Comparative role of pregabalin and carbamazepine regarding efficacy in painful diabetic neuropathy

Neuropathic pain is the most severe and resistant type of pain which has impact on quality of life ana behaviour; it most commonly occurs at night causing disturbed; sleep. Diabetes mellitus is a common cause of painful neuropathy. In this study, we are comparing the effectiveness of old treatment Carbamazepine with Pregabalin in painful diabetic neuropathy. The study was an open-label trial conducted in Diabetic Clinic of Medical Unit-Ill, Jinnah Postgraduate Medical Center, Karachi. The duration of the study was 90 days, from December 2010 to March 2011. The study has been approved from ethical committee of JPMC, Karachi with the reference NO.F.2-81/2010-GENL/195/JPMC. 60 established patients of painful diabetic peripheral neuropathy from Diabetic Clinic of Medical Unit-Ill OPD were included in the 90-day study, irrespective of gender, with duration of diabetes more than 10 years. All subjects are placed into two groups. In group A, comprising of 30 patients [n=30], Pregabalin was administered and in group B, also comprising of 30 patients [n=30], Carbamazepine. The intensity of pain was compared on visual analog scale of McGill pain questionnaire. In group A [Pregabalin], the mean pain score fell from 6.17+/-0.14 to 3.50+/-0.15 from day 0 to day 90 [p-value=0.001] and the percentage of change also in visual analog scale of McGill pain questionnaire was -43.31%. In group B [Carbamazepine], the changes in pain score from initially 6.07+/-0.14 falling to 4.23+/-0.13 from day 0 to day 90 [p-value=0.001] and the percentage of change was -30.31%. Pregabalin was observed to be more potent. Both drugs were well tolerated by all participants that also completed the entire duration of the trial

Three new anthraquinone derivatives isolated from Symplocos racemosa and their antibiofilm activity / 中国天然药物

Three new alkyl substituted anthraquinone derivatives, trivially named as symploquinones A-C (Compounds 1-3) were isolated from Symplocos racemosa. The structures of these compounds were determined on the basis of extensive spectroscopic analyses (UV, IR, Mass, H- and C-NMR, and two-dimensional (2D) NMR techniques). The resulting data were also compared with the reported literature. These compounds were then subjected to antibacterial or antibiofilm testing. Compounds 1 and 3 exhibited good antibacterial activity in the concentration range of 160-83 μg·mL against Streptococcus mutans, methicillin resistant Staphylococcus aureus and Proteus mirabilis. Both compounds were further screened for anti-biofilm activity, which revealed promising activities at sub-MIC concentrations. None of the compounds were found to be active against Klebsiella pneumoniae.

Analgesic activity of alkyl piperidine derivatives

Piperidine is the most significant scaffold which reveals therapeutic potential because of its conformationally flexible nature. During the course of present investigations synthetic quaternary salts of alkyl piperidine with various phenacyl bromides were explored for their possible analgesic activity. Compounds I analogs [1a-1f] and compound II analogs [IIa-IIf] showed varying degree of analgesic activity when compared with pethidine as standard and its duration by tail immersion method

Antimicrobial and antioxidant screening of N'-substituted sulphonyl and benzoyl derivatives of 4-Pyridine carboxylic acid hydrazide

In this research program, the antibacterial, antifungal and antioxidant activities of six N_-substituted sulfonyl and benzoyl derivatives of lead molecule PCH were reported. Out of these compounds, sulphonyl derivatives 2,3 and benzoyl derivative 5 showed moderate to good activity against different strains of gram-positive and gram-negative bacteria including B. cereus, B. subtilis, B. thruingiensis and S. pyogenes, S. fecalis and E. coli ATCC 8739. Moreover, upon antifungal screening, the compound, N?-[[2,4,6-trimethylbenzene] sulfonyl]pyridine-4-carbohydrazide possessed good antifungal activity against Candida species, a causative agent of systemic fungal infections. Antioxidant study demonstrated more than 50% inhibition in DPPH assay for sulphonyl derivative 2 indicating its potential as antioxidant while the other derivatives expressed low level of radical scavenging property

Antimalarial and insecticidal activities of newly synthesized derivatives of Benzimidazole

The bioactive benzimidazole and corresponding substituted phenacyl halides has been synthesized [11] new derivatives out of three compounds 8, 10 and 11 were found to inhibit the Plasmodium falciparum moderately after 72 hours of incubation hence acting as antimalarial agents. While these derivatives were exhibited negligible insecticidal activity too when analyzed by impregnated filter paper method

Synthesis of novel derivatives of 4-Pyridine carboxylic acid hydrazide and their activity on central nervous system

Six novel derivatives [2-7] of 4-Pyridine carboxylic acid hydrazide [PCH] were synthesized by treating this lead molecule with substituted arylsulphonyl and benzoyl chlorides

The molecular structures of the newly derived products were characterized by the help of UV Visible, IR, FAB, 1HNMR spectroscopy and CHN analysis

During the preliminary pharmacological screening, it was observed that the synthesized compounds induced noticeable changes on motor activity of the animals

Interesting structure activity relationship was also observed among the synthesized molecules. Because of the interesting affect on motor activity, the newly synthesized derivatives can further be evaluated for their effects on CNS

Antidepressant effect and categorization of Inhibitory activity of monoamine oxidase type A and B of ethanolic extract of seeds of Trigonella foenum graecum Linn

Trigonella foenum- graecum Linn [Fabaceae] is an annual aromatic herb and no wit is cultivated globally like in Pakistan, Egypt, India, Middle East etc. Traditionally it was used in anorexia, as febrifuge, to soothe gastritis and gastric ulcers, as a galactagogue and as condiment, hypoglycemic agent and employed in various as nervous disorders

The study aimed to investigate the antidepressant effect of ethanolic extract of seeds of Trigonella foenum graecum and underlying mechanism of action. For assessment of antidepressant activity Forced Swimming Test [FST], Tail Suspension Test [TST], Monoamine [MAO] Assay and Locomotor Activity Test were studied. Acute toxicity, Rota Rod and Grip Strength Tests were also performed. The significant declining in immobility time as compared to control was shown in Forced swimming test as compared to tail suspension test

Considerable change was not found in open field test [OFT]. EtOH extract of seeds of fenugreek represent maximum significant reduction which was 30 and 24.65%in MAO- A and B activity respectively in the rat's whole brain as compared to control animals in Monoamine oxidase [MAO] assay

All tested doses were found ineffective in impairment of muscle coordination in Rota rod and in grip strength related to muscle relaxant property. According to experimental findings it is revealed that ethanolic extract of seeds of Trigonella foenum graecum showed antidepressant effect by inhibiting the activity of MAO-A and B

Synthesis and cytotoxic activity of some derivatives of alkyl piperidine

Synthesis of novel phenacyl derivatives of alkyl piperidine as cytotoxic agents via simple and single step reaction procedure is going to be reported here. Twelve new compounds were successfully synthesized in moderate yield and in solid form. Their synthesis was confirmed by TLC, melting point, CHN analysis and through different spectral studies such as UV, IR, Mass and proton NMR. The advantages of this synthetic route are simple operation, mild reaction conditions and good yields. These newly synthesized derivatives were extensively explored for their cytotoxicity by brine shrimp lethality assay