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The aim of this study was to screen the in vitro antimicrobial, antioxidant and cytotoxicity effect of Curkolin®, a combination of curcumin and C. forskolin in the ratio 4:1. Curcuma longa L. is the source of curcumin while C. forskohlii has been used in traditional ayurvedic medicine for curing various disorders and therefore the forskolin is the source of the diterpenoids. The medicinal properties of plants are investigated throughout the world for scientific advancement for their important pharmacological activities, user convenient, economically viable with low toxicity. The antioxidant property of Curkolin® was determined to be 55.42 µg/ml using (Diphenyl picryl hydrazine) DPPH assay and was then compared with standard Butylated hydroxytoluene (BHT). The antimicrobial activity was assessed by calculating the MIC and MBC using microplate serial dilution technique. It exhibited 250 µg/ml, the least MIC value of Bacillus cereus as compared to the rest Gram-positive (Streptococcus mutans and Staphylococcus aureus) and Gram-negative (Escherichia coli and Salmonella typhi) bacteria. Further, it was analyzed for cytotoxic screening on MCF-7 breast cancer cell line by MTT assay, which has shown a strong anti-proliferative activity. The IC50 values of Curkolin® were found 135.8 μg/ml. Together these results suggest the combination to be an effective antioxidant, antimicrobial and cytotoxic agent. [ABSTRACT FROM AUTHOR]

In this study, the chemical composition and antimicrobial activity of the essential oils from the leaves of Ocimum obovatum were investigated. Hydrodistillation yielded 43 compounds representing 99.5% of the oil. The composition of the oil was analyzed using gas chromatography and mass spectrometry (GC-MS). The main compounds detected were phytol (21.46%); 2-isopropyl-5-methyl-9-methylene- bicyclo[4.4.0]dec-1-ene (8.2%); n-hexadecanoic acid (7.4%); 6,10,14-trimethyl 2-pentadecanone (5.2%); 2- ethylhexyl undecy l ester phthalic acid (5.2%); dibutyl phthalate (4.5%); 2,6-lutidine-N-oxide(3.4%) and 2- (1,1-dimethylethyl)-1,4-dimethoxy-benzene (3.1%). The essential oil was further tested in vitro against the bacteria Escherichia coli, Staphylococcus aureus, Klebsiella spp, Pseudomonas spp and Proteus spp. by disc diffusion method. The minimum inhibitory concentration against the bacteria was also determined. The oil sample was active against both gram positive and gram negative bacteria. Standard antibiotic discs with Chloramphenicol were used as positive controls. [ABSTRACT FROM AUTHOR]

The antioxidant potential of 80% aqueous methanol and methanol extracts of Biophytum reinwardtii (Zucc.) Klotzsch. was evaluated by in vitro DPPH free radical scavenging activity and the extracts exhibited poor Scavenging activity (725.5 and 560 µg/mL respectively). Chlorophyll, sugar, proteins and the non-enzymic antioxidants such as flavonoids, tannins and phenols present in the plant were estimated by adopting standard procedures. Ethyl palmitate, lupeol, β-sitosterol and linoleic acid were isolated from the hexane extract of the whole plant and characterized by its UV, IR spectra, m.p;, mixed m.p. and co-TLC with their standards. [ABSTRACT FROM AUTHOR]

The article provides information on a study which examined the antioxidant potential and acetyl cholinesterase inhibition activity of different extracts of Terminalia chebula, popularly known as Harde Combretaceae and is commonly used in many Ayurvedic preparations. The plant is used as treatment for constipation, diarrhea and ulcers, among others. It also discusses the drugs approved for the Alzheimer's disease (AD) therapy. The methods used for the research includes thin layer chromatography, total phenolic content (TPC) and acetylcholinesterase activity.

Earlier we have reported the effect of arecoline thiazolidinone and morpholino arecoline analogues as muscarinic receptor 1 agonist in Alzheimer's dementia models. To elucidate further our SAR study on the chemistry and muscarinic receptor binding efficacy, a series of novel N-alkyl/aryl substituted thiazolidinone arecoline analogues 6(a-m) were designed and synthesized from 3-pyridine carboxaldehyde by reacting with different amines in the presence of gamma-ferrite as catalyst and subjected to in vitro muscarinic receptor binding studies using male Wistar rat brain membrane homogenate and extended to in vivo pharmacological evaluation of memory and learning in male Wistar rats. Derivative 6j having diphenylamine moiety attached to nitrogen of thiazolidinone showed significant affinity for the M1 receptor binding.

Hypocholinergic function associated with Alzheimer's disease (AD) is well-accepted hypothesis, in this regard, many research attempts have been made to elevate the reduced cholinergic neurotransmission, among them two main treatment strategies were widely explored, namely stimulation of muscarinic receptor 1 and/or reversible inhibition of acetylcholinesterase (AChE) enzyme. In an attempt to improve the efficacy and to minimize general side effects of these AChE inhibitors, many lead molecules are developed in research; one among them is piperidine derivative. Donazepil is a widely prescribed AChE inhibitor which displays a piperidine ring in its structure. In the present study, we have docked cis-2,6-dimethyl piperidine sulfonamides (3a-i) on AChE enzyme and synthesized by nucleophilic substitution reaction between cis-2,6-dimethyl piperidine and alkyl/aryl sulfonyl chlorides in the presence of triethylamine. These piperidine sulfonamides were subjected to in vitro AChE enzyme inhibition studies and in vivo antiamnesic study to reverse scopolamine induced memory loss in rats. Two derivatives (3a and f) in this class of piperidines (3a-i) showed considerable inhibition against different sources of AChE in vitro and reduced average number of mistakes done by wistar rats as compared to scopolamine treated group in vivo (rodent memory evaluation).

A series of novel substituted 1-benzhydryl-piperazine sulfonamide 8(a-f) and benzamides 9(a-h) were synthesized and their antimicrobial activities evaluated in vitro by paper disc diffusion and micro dilution method against standard strains of Gram-positive (Staphylococcus aureus ATCC 25953, Staphylococcus epidermis 25212, Bacillus cereus 11778, Bacillus substilis 6051) and Gram-negative (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 2853, Proteus vulgaris ATCC 2853 and Salmonella typhi ATCC 9484) bacteria. Among the synthesized new compounds 8d, 8e, 9c, 9e, 9f and 9 h showed potent antimicrobial activities compared to the standard drug streptomycin.

A series of novel, potent, and selective muscarinic receptor 1 agonists (M1 receptor agonists) that employ a key N-substituted morpholine Arecoline moiety has been synthesized as part of research effort for the therapy of Alzheimer's diseases. The ester group of arecoline (which is reported as muscarinic agonist) has been replaced by N-substituted morpholine ring. The structure-activity relationship reveals that the electron donating 4-substituted sulfonyl derivatives (9a, 9b, 9c, and 9e) on the nitrogen atom of the morpholine ring increases the affinity of M1 receptor binding 50- to 80-fold greater than the corresponding arecoline. Other derivatives also showed considerable M1 receptor binding affinity.

The association of bioactive nucleus with other pharmacological agents is hoped to improve the efficacy of the treatment by combining the effects of different pharmacological mechanisms of action. Keeping this in view, a series of 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-one derivatives have been synthesized by interaction of 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-one with different bioactive aralkyl halides in presence of powdered potassium carbonate by two different methods viz., conventional and microwave irradiation. The yields under conventional and microwave irradiation methods were in the range of 60-65% and 80-90%, respectively. The structure elucidation of the new compounds has been carried out with the help of elemental analysis and spectral data. All the synthesized compounds have been screened for their efficacy as acetylcholinesterase (AChE) inhibitor. AChE inhibitory activity study was carried out by using Ellman colorimetric assay with neostigmine as a reference standard against targets from different species, such as pure electric eel AChE, human serum AChE, and rat brain AChE. Among the compounds synthesized, compounds 5a, 5b, 5j showed good inhibition against AChE.

Alzheimer's disease (AD) is a neurodegenerative disorder affecting the central nervous system, which is also associated with progressive loss of memory and cognition. The development of numerous structural classes of compounds with different pharmacological profile could be an evolving, promising therapeutic approach for the treatment of AD. Thus, providing a symptomatic treatment for this disease are cholinomimetics with the pharmacological profile of Acetylcholinesterase (AChE) inhibitors. In view of this, we have synthesized novel 3-aryl-N-methyl-1,2,5,6-tetrahydropyridine derivatives 5a-k by Suzuki coupling and screened the efficacy of these derivatives for their AChE inhibitor activity.

A series of novel substituted 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives (4a-g) and (5h-m) have been synthesized. The synthesized compounds were characterized by IR and 1H NMR. All the synthesized compounds were evaluated in vitro for their efficacy as antimicrobial agents against representative strains of Gram-positive (Staphylococcus aureus ATCC 25953, Streptococcus pneumoniae ATCC 49619, Bacillus cereus 11778, and Bacillus subtilis 6051) and Gram-negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 2853, Proteus vulgaris ATCC 2853, and Salmonella typhi ATCC 9484) by paper disc diffusion and microdilution methods. Among the newly synthesized compounds 4e, 5l, and 5m showed potent antimicrobial activities, when compared to the standard drug.

The cholinergic hypothesis of Alzheimer's disease (AD) has spurred the development of numerous structural classes of compounds with different pharmacological profile aimed at increasing central cholinergic neurotransmission. Thus proving a symptomatic treatment for this disease are cholinomimetics with the pharmacological profile of acetyl cholinesterase (AchE) inhibitors. The novel bioactive 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives were synthesized under mild conditions using different aryl/alkyl halides and heterocyclic alkyl halides with 1-[bis(4-fluorophenyl)-methyl]piperazine in the presence of powdered potassium carbonate in N,N-dimethylformamide. All the synthesized compounds were characterized by spectroscopic techniques, elemental analysis and were screened for their efficacy as AchE inhibitor. Some derivatives in this class showed good inhibition against AchE as compared to neostigmine as standard.