolia L. Against Scopolamine-Induced Cognitive Deficit Mice Model

Khurana

Sharma

Patil

et al. 2017

Asian J Pharm Clin Res

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Curculigo recurvata W.T.Aiton exhibits anti‐nociceptive and anti‐diarrheal effects in Albino mice and an in silico model

Ahmad

Nasrin

Reza

et al. 2020

Anim Models and Exp Med

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BackgroundCurculigo recurvata (C. recurvata) is an enthnomedicinally important herb reported to have significant medicinal values. The present study aimed to explore the in vivo and in silico anti‐nociceptive and anti‐diarrheal effects of a C. recurvate rhizome methanol extract (Me‐RCR).MethodsThe analgesic effects of Me‐RCR were assessed using acetic acid‐induced writhing and the formalin‐induced flicking test. The drugs were administered intraperitoneally (IP) at doses of 200 and 400 mg/kg body weight (bw). Anti‐diarrheal activity was evaluated by assessing intestinal motility, hypersecretion, and fecal score in mice at oral doses of 200 and 400 mg/kg·bw. Computer facilitated analyses for anti‐nociceptive and anti‐diarrheal activities of three isolated compounds from C. recurvata were undertaken to identify the best‐fit phytoconstituents.ResultsThe Me‐RCR showed significant (P < .05) peripheral anti‐nociception at the highest dose. The extract inhibited both early and late phases of nociception in the formalin‐induced writhing test. In the castor oil‐induced diarrhoea model, the extract significantly (P < .05) prolonged the onset time of diarrhoea, inhibited percentage of diarrhoea, and decreased both the volume and weight of intestinal contents. Rates of intestinal fluid accumulation inhibition were (33.61 ± 1.00)% and (46.44 ± 0.89)% at Me‐RCR doses of 200 and 400 mg/kg·bw, respectively. Moreover, a significant (P < .05) reduction in gastrointestinal motility was observed. An absorption, distribution, metabolism, excretion and/or toxicity (ADME/T) test showed that the selected compounds yielded promising results, satisfying Lipinski's rule of five for predicting drug‐like potential. Notably, of the three phytoconstituents curculigine and isocurculigine possessed the highest affinity for the COX‐1 and COX‐2. Isocurculigine was also identified as the most effective anti‐diarrheal compound in the computer‐facilitated model.ConclusionAn extract of the plant C. recurvata showed potential analgesic and anti‐diarrheal activity due to the presence of one or more active secondary metabolite(s).

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Exploring the Anti‐Cancer Potential of Hispidin: A Comprehensive in Silico and in Vitro Study on Human Osteosarcoma Saos2 Cells

Benarous,

Serseg,

Mermer

et al. 2024

Chemistry & Biodiversity

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Hispidin was initially discovered in basidiomycete Inonotus hispidus (Bull.) P. Karst and this extraordinary compound possesses immense potency and can be extracted from the wild mushroom through specialized bioreactor cultivation techniques. In our study, we isolated it from Inonotus hispidus (Bull.) P. Karst., with a yield of 3.6%. We identified and characterized hispidin through the implementation of spectroscopic techniques such as FTIR, NMR, and MS. Additionally, we utilized Thermogravimetric Analysis for thermal characterization of the compound. Computational studies based on DFT were performed to investigate the molecular structure, electronic properties, and chemical reactivity of hispidin. PASS analysis for hispidin demonstrated that 19 of them are anti‐neoplastic activities. The Pharmacology prediction of hispidin confirm that it is not toxic, non‐carcinogenesis with a good human intestinal absorption. The effect of hispidin on the viability of bone cancer cells was evaluated by MTT assay. The results showed that hispidin significantly reduced SaoS2 cell viability in a dose‐dependent manner. Molecular docking was carried out using five targets related to bone cancer to determine the interactions between hispidin and the studied proteins. The results demonstrate that hispidin is a good inhibitor for the five targets. Dynamic simulation shows a good stability of the complex hispidin‐protein.

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PASS assisted prediction and pharmacological evaluation of novel nicotinic analogs for nootropic activity in mice

Cited by 97 publications

References 37 publications

Ameliorative Effect of Sida Cordifolia L. Against Scopolamine-Induced Cognitive Deficit Mice Model

Ameliorative Effect of Sida Cordifolia L. Against Scopolamine-Induced Cognitive Deficit Mice Model

Curculigo recurvata W.T.Aiton exhibits anti‐nociceptive and anti‐diarrheal effects in Albino mice and an in silico model

Exploring the Anti‐Cancer Potential of Hispidin: A Comprehensive in Silico and in Vitro Study on Human Osteosarcoma Saos2 Cells

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