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Aim: This study aimed at screening and development of TG2 inhibitors as anti lung cancer agent. Background: Transglutaminase 2 (TG2) is multifunctional and ubiquitously expressed protein from the transglutaminase family. It takes part in various cellular processes and plays an important role in the pathogenesis of autoimmune, neurodegerative diseases, and also cancer. Objective : The proposed study focused on screening potent inhibitors of TG2 by in-silico method and synthesize their derivative as well as analyse its activity by utilizing an in-vitro approach. Material and Methods: Molecular docking studies have been carried out on the different classes of TG2 inhibitors against the target protein. Nearly thirty TG2 inhibitors were selected from literature and docking was performed against transglutaminase 2. The computational ADME property screening was also carried out to check their pharmacokinetic properties. The compounds which exhibited positive ADME properties with good interaction while possessing the least binding energy were further validated for their anti-lung cancer inhibition property against A549 cell lines using cytotoxicity studies. Results: The results of the present study indicate that the docked complex formed by cystamine showed better binding affinity towards target protein, so this derivative of cystamine was formed using 2,5 dihydrobenzoic acid. Invitro results revealed that both molecules proved to be good cytotoxic agents against A549 lung cancer (875.10, 553.22 μg/ml), respectively. Further, their activity needs to be validated on TG2 expressing lung cancer. Conclusion : Cystamine and its derivative can act as a potential therapeutic target for lung cancer but its activity should be further validated on TG2 expressing lung cancer.

A series of novel benzo[a]xanthen-11(12H)-one derivatives 4a–m were designed and subjected to docking studies. The title compounds were synthesized from 3-aryl-4-formylsydnones 1a–m, β-naphthol and dimedone in presence of molecular iodine as a catalyst and evaluated for their in vitro inhibitory effects on the hyaluronidase.

A series of novel benzothiazole based azo dyes were synthesized and fully characterized by using different analytical techniques. The antioxidant activity of synthesized azo dyes was studied with the DPPH, hydrogen peroxide, metal chelating and nitric oxide radical methods and compared with the known antioxidant ascorbic acid. Further, the anticancer properties of synthesized azo dyes were carried out against breast cancer (MCF-7) cell lines by MTT assay and results revealed that the synthesized compounds exhibited good anticancer property in micro-molar range. Additionally, the anti-inflammatory activities of target compounds were also investigated by protein denaturation method and were found to have effective anti-inflammatory property. In order to predict the binding modes and binding affinity of synthesized compounds, they were docked into the active sites of protein B-cell lymphoma-extra-large (Bcl-xL) to predict their anticancer property. The synthesized compounds were found to have good affinity for B-cell lymphoma-extra-large (Bcl-xL). A good correlation was found between in-silico docking analysis and in biological screening of all synthesized azo dyes with less binding energies and higher inhibition constants value against the target protein.

Aims: To evaluate the anthelminthic activity of Annona reticulata seeds extracts against Pheretima posthuma. Study Design: Helminth infections have tormented humans and animals for thousands of years. The indiscriminate uses of the anthelminthic drugs have lead to the emergence of resistant helminths against many anthelminthic agents. Thus the need for the treatment of helminthic infections and the prevention of the emergence of resistant strains has led to the screening medicinal plants for their anthelminthic activity. Place and Duration of Study: Department of Biotechnology, The Oxford College of Science, Bangalore, Karnataka, India, between January 2012 and March 2012. Methodology: The main aim of the present exploratory study is to evaluate the anthelminthic activity of A. reticulata seeds extracts. The in vitro studies revealed that the anthelminthic effects of crude chloroform and ethanolic extracts of A. reticulata on Pheretima posthuma was evident from induction of paralysis and mortality. Piperazine citrate was used as the standard reference drug and normal saline as a control group. Results: Among all the concentrations of chloroform and ethanolic extracts tested, 12.5 mg/ml showed significant (p

The wound healing promoting property of stem bark methanol extract of Semecarpus anacardium was evaluated at three different dosages by excision, incision and dead space wound models using Wistar albino rats. Framycetin skin ointment was used as standard. LD(50) of methanol extract was determined to be 500 mg kg(-1). In methanol extract (20% ointment) treated group, epithelialisation of the incision wound was faster with a high rate of wound contraction. The tensile strength of the incision wound was significantly increased when compared to other treated groups. The histological examination of the dead space wound model granulation tissue of the methanol extract (100 mg kg(-1)) treated group showed increased cross-linking of collagen fibres and absence of monocytes as compared to control. Methanol extract at 100 mg kg(-1) exhibited significant wound healing activity but was lesser than standard; whereas, in animals treated with 50 and 75 mg kg(-1) showed moderate activity. This investigation supported the ethnomedicinal claims of S. anacardium.

The prophylactic effects of oleanolic acid (OA) isolated from chloroform extract (CE) of Flaveria trinervia against ethanol induced liver toxicity was investigated using rats. CE and OA at three different doses were tested by administering orally to the ethanol treated animals during the last week of the 7 weeks study. Silymarin was used as the standard reference. The substantially elevated serum enzymatic levels of serum glutamate oxaloacetate transaminase, glutamate pyruvate transaminase, alkaline phosphatase and bilirubin in ethanol treated animals were restored towards normalcy by treatment of CE and OA. In vivo antioxidant and in vitro free radical scavenging activities were also positive for all the three concentrations of CE and OA. However, OA at 150 mg/kg showed significant activity when compared to the other two doses. Biochemical observations in support with histopathological examinations revealed that CE and OA possess hepatoprotective action against ethanol induced hepatotoxicity in rats.

A new tetra-aza macrocyclic ligand, L (C24H16N12O2S4) and its complexes of type, [MLCl2] and [CuL]Cl2 (where M = Ni(II), Co(II); L = N,N′-(benzene-1,3-diyldi-1,3,4-thiadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-thiadiazol-2-yl)amino]acetamide}) were synthesized and characterized by the spectral and analytical techniques. An octahedral geometry has been proposed for Ni(II) and Co(II) complexes while Cu(II) complex exhibit a square planar geometry. All the synthesized metal complexes were screened for their in vitro antimicrobial activity against selected species of pathogenic bacteria and fungi. The binding property of the complexes with CT-DNA was studied by absorption spectral analysis, followed by viscosity measurement and thermal denaturation studies. The photo induced cleavage studies revealed that the complexes possess photonuclease property against pUC19 DNA under UV–visible irradiation.

The antinociceptive activity of Flaveria trinervia extracts by tail-flicking and writhing methods was evaluated using mice. The abdominal writhing method was carried out by administering petroleum ether, chloroform and methanol extracts orally. After 1 h of incubation, 0.6% acetic acid (10 mL kg(-1)) was administered intraperitoneally. After 5 min, each group of mice was observed for the amount of writhing for a duration of 20 min. Acetyl salicylic acid was used as the standard reference. The tail-flick method was carried out using a thermal model and the maximum possible analgesia was calculated. The LD₅₀ values of petroleum ether, chloroform and methanol extracts were 700, 700 and 500 mg kg⁻¹, respectively. The methanol extract at 50 mg kg⁻¹ showed significant antinociceptive activity. The petroleum ether and chloroform extracts showed moderate antinociceptive activity at a dose of 70 mg kg⁻¹. The methanol extract showed more significant antinociceptive activity than the other extracts but was less effective than the standard. This investigation finds support for the ethnomedicinal claims of F. trinervia.

A B S t r A c t Helminths infections are also among the most common infections in human, affecting a large proportion of the world’s population in developing countries and produce a global burden of disease. Pherithema posthuma a helminthes is commonly known as earth-worms, Leucas aspera herb is distributed throughout India. the anthelminthic property of Leucas aspera was evaluated using Pherithema posthuma as an experimental model. Piperazine citrate was used as the standard reference. earthworm belonging to control group showed paralysis time as 64.33 min and death time as 200 min. Among the various concentrations of aqueous extract tested, concenration at 250 mg/ml showed efficient anthelminthic activity and among all the concentrations ethanol extract tested, concentration at 250 mg/ml gave significant results. This investigation revealed that ethanol extract of Leucas aspera showed significant anthelminthic activity against Pheretima posthuma when compared aqueous extract. Ethanol extract also proved to be efficient than the standard drug. this investigation supported the ethnomedical claims of Leucas aspera as anthelminthic plant.

The antibacterial activity, in-silico DNA molecular docking, DNA binding and photo cleavage studies of newly synthesized pyrazole is described. Antibacterial potential of these compounds screened against a wide range of Gram-positive and Gram-negative bacteria showed significant zone of inhibition and MIC with standard drug ciproflaxin is investigated. Among all the orientation of binding, fourth orientation showed significant binding and revealed that the binding and docking energy of 4a was -8.62 and -8.66 and inhibition constant 7.46 X e -6 . The absorption spectra showed the dynamic interaction with CT DNA and as proficient DNA intercalator (Kb = 4.5×10 4 M -1 ). The viscosity measurements and thermal denaturation affords the positive results towards DNA intercalation in both the studies. The light induced DNA damage was pragmatic in the absence of various ‘‘inhibitors’’ shows in photo cleavage activities at 360 nm.

Background: The analgesic activity of petroleum ether, chloroform and methanol extracts of Semecarpus anacardium was investigated by tail flicking and writhing method using acetyl salicylic acid as the standard reference. Materials and Methods: The staircase method was adopted for the determination of the acute toxicity. LD 50 of the petroleum ether extract and the chloroform extract was 700 mg/kg; however, the LD 50 for the methanol extract was 500 mg/kg. After 1 h of oral administration of the extracts, 0.6% acetic acid was administered intraperitoneally and the analgesic activity was evaluated. Results: The number of writhing observed in the control group was 73.33 writhes. The methanol extract showed a significant analgesic activity, with 28.33 writhes, than the petroleum ether extract and the chloroform extract. But, all the extracts showed proved to be less potent than the standard drug which showed 2.33 writhes. Animals pretreated with saline did not show a signify cant effect on the latent period of tail-flick response. The analgesic effect of the petroleum ether extract was comparatively less evident. The maximum possible analgesia (MPA) increased up to 9.1% which remained elevated above the basal levels throughout the observation period. The MPA calculated for the chloroform extract increased to 14.03%. However, the analgesic effect of the methanol extract was also observed at 0.5 h following oral administration and the effect remained significant throughout the 3 h observation period, and was increased to 20.43%. Conclusion: Consistent analgesic activity of all the three S. anacardium extracts was observed by both the methods. The methanol extract was more potent than the petroleum ether and chloroform extracts but was less effective than the standard drug. This investigation supported the ethnomedicinal claims of S. anacardium.

Objective To evaluate antinociceptive property of the leaf extract of Delonix elata (Linn.). Methods Antinociceptive activity was evaluated by abdominal writhing and tail flick methods in Swiss albino mice. Acetyl salicylic acid was used as standard drug. Results A dose dependent significant ( P P Conclusions The significant antinociceptive activity of the leaf extract is due to the presence of a single active constituent in higher levels or due to the combined effect of more than one phytoconstituent. This investigation supported the ethnomedicinal claims of Delonix elata .

A new series of N,N'-(benzene-1,3-diyldi-1,3,4-oxadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-oxadiazol-2-yl)amino]acetamide}(macrocycle 1), N,N'-(benzene-1,3-diyldi-1,3,4-thiadiazole-5,2-diyl)bis{2-[(5-benzene-1,3-diyl-1,3,4-thiadiazol-2-yl)amino]acetamide} (macrocycle 2) and S,S'-[benzene-1,3-diylbis(4H-1,2,4-triazole-5,3-diyl)]bis{[(5-benzene-1,3-diyl-4H-1,2,4-triazol-3-yl)sulfanyl]ethanethioate}(macrocycle 3) was synthesized from isophthalic dihydrazide (4) through a multistep reaction sequence. All the synthesized compounds were screened for their inhibitory effect against four different bacterial strains: P. aeruginosa ATCC-20852, K. pneumoniae MTCC-618, S. aureus ATCC- 29737, S. typhi MTCC- 3214. The synthesized compounds showed a significant zone of inhibition and the results were comparable with that of the standard drug ciprofloxacin. The synthesized compounds were further studied for their possible in vitro antioxidant effects by DPPH scavenging, total antioxidant capacity, total reductive capacity and H(2) O(2) scavenging activity. The results indicated that the in vitro antioxidant activity for all the three molecules was efficient when compared to the standards. The DNA interaction behavior of macrocycles 1-3 with CT-DNA was investigated by the absorption spectra obtained (K(b) constant for 1 is 4.53 × 10(4) M(-1) , for 2 is 5.75 × 10(4) M(-1) and for 3 is 5.86 × 10(4) M(-1) ). Based on the results it can be interpreted that the reducing power effect of the newly synthesized compounds demonstrates a direct effect on DNA binding and hence inhibiting the bacterial growth through their action on DNA by inhibiting DNA replication or DNA transcription.