Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone

Venkanna, Arramshetti,Cho, Kyo Hee,Dhorma, Lama Prema,Kumar, Duddukuri Nandan,Hah, Jung Mi,Park, Hyeung-geun,Kim, Sun Yeou,Kim, Mi-hyun Elsevier 2019 European journal of medicinal chemistry Vol.163 No.-

<P><B>Abstract</B></P> <P>Here we first time report an unprecedented and unnatural six-membered 1,5-oxaza spiroquinone scaffold with structural novelty, a convenient and efficient synthetic route was developed for the synthesis of new 1,5-oxaza spiroquinone derivatives (<B>1a-1r)</B> in high yields from readily available starting materials. The logic of the present work consists of (1) the identification of a promising unprecedented scaffold from privileged scaffolds of biological active molecules through our ‘Chemistry-oriented Synthesis’ (ChOS) approach, a compensatory strategy for target-based drug discovery, (2) the positioning of the identified 1,5-oxaza spiroquinone scaffold on neuroinflammation and neurodegenerative disease through nitric oxide (NO) inhibitory activity without cytotoxicity in hyper-activated microglia (IC<SUB>50</SUB> of NO production: 0.07–1.82 μM) to establish structure–activity relationship (SAR), (3) the investigation on the possibility as a selective kinase inhibitor related to neurodegenerative diseases (eg. JNK1, CDK2, DAPK1) through kinase full panel screening of the most potent compound <B>1n</B>, and (4) the evaluation on <I>in vivo</I> efficacy of the compound <B>1n</B> through Y-maze test.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Designed unprecedented 1,5-oxaza spiroquinone core with our ‘Chemistry-oriented Synthesis’ (ChOS) approach and synthetic route was developed for six-membered 1,5-oxaza spiroquinone core. </LI> <LI> Eighteen derivatives were synthesised, characterized and evaluated their neuroprotective effect. </LI> <LI> Compound <B>1n</B> displayed excellent effect on NO (Nitic Oxide) inhibition in BV-2 Cell lines with IC<SUB>50</SUB> values <B>0.07 ± 0.01</B> μM. </LI> <LI> Kinase screening and Molecular docking studies were performed with potent compound <B>1n</B> to explore kinase inhibition activity and its potential binding mechanisms. </LI> <LI> Compound <B>1n</B> could prevent spatial short-term memory deficits induced by scopolamine. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Design of a Robot Head Shaped Microstrip Patch Antennas for Multi-band Applications

P.Venkanna Chowdary,T.Mohan Krishna,A.Tathababu 보안공학연구지원센터 2015 International Journal of Signal Processing, Image Vol.8 No.8

In this paper, two different types of robot head shaped patch antennas are proposed and a comparative study is presented. Both the proposed antennas have same dimensions except at the mouth position. These antennas are fed by coaxial feeding technique and are etched on an FR-4 substrate with relative permittivity 4.4. The proposed antennas produce multiple bands resonating at 1.63 GHz, 5 GHz, 6.13 GHz, 6.91 GHz and 9.5 GHz frequencies with excellent return loss characteristics. These frequencies have applications in wireless, satellite, radar and mobile communications.

Conductivity enhancement in K+-ion conducting solid polymer electrolyte [PEG : KNO3] and its application as an electrochemical cell

Polu Anji Reddy,Kareem Aseel Abdulameer,Kim Kwangmin,Kim Dongkyu,Venkanna Mekala,Rasheed Hussein Kh.,Kumar Kanapuram Uday 한국화학공학회 2023 Korean Journal of Chemical Engineering Vol.40 No.12

The solution-cast method was used to prepare new solid polymer electrolytes (SPEs) that conduct potassium ions and are based on polyethylene glycol (PEG) complexed with potassium nitrate (KNO3). This polymer electrolyte system was characterized using different experimental techniques, such as X-ray diffraction (XRD), differential scanning calorimetry (DSC), composition vs. conductivity, temperature vs. conductivity, frequency-dependent conductivity, and dielectric measurements. The degree of crystallinity decreased with increasing salt concentration, according to the X-ray diffraction and DSC patterns of PEG with KNO3 salt. For PEG: KNO3 (80 : 20) composition, an optimum conductivity of 8.24× KT−6 S/cm was recorded at 30 °C. Compared with pure PEG, the optimum conducting composition (OCC) conductivity increased by two orders of magnitude. The temperature range of 303 to 333 K was used for the temperature-dependent conductivity experiments. The findings demonstrate that the conductivity obeys the Arrhenius rule and increases as the temperature rises. A dc plateau and a dispersive zone were observed in the conductance spectrum, which also follows Jonscher’s power law. It was investigated how temperature and frequency affect the dielectric permittivity. An electrochemical cell with the configuration K/(80PEG : 20KNO3)/(I2+C+electrolyte) was constructed using an 80 : 20 electrolyte system, and its discharge properties were investigated. The cell’s open circuit voltage was measured at 2.48 V.

IM-133N - A Useful Herbal Combination for Eradicating Disease-triggering Pathogens in Mice via Immunotherapeutic Mechanisms

Firashathulla, Syed,Inamdar, Mohammed Naseeruddin,Rafiq, Mohamed,Viswanatha, Gollapalle Lakshminarayanashastry,Kumar, Lakkavalli Mohan Sharath,Babu, Uddagiri Venkanna,Ramakrishnan, Shyam,Paramesh, Ran KOREAN PHARMACOPUNCTURE INSTITUTE 2016 Journal of pharmacopuncture Vol.19 No.1

Objectives: The present study was undertaken to evaluate the immunomodulatory (IM) activity of IM-133N, a herbal combination in various immunotherapeutic experimental models. Methods: The IM activity of IM-133N was evaluated against three experimental models namely, effect of IM-133N against Escherichia coli (E. coli)-induced abdominal sepsis in mice, and carbon clearance test was performed in Wistar albino rats to evaluated the phagocytic potential of IM-133N, in addition IM-133N was evaluated for its immunoglobulin enhancing potential in rats, where the immunoglobulin levels were measured by zinc sulphate turbity (ZST) test. Further, IM-133N was subjected for detailed liquid chromatography-mass spectrometry (LC-MS)/MS analysis to identify the probable active constituents present in it. Results: The findings of the present study has demonstrated very promising IM property of IM-133N in all the experimental models. Briefly, pretreatment with IM-133N at 125, 250, 500 and 1,000 mg/kg, p.o. doses had protected the mice against E. coli-induced abdominal sepsis and mortality, further the effect of IM-133N was found to be significant and dose-dependent. In support of this, in another study administration of IM-133N showed a significant and dose-dependent increase in serum immunoglobulin levels, estimated by ZST test. In line with the above findings, in the carbon clearance test the low doses (125 and 250 mg/kg, p.o.) of IM-133N increased the rate of carbon clearance, whereas the higher doses (500 and 1,000 mg/kg, p.o.) did not sustain the response, and saturation effect was considered as one of the possible reason for futility of higher doses for IM-133N. In addition, A detailed LC-MS/MS analysis of IM-133N showed 17 bioactive phytochemical constituents: namely, apigenin, chaulmoogric acid, mesquitol, quercetin, symphoxanthone, salireposide, ${\beta}$-sitosterol, nonaeicosanol, ${\beta}$-amyrin, betulic acid, oleanolic acid, symplososide, symponoside, symploveroside, symplocomoside, symconoside A and locoracemoside B. Conclusion: These findings suggest that IM-133N possesses significant IM activity and, hence, could be useful for eradicating opportunistic disease-triggering pathogens via immunotherapeutic mechanisms. The findings also suggest IM-133N may also useful in other immunity disorders.

IM-133N - A Useful Herbal Combination for Eradicating Disease-triggering Pathogens in Mice via Immunotherapeutic Mechanisms

Syed Firashathulla,Mohammed Naseeruddin Inamdar,Mohamed Rafiq,Gollapalle Lakshminarayanashastry Viswanatha,Lakkavalli Mohan Sharath Kumar,Uddagiri Venkanna Babu,Shyam Ramakrishnan,Rangesh Paramesh 대한약침학회 2016 Journal of pharmacopuncture Vol.19 No.1

Objectives: The present study was undertaken to evaluate the immunomodulatory (IM) activity of IM-133N, a herbal combination in various immunotherapeutic experimental models. Methods: The IM activity of IM-133N was evaluated against three experimental models namely, effect of IM- 133N against Escherichia coli (E. coli)-induced abdominal sepsis in mice, and carbon clearance test was performed in Wistar albino rats to evaluated the phagocytic potential of IM-133N, in addition IM-133N was evaluated for its immunoglobulin enhancing potential in rats, where the immunoglobulin levels were measured by zinc sulphate turbity (ZST) test. Further, IM-133N was subjected for detailed liquid chromatography-mass spectrometry (LC-MS)/MS analysis to identify the probable active constituents present in it. Results: The findings of the present study has demonstrated very promising IM property of IM-133N in all the experimental models. Briefly, pretreatment with IM-133N at 125, 250, 500 and 1,000 mg/kg, p.o. doses had protected the mice against E. coli-induced abdominal sepsis and mortality, further the effect of IM- 133N was found to be significant and dose-dependent. In support of this, in another study administration of IM-133N showed a significant and dose-dependent increase in serum immunoglobulin levels, estimated by ZST test. In line with the above findings, in the carbon clearance test the low doses (125 and 250 mg/ kg, p.o.) of IM-133N increased the rate of carbon clearance, whereas the higher doses (500 and 1,000 mg/kg, p.o.) did not sustain the response, and saturation effect was considered as one of the possible reason for futility of higher doses for IM-133N. In addition, A detailed LC-MS/MS analysis of IM-133N showed 17 bioactive phytochemical constituents: namely, apigenin, chaulmoogric acid, mesquitol, quercetin, symphoxanthone, salireposide, β-sitosterol, nonaeicosanol, β-amyrin, betulic acid, oleanolic acid, symplososide, symponoside, symploveroside, symplocomoside, symconoside A and locoracemoside B. Conclusion: These findings suggest that IM-133N possesses significant IM activity and, hence, could be useful for eradicating opportunistic disease-triggering pathogens via immunotherapeutic mechanisms. The findings also suggest IM-133N may also useful in other immunity disorders.