Cerebral metabolism will be affected in T2DM either by chronic hyperglycemia or by chronic hypoxia. Proton magnetic resonance spectroscopy ((1)H-MRS) of the brain provides detailed information about the structure, dynamics, reaction state and chemical environment of molecules. It also measures the levels of brain metabolites such as myo-inositol (mI), N acetyl aspartate (NAA), creatine (Cr), choline (Cho), glutamate (Glu), glutamine (Gln) and gamma amino butyric acid (GABA). Several studies suggest that people with type 2 diabetes mellitus (T2DM) are at an increased risk of cognitive impairment in comparison with the general population. The altered metabolites may cause cognitive dysfunction in T2DM. This review article concludes that in T2DM, metabolite levels were altered in different regions of brain.
Dry and wet methods can be applied for granulation. It is said that final use of prepared granules as tabletsdictates the preparation method. At the present study the formulation of the extract of the stem bark of G.parvifolia as tablet dosage form was performewd by use of formulation using dry and wet methods andcompared inrespect to characteristics like hardness test, weight uniformity test, friability test, disintegrationtime and dissolution test and other properties. Results showed that it was concluded that it is better to usewet method for granulation it final aim is produce tablets of the granules. Other wise if the granules will beused as such and there method can be used because of the advantages of this method in respect to low costof production course, no need to use organic solvents and feasibility in industrial scale production
The present investigation provides the effect of combined treatment of gamma rays and SA (Sodium Azide) on the morphology of Linum usitatissimum. Fasciated plants were obtained in M2 and M3 generation. Various widened and flattened organs were found such as fasciated stems, abnormal branches arising from fasciated stems, broad and abnormal leaves. The enhanced activity of apical meristem and cambium resulted in a significantly increased circumference of the stem resulting into increasing number of leaves, buds, flowers, fruits and seeds. Moreover the size of fruits and seeds were much bigger than control.
Our aim is to evaluate safety and efficacy of topical Eosin 2% + Chloroxylenol 0.3% + Propylene glycol 30% (Neo mercurocromo) and Colloidal Silver to improve Lichen Sclerosus (LS) symptoms.We postulated that the disinfectant, anti-moist, anti-dystrophic, antifibrotic and cytoprotective activity of NEOMercurocromomight be of help in improving LS symptoms. Forty-four LS patients were randomised into two groups: 22 patients received the active drugs (Group 1) and 22 received the placebo (NaCl 0.9%) for 4 weeks (Group 2). The active drugs were used for two weeks each: NEOMercurocromo first and subsequently Colloidal Silver. Active drugs and placebo were rubbed with a sterile gauze on the LS lesions twice a day. Three clinical controls using a photo archive (baseline, and one and three months after active drug or placebo delivery) were carried out on each patient using a specific LS scale score, and the Dermatology Life Quality Index (DLQI) score. One and three months after active drugs or placebo delivery, the patients defined their post-treatment condition using the Patient Global Impression of Improvement (PGI-I) scale. The scores were compared within and between groups using non parametric tests, and the side effects were compared between the groups using the Chisquared test (χ²). The LS and the DLQI scores were similar between the groups at baseline. Both scores significantly improved in Group 1 to a larger extent than in Group 2 at one and three months. The PGI-I score in Group 1 was higher than in Group 2 at one and three months. No side effects emerged in either group. NEOMercurocromo + Colloidal Silver is a safe and efficient therapy for LS. KEYWORDS: Chloroxylenol, NEOMercurocromo, colloidal silver, topical treatment, lichen sclerosus.
Levobupivacaine, the pure S enantiomer of bupivacaine has emerged as a safe local anaesthetic than its racemic counterpart. Dexmedetomidine the novel selective alpha2 adrenergic agonist has several advantages when given through epidural route as an adjuvant. To compare plain 0.5% Levobupivacaine with Dexmedetomidine and 0.5% levobupivacaine epidurally for the time of onset of sensory blockade and its duration. 60 patients undergoing infraumblical and lower limb surgeries were randomized to two groups. Group A(n=30) received only Levobupivacaine 0.5% 20 ml epidurally. Group B(n=30) received 50 mcg of dexmedetomedine with Levobupivacaine 0.5% 20 ml epidurally. The time of onset of sensory blockade, maximum height of sensory blockade and duration of blockade were noted. Statistical work done by student t test and chi-square test and p<0.05% were taken to be significant. Dexmedetomidine fastens the onset of sensory blockade and the duration of blockade without any significant adverse effects.: We conclude that Dexmedetomidine can be used as an adjuvant to Levobupivacaine which fastens the onset and prolong the duration of sensory blockade.
Under different growth conditions such as pH, temperature and metal ions, Bacillus subtilis KCX006 was tested for amylase production and kinetic properties of amylase was determined. The enzyme activity was more in the stationary phase and the value was 21.78 U/mL (at 30 h) and protein content was 0.303 mg/mL. The maximum amylase activity (38 U/mL) was also found at stationary phase when the culture was grown at 37°C. The enzyme was purified to homogeneity with an overall recovery of 24.2% and specific activity of 4133 U/mg. Either acidic or alkaline condition significantly affected the growth and enzyme production. Enzyme activity was more in reaction mixture containing NiCl 2 and its residual activity was found to be 117.5%. These results suggest possible application in food and detergent industries where moderate pH and temperature are employed.
The acute and sub-chronic 28-day repeated dose toxicity studies in rodents were performed to assess the safety of polyherbal formulation of Isabgol husk (Plantago ovate), Swarnapatri leaf extract (Cassia angustifolia) and Triphala fruits extract (Emblica officinalis, Terminalia chebula and Terminalia belerica) (TLPL/AY/01/2008). The studies were conducted according to current OECD toxicology guidelines for acute and repeated dose. No mortalities or evidence of adverse effects were observed following acute oral gavage administration up to 2000 mg/kg of TLPL/AY/01/2008 in Sprague dawley rats. The 28-day repeated dose study involving daily oral administration of 70, 175 and 350 mg/kg body weight of TLPL/AY/01/2008, with a post trial 14 day no treatment observation period at high dose level, resulted in no clinical signs and animal deaths. No toxicological significant differences were observed in any of the TLPL/AY/01/2008 treatment groups for body weights, feed consumption, physical appearance, neurological behaviour and urine analysis. Evaluation of haematology and clinical chemistry parameters revealed no toxicological and treatment related effects. No treatment related changes noted in absolute and relative organ weights. Macroscopic and microscopic evaluation of organs revealed no treatment related. Results of this study demonstrate that polyherbal formulation TLPL/AY/01/2008 is not acutely toxic at 2000 mg/kg of body weight/day, with a NOAEL (no-observed-adverse-effect-level) of greater than 350 mg/kg of body weight/day for systemic toxicity from repeated dose 28-day oral gavage administration. The present study demonstrates the non-adverse nature of the polyherbal formulation TLPL/AY/01/2008 on long term administration.
Preliminary investigations on photoproduction of hydrogen by free viable cells of Rhodocyclus tenuis KU 017, and immobilized cells in sodium alginate matrix, under different cultural conditions with various carbon and nitrogen sources were carried out. Growing cells produced more amount of hydrogen under aerobic dark than aerobic light conditions. In contrast, under anaerobic conditions, hydrogen production was more in light than dark. Actively growing cells were more efficient and sustained hydrogen production for longer period than resting cells. Resting cells preferred light anaerobic conditions for hydrogen production. Resting cells required more lag period for hydrogen production, while growing cells produced more hydrogen during early phase of growth. Immobilization of bacterial cells not only enhanced hydrogen production but enabled the cells to produce hydrogen over an extended period. Among carbon sources formate induced maximum production of hydrogen at 96h and among nitrogen sources ammonium chloride induced maximum production at 192h incubation period. Lactate and L-tyrosine were poor carbon and nitrogen sources respectively for hydrogen production.
Indian economy gains 1.9% of National GDP by sugarcane cultivation. Plant growth hormones such as BAP, NAA, 2, 4-D, Kn, IBA were used to initiate cultures. A successful procedure was established in the culture conditions of variety 018. MS medium supplemented with 2,4-D (3.0 mg/l), Kn (0.2 mg/l) and 3% sucrose was the best for the initiation of callusing from leaves and MS medium supplemented with BAP (1.0 mg/l), Kn (0.5mg/l) and 3% sucrose was best for shooting in eye bud from nodal region. The best multiplication rate of shooting in case of nodal eye bud was in MS medium supplemented with BAP(0.1 mg/l), Kn (0.5) & NAA (0.25 mg/L) and 3% sucrose where as for leaves MS medium supplemented with BAP (4.0 mg/l), IBA (0.5 mg/L) and 3% sucrose. Root system was found in 1/2 MS medium with NAA (3.0 mg/l) and 6% sucrose.
Microbial esterases have a promising biotechnological potential to be used in various industrial purposes from the food industry to pharmaceutical industry. To accomplish appropriate function and higher quantity of the biocatalysts there is a need to govern the specific control of the enzyme synthesis. This article reports the regulation of a trybutyrin-esterase synthesis in a thermophilic bacterium, Geobacillus sp. AGP-04. Tributyrin alone itself induced esterase synthesis. Other triglycerides, sugar-alcohol and other carbon sources exhibited little or no enzyme induction. Lower concentration (0.01-0.15% v/v) of the enzyme catalyzed end products, i.e. glycerol and butyric acid in the presence of tributyrin induced enzyme synthesis though higher concentration (>0.15%) was inhibitory. The addition of superfluous energy rich phosphonucleotides did not enhance the enzyme synthesis. Addition of glucose (about 0.2%) to the media supplemented with tributyrin repressed tributyrin-esterase biosynthesis. cAMP alleviated the enzyme synthesis in the glucose mediated repressed cell. Potent ionophores like 2- 4-dinitrophenol and Carbonyl cyanide 3-chlorophenylhydrazone (CCCP) repressed enzyme synthesis by inhibiting ATP synthesis in the cell. The study revealed that tributyrin-esterase synthesis to be an energy dependent process and it is under the control of catabolic repression.
Given the widespread use of insecticides in the environment, it is important to perform studies evaluating their potential effects on non target species. The use of pyrethroids in household pest control is increasing. Cyfluthrin is extensively used synthetic pyrethroid pesticide. The present study was designed to analyze the liver response to the acute dose of this synthetic pyrethroid in Swiss Albino Mice. The experiments were conducted to determine the concentration of GSH and LPO in the liver of Mice after the administration of acute dose. The value of LPO significantly increased (p>0.05) whereas GSH values showed increase followed by significant decline.
Bismarck Brown Y was selected as model textile dye. The fungal strain Alternaria brassicae TSF -07 isolated from textile wastewater sludge was screened for decolourization of Bismarck Brown Y. Optimization was carried out with respect to carbon source, nitrogen source, pH, inoculums size, incubation period and temperature. It was found that the optimum inoculum size, pH and temperature were 2.5%, 5.0 and 350C respectively. Fructose at 1.0 % and yeast extract at the concentration of 0.1 % was found to give maximum decolourization. Further, it was found that the culture has brought about almost 96.03% decolourization of a recalcitrant dye, Bismarck Brown Y (100 mgL-1) at shaking condition within 3 days. This isolate also showed the degradation as evidenced from the reduction in the term of COD mg/L to the extent of 68.09 % within three days. The biodegradation was monitored by UV-Vis and FTIR spectroscopy. This study revealed the enormous biodegradation abilities of indigenous microbial flora.
Data mining methods based on support vector machine are attractive to address the curse of dimensionality. The Kernel mapping contributes a unifying frame work for most of the commonly employed models to get the linear planes in the higher dimensional space. In this paper, we prove this approach enhances the accuracy of diabetes data set. We further refine the results with parameter tuning for the selected kernels. The natural question that arises in case of many such different mappings to choose from, which is the best for a particular problem? The selection can be validated using independent test sets or variety of data sets and methods of cross validations.
The main objective of the present study was Antidiabetic activity of aqueous extract of leaves of Boerhaavia diffusa in alloxan induced diabetic rats was assessed. After the treatment, blood samples were collected and the serum was subjected to estimate different biochemical parameters viz. blood glucose, insulin, cholesterol, urea, glycosylated haemoglobin, triglycerides and protein levels. There was a steep decrease in protein, insulin and elevated level of blood glucose, urea, glycosylated hemoglobin, cholesterol and triglycerides are seen. It becomes normal after exposure of aqueous leaf extract of Boerhaavia diffusa. It may be concluded that Boerhaavia diffusa might be used in the treatment of diabetics.
Here, relative total phenolics, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, total antioxidant potentials and phytochemical profiles of seven ethnomedicinally important, mostly antitumor, plant parts’ aqueous extracts (leaves of: Cordia dichotoma, Holoptelea integrifolia, Crinum asiaticum; aerial parts of: Croton bonplandianum, Cayratia carnosa, Scadoxus multiflorus and seeds of: Trigonella foenum-graecum) were analyzed. Data indicate the different extracts with varied amounts of phenolics and their differential capacity to neutralize the DPPH free radicals and total antioxidant activity. Out of the seven extracts, the maximum free radical scavenging, total antioxidant activity and the highest phenolics content was found in C. asiaticum. The preliminary phytochemical analysis indicates the prevalent secondary metabolites are alkaloids, terpenoids, tannins and saponins. In summary, considering the relative phenolics abundance and antioxidant activities, it can be concluded that out of seven anticancer plant products tested here C. asiaticum leaf aqueous extract possesses the highest efficient free radical scavengers and antioxidant potentials. Therefore, further study demands for in vivo antioxidant and cytogenotoxic potentials of C. asiaticum.
The two new complexes Ag(L1)2L2(PF6)2[Complex (1) and Cu(L1)2L2(PF6)2[Complex (2)] containing bioactive mixed ligand of typeL1=8-Hydroxyquinoline and L2=1,10-Phenanthroline have been synthesized and characterized by analytical and spectral methods. The binding constant of the complexes in 5 mM Tris-HCl/50 mM NaCl buffer at pH 7.2, are 25.79 x 106 M-1and 9.95 x 106 M-1for complex (1) and (2) respectively. The synthesized compounds have been tested against microorganisms such as Gram positive bacteria (Staphylococcus aureus and Proteus vulgaris), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and fungus (Aspergillus niger). A comparative study of the Minimum Inhibitory Concentration(MIC) values of the ligands and their complexes indicates that the complexes exhibit moderate antimicrobial activity than the free ligand and control.
The kinetics of oxidation reactions and the investigations of the reaction mechanisms from the kinetic data have been always the more interesting in the chemical research and industrial applications. The kinetics of oxidation of sugars has been a subject of extensive research in recent years. The biological as well as the economic importance of carbohydrates is responsible for the great interest in the study of their bio- and physio -chemical properties. The kinetics of oxidative degradation of different sugars by metal ions including Cr (VI) has been studied under different conditions. Chomium (VI) compounds are powerful oxidants at low or neutral pH as well as Cr (VI) is a well-known oxidant in acetic media. Aim of our present investigation deals with oxidation of D-Lactose using Cr (VI) Oxidizing agent, Trimethylammonium fluorochromate [TriMAFC] which was carried out in protic solvent as a medium at 308 K in the presence of 1,2-bis(4-pyridyl)ethane as a catalyst . The oxidation of D-Lactose yields the corresponding aldonic acid and Cr3+ as final products. Lactobionic Acid (LBA) has been used for food and pharmaceutical applications. Thus the kinetics and mechanism of carbohydrates using Cr (VI) as oxidant, 1,2-bis(4-pyridyl)ethane as a catalyst is very important from biochemical and kinetic viewpoints. Our experimental studies showed that reaction progressed with first order kinetics with respect to [TriMAFC], [1,2-bis(4-pyridyl)ethane] and [H+] with the fractional Order dependence on [D-Lactose]. It was found that introduction of sodium perchlorate results in decrement of the reaction rate substantially. The rate constant increased with increase in the concentration of perchloric acid. Also, the rate of reaction decreases with increasing the concentration of acetic acid. For acrylonitrile, no polymerization occurs. The reaction was carried out at four different temperatures to determine the activation parameters. An appropriate mechanism was suggested based on the observed kinetic effects.
4-amino-5-biphenyl-4-yl-4H-[1, 2, 4] triazolo-3-thiols have been prepared from biphenyl-4-carboxyclic acid (1), carbon disulphide (CS2) and hydrazine hydrate. The resulting 4-amino-5-biphenyl-4-yl-4H-[1, 2, 4] triazolo-3-thiol was treated with substituted aromatic aldehydes to give the Schiffbase. The synthesized compounds were characterized by elemental and spectral analysis (IR, 1H NMR and mass spectrometry). All synthesized compounds were screened for their in vitro antimicrobial activity against bacterial strains and fungi strain and found to have significant effect against the tested microorganisms.
A series of new 6-methyl-3,4-dihydroimidazo[1,5-b][1,2,4]triazin-2(8H)-one derivatives have been synthesized with the initial reaction of various aromatic aldehydes and Nacetylglycine in acetic anhydride and anhydrous sodium acetate by Erlenmeyer- Azlactone synthesis to give oxazol-5(4H)-one derivatives which on reaction with substituted phenylhydrazine in dry benzene gave 1H-imidazol-5(4H)-one and lastly condensation with chloroacetamide in N, N-dimethylformamide gave final compounds. All synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR, LC-MS and HPTLC etc and are well supported by spectroscopic data. These novel compounds are investigated for their in vitro antimicrobial activity using zone of inhibition using cup plate method. The antibacterial activities were compared with standard drug such as ciprofloxacin and antifungal drug such as cotrimazole at concentration of 250, 500 and 750 μg/L. Synthesized analogues showed favorable antimicrobial effect.
The reaction of thiocarbohydrazide with substitutedphenoxy acetic acid to obtained 3-substituted-4-amino-5-mercapto-1,2,4-triazoles (1) by condensing compound 1 with aromatic carboxylic acid and substituted phenoxy acetic acids resulted the title compound triazolothiadiazoles 2a-j. The purity of the newly synthesized compounds was confirmed by TLC. Structures of all the newly synthesized compounds were confirmed by spectral data. All the newly synthesized compounds were screened for their in-vitroantimicrobial activity.Among the series the compounds 2e, 2f and 2b, 2c, 2f, 2d, 2i were exhibited equipotent antibacterial and antifungal activity a MIC of 1 μg/mL when compared with standard drugs respectively. From the results the compounds 2c, 2f, 2j were showed comparable antitubercular activity againstM. tuberculosisH37Rv at MIC of 0.50 μg/mL, when compared with standard drug Rifampin and INH which showed MIC of 0.25 μg/mL.
Condensation of substituted salicylaldehydes with primary amine of naphtha-thiazole gave a of Schiff base, such as 2-[N-(3,4-dimethoxy-2-hydroxyphenyl)-methylidinyl]-amino-4, 5-dihydronaphtho[1,2d]-thiazole (HL); Complexes were synthesized by reaction between cobalt chloride, nickel chloride and copper chloride with the ligand (HL). These complexes were characterized by elemental analyses, conductance measurements, magnetic susceptibility measurements, IR, 1H NMR, and electronic spectral studies. On the basis of magnetic and spectral studies, octahedral geometry was assigned for these complexes. These complexes have been screened in vitro for their possible antimicrobial activity.
Cancer is a leading lethal disease. Hepatocellular carcinoma (HCC) is one of the most common malignant tumors worldwide, Which caused by various factors such as environmental pollutions, Chemical usages, alcohol and Hepatitis B virus (HBV).Now a day researchers involved to develop drug fro HCC. In our present study1,3-Bis-[(hydroxylnaphthalen- 2-yl)-phenyl-methyl]-urea is a newly synthesized mannich base has showed a wide variety of biological activities for the treatment of oxidative mediated diseases. The present study is aimed to evaluate its receptor binding score value of insilico docking, therapeutic potential of 1, 3BPMU on DEN induced rats were estimated by various biochemical parameters such as total albumin, globulin and bilurubin urea, creatinine enzymatic and non enzymatic antioxidant status in control and experimental rats. 1, 3BPMU treatment significantly normalized the altered biochemical levels and antioxidant activity in DEN induced rats. Further, SEM analysis revealed that the 1, 3BPMU protects the membrane changes induced by the DEN in rats. Therefore, we suggest that 1, 3BPMU could be useful for drug development against Hepatocellular carcinoma.
Inflammation is the vital part of the immune system's response to injury and infection. It is the body's way of signaling the immune system to heal and repair damaged tissue. The objective of this paper is to design and synthesize a new isoindoline 1,3-dinoe derivative and investigate their selective anti inflammatory activity to COXs. As a potential anti-inflammatory compound, Isoindoline-1,3-dione derivatives were synthesized from the addition reaction of phthalimide, formaldehyde, catalytic amount of potassium hydroxide and cyclic amine in ethanol yielded the desired Isoindoline-1,3-dione compounds (ZJ1-ZJ6. 1H-NMR, ¹³C-NMR, FT-IR and elemental analysis were consistent with the assigned structures. Isoindoline-1,3-dione derivatives exhibited good inhibitory activity against the COX enzymes. To explain the result of our investigation to COX-1 and COX-2 and the selectivity of our compounds to either COX-1 or COX-2, the rationalization in COX-1, the amino group participate more effectively in binding with the ligand while in COX-2, the aryl group is more effective in binding to the ligand. The amino acetylenic compounds behave differently toward COXs from our compound. ZJ4 have shown some selective COX-1 ligand efficiency while ZJ1 promised a potent blockage and ligand efficiency toward the COX-2 enzyme which was found to be higher than the marketed drug Indomethacin and near potency score of Celecoxib. For the first time, this indicates the requirement of investigating the removal of acetylenic group in this study showed that it might be a different binding site in COXs which may result in effective compounds.
Synthesis of a series of new 1, 3, 2- dioxaphosphinane derivatives (3a-j) was accomplished. The key step in the synthesis of 3a-j involves the cyclization reaction of tris (hydroxy methyl) nitromethane (1) with P(X)Cl3 (X=S, O) in presence of TEA in THF at 40-45°C to afford the phosphoryl mono chloride intermediate (2). The intermediate (2) when treated with different substituted aromatic amines and with a few substituted phenols in situ in the presence of TEA at 0-15°C afforded 3a-j. The structures of 3a-j were established by IR, NMR (1H, 13C and 31P) and Mass spectral data and elemental analysis. All these compounds exhibited good antimicrobial activity.
Synthesis of alkyl-2-{[3-(3'-chloro-4'-nitrophenyl)-2-oxo-3,4-dihydro-2H-1,3,2 λ 5-benzoxazapho sphinin- 2-yl]amino} alkanoates (4a-j) were accomplished via a two-step process, involving the condensation of 2-[(3'-chloro-4'-nitrophenyl amino)methyl]phenol (1) with phosphorusoxychloride in the presence of triethylamine (TEA) in dry tetrahydrofuran (THF) to produce the corresponding monochloride intermediate (2), and subsequent reaction with the amino acid alkyl ester in dry THF in the presence of TEA at various temperatures. These compounds were characterized by IR, 1H, 13C, 31P NMR and mass spectral data and all them exhibited significant antibacterial and fungal activity.
Sericulture or silk farming is the rearing of silkworms for the production of raw silk. The mulberry silkworm, Bombyx mori, is a domesticated and monophagous insect which feeds only on the leaves of mulberry for its nutrition. Thiadiazoles are heterocyclic compounds containing oxygen and nitrogen. 1, 3, 4, thiadiazoles are extensively studied and are known to play diverse biological activities. Diamines or polyamines are found in various biological fluids and are necessary for optimal growth, replication and metabolism of every cell in the body. This report describes the synthesis of diamino substituted thiadiazole and its effect on the growth parameters of Bombyx mori silk worm. Results show that the title compound at high concentration resulted in increased worm weight, silk gland weight and cocoon weight and at low concentrations proved to be beneficial for improving the pupal weight. We conclude that the synthesized compound can be fed to B. mori silk worms for improving their economic parameters.
A series of new 2-(2,4-dimethoxyphenyl)-1,3,4-oxadiazole derivatives, 4(a-m) were synthesized by using 2,4-dimethoxybenzoic acid (1) as starting material. Different spectral data were used to characterize the newly synthesized compounds. All the compounds were screened for their in vitro antimicrobial activity. The results indicated that some of the compounds showed potential activity and comparable to those of commercial antibiotics. Few compounds showed good antimicrobial activity against tested strains.
This article outlines the medicinal and biological significance of privileged scaffold, the 1,4-benzodiazepine. 1,4-benzodiazepine derivatives are showing very promising and excellent therapeutic effectiveness either as single heterocyclic derivatives or in fusion with the other cycles. An attempt is made in this article to highlight the medicinally active compounds which were reported to posses various biological activities.
In the anticipation of finding potential substitutes of highly active antiretroviral therapy [HAART], several molecular probes (9-12) have been developed by incorporating the vital fragments of RT inhibitor 'etravirine' to the anti-HIV prone privileged template of 1,4-benzodiazepine (2), on the premise that their presence in tandem in the same molecular framework could produce a positive impact in overcoming the problem arising due to the emergence of the multidrug resistant mutants of the virus.
Intention in this review is to present a picture of 1,4-benzodiazepine with particular attention to their reactionsand uses in synthetic organic chemistry. Some of these reactions have been applied successfully to the synthesis of biologically important compounds. The main purpose of this review is to present a survey of the literature on 1,4-benzodiazepine chemistry.
An efficient novel single step strategy for the heteroannulation of 2-chloro-1,4- benzodiazepine ring, substituted in its 5-position with a carboxamido group (5), has been developed to allow the easy installation of thiadiazole (8) ring through thiosemicarbazone (7) intermediate. In this communication, exceedingly facile single step expedient protocols based on the versatility and reactivity of corresponding intermediate thiosemicarbazone (7), derived from 5-carboxamido-1,4-benzodiazepin-5- (4'-methylpiperazinyl)-carboxamide (5) have been developed to provide an easy installation of the thiadiazole (8) privileged template at 2-position of 5-carboxamido-1,4- benzodiazepin-5-(4'-methylpiperazinyl)-carboxamide, through a phenoxyl spacer.
Diazepines are an eminent class of drugs owing to their psychotherapeutic activities. Among these, 1,5-benzodiazepines are regarded as privileged structures due to their clinical importance and commercial success. Although immense work has been carried out on the benzodiazepine nucleus, it continues to receive a great deal of attention. Due to their vast range of biological properties the benzodiazepine nucleus has fascinated many investigators to synthesize and screen the analogues for all possible activities through all possible routes. This current review article mainly covers the various routes of synthesis utilized, the numerous solvents employed, catalysts used and the different pharmacological activities exhibited by 1,5-benzodiazepine derivatives. This review encompasses the research work that has been accomplished since the past decade.
It was thought of interest to synthesis 1,5 benzodiazepine substituted with isoxazole, and thiadiazole derivatives on its 2-position linked through oxyphenyl spacer. The conceived synthetic plan for the preparation of these materials proceeded through the acceptable protocol which emerged from the face 'c' cyclohexano substituted 1,5 benzodiazepine bearing the thiomethylether function on its 2-position is formed from the reaction of o-phenylenediamine with 2-oxoketenedithioacetal derivative of cyclohexanone. Its treatment with 2-aminobenzonitrile, p-hydroxy benzaldehyde and phydroxyacetophenone afforded the corresponding 2-amino substituted derivative of annulated 1,5-benzodiazepine, p-benzaldehyde and p-acetyl substituted derivatives. On its further reaction with 2-amino substituted derivative of annulated 1,5-benzodiazepine formed amidine and imidates esters derivatives which formed oxadiazoles, imidazoles benzimidazole derivatives of face 'c' annulated 1,5-benzodiazepine. The purity of the compounds was checked by TLC and their structures were established on the basis of their spectral data.
A chelating resin of chitosan-1,5-diphenylcarbazide modified with the alginate salts and utilization as a filler material column has been synthesized and the sorption properties have been investigated for preconcentration and determination of Cr(VI) at trace levels The optimal composition of the formation of Ca-alginate-chitosan-1,5-diphenylcarbazide microcapsules were 1% Na-alginate, 0.1M CaCl2 and 0.6 g resin. The retention capacity of resin modified was 2.2124 mg Cr (VI) /g resin at optimum pH 4-6. The analytical performance this method is good which are shown by the limit of detection was 1.14 μg/L and the reproducibility level shown by the percentage of the coefficient variance was 1.9563 %. This method was applied for Cr(VI) determination in river water samples collected from Karang Mumus and Mahakam Rivers, East Kalimantan, Indonesia.
1,5-Benzothiazepine scaffold is an important class of heterocycles and has featured in a number of clinically used drugs. Compounds bearing 1,5-benzothiazepine moiety shows a broad spectrum of biological activities such as CNS-acting agents, anti-HIV and anticancer drugs, angiotensin converting enzyme inhibitors, antimicrobial, calmodulin antagonists, bradykinin receptor agonists, as well as Ca2+ blockers.
Polyhydroxyalkanoates (PHAs) are a group of microbial biodegradable polymers having potential to replace synthetic plastics. Several factors are known to influence PHA biosynthesis e.g., bacterial strain used, carbon and nitrogen sources provided, culture conditions, etc. These factors interact with each other during productionand their interaction can be assessed using statistical methods. In the present study, Taguchi Design of Experiments is performed to find out the effect of six different factors viz. incubation period, medium: flask volume ratio, pH of production medium, concentration of maltose, yeast extract and sodium chloride at three levels on production of PHA with 18 well defined experiments (L18 Orthogonal Array). The data obtained was analyzed statistically and it was found that incubation period was the most significant factor contributing 28.84% to PHA production while concentration of maltose was found to be the least significant (1.81%) in the PHA production.
Cyclodextrin glycosyl transferase (CGTase; EC 2.4.1.19) is an enzyme which converts starch into cyclodextrins (CDs). Cyclodextrins are closed-ring structures in which six or more glucose units are joined by a-1, 4 glucosidic bonds. Cyclodextrins have applications in food, pharmaceutical and cosmetic industries. This paper reports the exploration of aerobic alkaliphilic bacteria from alkaline sodalake of Lonar, India for CGTase production. Paenibacillus sp L55 isolated from Lonar lake was used for production of CGTase. Three medium components Starch, Peptone and Yeast extract and initial pH of medium were optimised by Taguchi Design of Experiments (DOE). The contribution of starch in CGTase production was the highest while pH showed the least contribution in CGTase production. The optimised medium was used for CGTase production and the yield of CGTase was increased from 3 U/ml to 5.1 U/ml.
Aspergillus foetidus MTCC 10367 associated with industrial fruit waste sample from Galla food processing industry, Chittoor District, Andhra Pradesh, was isolated and identified using standard microbiological method (serial dilution-spread plate technique).This fungal isolate was screened for hydrolytic and depolymerising multiple enzymes of industrial importance. Many enzymes such as Pectinases, Cellulases, Proteases, Phytases and Amylases produced by Aspergillus foetidus have relevant biotechnological applications in several industrial areas. This study revealed the ability of Aspergillus foetidus to produce varieties of hydrolytic enzymes and provides additional information to support future research about industrial potential of Aspergillus foetidus MTCC 10367.
The tetraspanins are a superfamily of four-span membrane proteins that are widely expressed in mammalian cells. Although they have been implicated in important cell processes and some diseases, it has been difficult to characterise their exact functions. Tspan-11 is a recently identified member of the tetraspanin family. Little is known about Tspan-11; however sequence evidence indicates that Tspan-11 most closely resembles tetraspanin CD151. Recently, Tspan-11 GFP transfected CHO cells were used to immunize mice for generation of monoclonal antibodies (mAbs) and found that these mAbs bound to the surface of Tspan-11 GFP transfected CHO cells, indicating that they are able to recognize native forms of the tetraspanin. Surprisingly, one of cancer cell lines tested, the A549 lung adenocarcinoma cell line, was strongly positive for Tspan-11 mAbs, showing both intracellular and plasma membrane staining. Some preliminary investigations have been carried out on normal cells/tissues; these indicate that Tspan-11 is only expressed weakly, if at all on white blood cells, and may be present on epithelial cells in the colon. Taken together, these findings suggest that Tspan-11 has low, or restricted expression, or that the mAbs characterised so far recognize only some forms of the protein.
Asthma is a chronic respiratory syndrome. An Insilco study to identify possible drug target for blocking the 11-beta hydroxysteroid dehydrogenase (11-ßHSD) enzyme that catalyses the conversion of hydrocortisone to cortisone in the cholesterol metabolism the level of hydrocortisone, which plays a vital role in the control of asthma has been attempted. The inhibition of 11-βHSD by glycyrrhetinic acid, resulted in halting the inflammation in the epithelial cells and ultimately controlling the allergy and Asthma. In this work, we carried out docking studies of the protein 11-βHSD and ligand. Glycyrrhetinic acid, which reveals a better binding of the ligand to the protein. ME Dock, Patch Dock, Hex dock, Gold Dock has been used in this study to reveal the binding. The docking programs successfully works by binding the protein and the ligand gives very useful data about the enzyme values, hydrogen bonds between them, hydrophobic bonds, inter atomic contents between them, and the neighboring amino acids to which the drug has contact. All these studies will give insight in determining the property of the drug.
Hepatocarcinoma (HCC) and colorectal cancer (CRC) are the most malignant tumors with increasing incidences of morbidity and mortality globally.The aim of the present study was to determine in vitro antitumor activity of quercetin, gallic acid, and ellagic acid against HCC and CRC. This was achieved through testing the effects of these compounds on HepG2 and HCT 116 cells, ranging from cell growth inhibition assay and fold dose advantage, passing by mitochondrial activity assessment, to cellular protein content measurement. The efficacies of these compounds were compared with doxorubicin in case of HepG2 cells and 5-fluorouracil in case of HCT 116 cells. The present findings indicated that in both cell types, gallic acid elicited the most pronounced anti-cancer activity and mitochondrial dysfunction compared to quercetin and ellagic acid. Extensive research is warranted to assess the precise molecular mechanisms of these natural products in bridling HCC and CRC.
Bio prospecting of plants with anti-proliferative activity has been a major focus on the search of plants based cure. The pharmacological importance of Ceropegia species (Apocynaceae) is mainly due to the presence of a pyridine alkaloid 'Ceropegin' a potential antipyretic, analgesic, local anesthetic, antiulcer, mast-cell stabilizing, hepato-protective, tranquilizing, and hypotensive. Use of plant derived compounds as potent anticancer agents is of recent research interest. In the continuing effort to screen Ceropegia species (Ceropegia spiralis, Ceropegia juncea, and Ceropegia candelabrum) for anticancer activity, plants were collected, micro propagated and hardening. In-vitro propagated plants are collected, extracts tested for the activity using cell lines namely HCT-118 (Colon cancer cell) of the extracts from three species of same families tested (10,50,and100μg/ml). 10ug ofCeropegia spiralis showed 47.15% of cell death, which can be considered significant. Apoptosis was confirmed by acridine orange (AO) ethidium bromide (EB) fluorescent double staining which confirms the potent anticancer effect of ethyl acetate fraction of Ceropegia spiralis.
