Browsing by Author "Anil Kumar Mishra"

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A Step Towards Development and Bio-evaluation of a Novel Radio-ligand 99mTc-CYX-DTPA Targeting Sigma 2 Receptors
(Bentham Science Publishers, 2025) Ritika Chaudhary; Shubhra Chaturvedi; Divya Gautam; Vishakha Chaudhary; D. R. Sharma; Presenjit; Aastha Garg; Madhu Chopra; Anil Kumar Mishra
Introduction: Development of theranostics agents targeted towards particular receptors can effectively help in the management of cancer. The overexpression of the sigma-2 receptor (S2R) in tumors establishes it as a prominent biomarker for cancer cells. Methods: Radiotheranostics rely on the design of specific molecules having versatility in applications of diagnosis and therapy by merely changing the radioisotope. We have designed a novel radiotheranostic S2R-targeted ligand using cyclohexylpiperazine and performed docking studies to narrow down the potential efficacious ligand. The potential molecule with G-score = -7.0 kcal/mol, was then synthesized using a three steps reaction including conjugation of 2-(4-cyclohexylpiperazine-1-yl)ethyl(CYX) with DTPA chelator. Subsequently, the molecule has been radiolabelled with 99mTc using stannous chloride as a reducing agent, and a radiolabellieng efficiency of 95.0 ± 0.59% for 99mTc-CYX-DTPA. As proof of concept, the molecule has been evaluated for its binding affinity and specificity using sigma receptors isolated from the liver membrane homogenates of mice. The binding affinity was found to be Kd = 12.84 ± 0.395 nM; Bmax = 0.5258 ± 0.001 fmol/mg, indicating a high affinity for the receptors. Results: In addition, the molecule was also assessed for biocompatibility using haemolysis analysis and cytotoxicity on HEK cells and MDA-MB-23, wherein the molecule showed no significant cytotoxicity up to 72 h on HEK cells and 32.42% cytotoxicity on MDA-MB-231 cells. Conclusion: The future work will concentrate on the demonstration of in vivo targeting and site-specific accumulation of the molecule along with its suitability for theranostics applications. © 2025 Bentham Science Publishers.
Bolstering Buck Fertility: The Impact of Asparagus racemosus Aqueous Extract on Semen Cryopreservation and Antioxidant Defense System
(Mary Ann Liebert Inc., 2025) Chetna Gangwar; Ashok Kumar; Kumaresan Gururaj; Anshuman Kumar; Salauddin D. Qureshi; Manish Kumar; Anil Kumar Mishra; Ravi Ranjan
Importance of Study: Semen cryopreservation results in sperm damage due to lipid peroxidation or oxidative stress, leading to a decrease in conception rate. The sperm damage during cryopreservation can be minimized with the use of suitable antioxidant supplements in semen diluent. Some herbs have potent antioxidant potential and can be used in semen diluent to protect the spermatozoa. Objective: Hence, the investigation was planned to evaluate the effect of Asparagus racemosus (A. racemosus) aqueous extract on buck semen quality during cryopreservation. Methodology: In the current study, semen was collected from eight Sirohi bucks, and from each buck, 8 ejaculates were collected. Good-quality semen samples were pooled during each collection. Pooled semen samples were then divided into four equal parts and diluted in TRIS buffer containing different concentrations of A. racemosus aqueous extract (different groups, i.e., G I −5 mg, G II −2.5 mg, G III −1.25 mg, and G IV −0 mg of A. racemosus aqueous extract in 1 mL TRIS buffer). All the diluted semen samples were kept at equilibration temperature (5°C) for 2 hours and then cryopreserved by the manual method. Semen samples were evaluated for various sperm characteristics and antioxidant status before and after cryopreservation. Results: Asparagus racemosus aqueous extract showed significant (p < 0.05) enhancement of sperm viability, sperm motility, acrosomal integrity, and plasma membrane integrity, whereas it reduced sperm abnormality. Furthermore, in the experimental groups, the antioxidant gene expression was found to be increased compared to that of the treatment group. G III (p < 0.05) showed significantly better results in terms of sperm viability, sperm motility, acrosomal integrity, and plasma membrane integrity. Conclusion: Asparagus racemosus aqueous extract has the antioxidant potential to protect buck spermatozoa during semen cryopreservation. © 2025, Mary Ann Liebert, Inc., publishers.
Bolstering Buck Fertility: The Impact of Asparagus racemosus Aqueous Extract on Semen Cryopreservation and Antioxidant Defense System
(Mary Ann Liebert Inc., 2024) Chetna Gangwar; Ashok Kumar; K. Gururaj; Anshuman Kumar; Salauddin Qureshi; Manish Kumar; Anil Kumar Mishra; R. Ranjan
Importance of Study: Semen cryopreservation results in sperm damage due to lipid peroxidation or oxidative stress, leading to a decrease in conception rate. The sperm damage during cryopreservation can be minimized with the use of suitable antioxidant supplements in semen diluent. Some herbs have potent antioxidant potential and can be used in semen diluent to protect the spermatozoa. Objective: Hence, the investigation was planned to evaluate the effect of Asparagus racemosus (A. racemosus) aqueous extract on buck semen quality during cryopreservation. Methodology: In the current study, semen was collected from eight Sirohi bucks, and from each buck, 8 ejaculates were collected. Good-quality semen samples were pooled during each collection. Pooled semen samples were then divided into four equal parts and diluted in TRIS buffer containing different concentrations of A. racemosus aqueous extract (different groups, i.e., G I −5 mg, G II −2.5 mg, G III −1.25 mg, and G IV −0 mg of A. racemosus aqueous extract in 1 mL TRIS buffer). All the diluted semen samples were kept at equilibration temperature (5°C) for 2 hours and then cryopreserved by the manual method. Semen samples were evaluated for various sperm characteristics and antioxidant status before and after cryopreservation. Results: Asparagus racemosus aqueous extract showed significant (p < 0.05) enhancement of sperm viability, sperm motility, acrosomal integrity, and plasma membrane integrity, whereas it reduced sperm abnormality. Furthermore, in the experimental groups, the antioxidant gene expression was found to be increased compared to that of the treatment group. G III (p < 0.05) showed significantly better results in terms of sperm viability, sperm motility, acrosomal integrity, and plasma membrane integrity. Conclusion: Asparagus racemosus aqueous extract has the antioxidant potential to protect buck spermatozoa during semen cryopreservation. Copyright 2024, Mary Ann Liebert, Inc., publishers.
Design, synthesis, and in vitro antiproliferative activity of benzimidazole analogues for radiopharmaceutical efficacy
(2010) Sweta Singh; Himanshu Ojha; Anjani K. Tiwari; Nitin Kumar; Bachcha Singh; Anil Kumar Mishra
The synthesis of eight ligands by using 2-amino benzimidazole with different mono/bis aldehydes is described herein. The final products were characterized by spectral techniques such as FT-IR, 1H NMR, and EI-Mass. The structure-activity relationships of the benzimidazole derivatives are also reported. Studies on the complexation of the ligands with 99mTc were optimized by using stannous tartrate as reducing agent under various reaction conditions. The radiochemical stability was ≥95% for all the complexes, and they were to be stable for 12-14 hours in serum. Most of the ligands showed fast blood clearance. Biodistribution studies of the 99mTc complexes of these ligands showed no significant uptake in the brain or in the heart, and the clearance was mainly through the hepatobiliary system. Among the eight compounds evaluated for their antiproliferative activity in vitro, L8 produced good activity against the cancer cell lines A549 and PC-3. © Mary Ann Liebert, Inc.
Homology modeling, molecular docking and MD simulations study of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands
(Taylor and Francis Ltd., 2025) Vishakha Chaudhary; Shubhra Chaturvedi; Anju Wadhwa; Presenjit Verma; Divya Gautam; D. R. Sharma; Aastha Garg; Vishal Singh; Rupesh Kumar; Anil Kumar Mishra
The sigma-2 receptor has gathered attention as a promising target for cancer diagnosis and therapy since biochemical studies have evidenced the presence of the receptor in highly proliferating tumor cells. Computational drug design can help create targeted ligands against sigma-2, but a three-dimensional receptor structure is required as input. This study aims to develop a homology model of the human sigma-2 receptor. The template protein bovine sigma-2 (7m93) was aligned with the query sequence (Q5BJF2) to generate five models. These models were screened using potential energy parameters and molecular dynamics, with the model having the lowest energy and maximum stability being validated using stereo chemical parameters. The accepted model had 95.9% residues in allowed regions of the Ramachandran plot and an overall quality factor of 87.2611%. The model was tested using correlation analysis (R2= 0.744) of docking score and literature values of pKi. In addition, the model is used to understand the binding pattern of emerging selective 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline scaffold-based derivatives for designing ligands. The molecular dynamics studies of the model and ligand-bound model were performed for 100 ns to study the stability of the complexes, and the interactions compared with the known antagonist of sigma 2. © 2025 DRDO, India (previous affiliation). Published by Informa UK Limited, trading as Taylor & Francis Group.
Molecular detection of important abortion-causing microorganisms in preputial swab of breeding bucks using PCR-based assays
(Blackwell Publishing Ltd, 2020) Chetna Gangwar; Gururaj Kumaresan; Anil Kumar Mishra; Anshuman Kumar; Anjali Pachoori; Sonia Saraswat; Narendra Pratap Singh; Suresh Dinkar Kharche
Infectious diseases and aetiological agents related to female reproductive systems were extensively covered compared to its male counterpart. There needs a proper study to bridge this gap, where microflora and infectious agents of both male and female reproductive are mutually intelligible. With this study, we aimed to evaluate the microbial contamination of the preputial cavity and also screened for abortion-causing agents which are zoonotic as well. In goats, such types of abortions are caused by Brucella melitensis, Chlamydophila, Campylobacter and Coxiella etc. One of the major sources of contamination of semen is the preputial cavity, which is exposed to the external environment leading to spread of infection into the female via semen straws or by natural service. In the current study, good quality bucks (n = 32, Barbari = 12, Jamunapari = 10, Jakhrana = 10) which were routinely used for semen collection were screened for their preputial swabs, for the presence of the above pathogens. For detection of Brucella melitensis, OMP31 based TaqMan® probe real-time PCR assay was used, and for Chlamydia, 16srRNA gene based SYBR® green real-time PCR assay was employed for detection of Chlamydophila abortus. While for Campylobacter spp. and Coxiella burnetii, 16srRNA gene based conventional PCR and Trans-PCR were used, respectively. In the current study, of the screened preputial swabs, none of them showed positive for Brucella and Coxiella, but of the screened 32 samples 17 showed positive for Chlamydia (53.13%) and two (6.25%) showed positive for Campylobacter spp. The current study emphasizes on the farms and laboratories which were regularly involved in screening of brucellosis also often overlook the other potential non-brucella pathogens, causing abortions eventually incurring severe economic losses to the goat keepers. © 2020 Wiley-VCH GmbH
Retraction notice to “The role of ASIC1a in neuroprotection elicited by quercetin in focal cerebral ischemia” [Brain Res. Vol. 1383 (2011) 289–299] (Brain Research (2011) 1383 (289–299), (S0006899311001934), (10.1016/j.brainres.2011.01.085))
(Elsevier B.V., 2022) Anand Kumar Pandey; Puja Panwar Hazari; Ranjana Patnaik; Anil Kumar Mishra
This article has been retracted: please see Elsevier Policy on Article Withdrawal (http://www.elsevier.com/locate/withdrawalpolicy). This article is being retracted at the request of the Authors. The authors provided the following reasons: 1. The first author of the paper omitted the name of one of the contributors and did not disclose that he had been involved in similar studies at another Center. The results of these studies were previously published in another journal, resulting in a striking similarity between the images in this article and that of Mishra V et al., 2010 Neuropharmacology https://doi.org/10.1016/j.neuropharm.2010.08.015. 2. The authors were not able to reproduce the results of the Western blotting data given in the paper. It should be noted that the Editor-in-Chief has serious concerns about the fact that some images in these studies were previously published in unrelated studies in another journal. © 2021 Elsevier B.V.
Semen quality and total microbial load: An association study in important Indian Goat breeds during different seasons
(Blackwell Publishing Ltd, 2021) Chetna Gangwar; Anil Kumar Mishra; Kumaresan Gururaj; Anshuman Kumar; Suresh Dinkar Kharche; Sonia Saraswat; Ravindra Kumar; Natesan Ramachandran
The invasion of the male urogenital tract by microorganisms, and its subsequent effects on sperm fertilising ability, has not been well discussed in bucks. The present study was conducted to assess the bacterial load in fresh semen of the 2–6 years old bucks. For conducting the experiment, semen ejaculates from 18 bucks (6 from each breed namely Jakhrana, Jamunapari and Barbari) were used. We collected 5 ejaculates from each buck in each season (Summer-April to June, Rainy-July to Sept and Winter-November to January). Semen was collected with the artificial vagina (AV) method, and separate AV was used for each buck every time. The semen collection frequency was once in a week. Immediately after initial evaluation, collected semen samples were transferred to the microbiology laboratory of the institute. Thereafter, the semen samples were subjected to bacteriological examination to assess the microbial load. The results of the current study indicate that the microbial load in the semen was significantly (p < 0.05) higher in the Jamunapari bucks and in aged bucks. Bacteriospermia in different seasons was not significantly varied; however, nonsignificant increase in microbial load during the rainy season was observed. Overall, the average bacterial load in the semen of Jamunapari, Barbari and Jakhrana bucks was found 540.50 ± 55.88 CFU/ml, 391.81 ± 46.33CFU/ml and 388.93 ± 44.71 CFU/ml respectively. No significant difference in bacterial counts in the subsequent ejaculates among bucks was observed. Moreover, correlation analysis revealed that the proportions of motility, viability, plasma membrane integrity and acrosomal integrity were negatively influenced by the increased bacterial contamination of buck semen. © 2021 Wiley-VCH GmbH