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Authors = Amita Verma ORCID = 0000-0001-6653-7335

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22 pages, 1368 KiB  
Review
The Genus Ravenelia: Insights on Taxonomy, Diversity and Distribution
by Shubhi Avasthi, Ajay Kumar Gautam, Rajnish Kumar Verma, Kunhiraman C. Rajeshkumar, Mekala Niranjan, Amita Sharma, Samantha Chandranath Karunarathna and Nakarin Suwannarach
Pathogens 2024, 13(9), 775; https://doi.org/10.3390/pathogens13090775 - 9 Sep 2024
Viewed by 1460
Abstract
Ravenelia is the third largest rust genus of the order Pucciniales with more than 200 described species. It is an important rust genus that has undergone tremendous taxonomic changes. This genus produces teliospores united into a head on a compound pedicel composed of [...] Read more.
Ravenelia is the third largest rust genus of the order Pucciniales with more than 200 described species. It is an important rust genus that has undergone tremendous taxonomic changes. This genus produces teliospores united into a head on a compound pedicel composed of two to several hyphae with autoecious, macro-, demi- to hemi-, and, more rarely, microcyclic modes of their life cycle which provide it a unique identity and have proved helpful in the identification of the genus. The current understanding of the taxonomy, history, diversity and distribution of this genus is discussed in this paper. Both online and offline resources were searched to gather data of the published literature. The data thus obtained were analyzed for numerical and graphical summaries to provide the diversity and distribution of the genus. In addition, a phylogenetic analysis based on the ITS and nLSU DNA sequence data available in GenBank and the published literature was performed to examine the taxonomic placement of different species within the genus. The genus was reported to be distributed over 53 countries of the world. Around 51 plant genera belonging to four plant families, viz., Fabaceae, Phyllanthaceae, Asphodelaceae and Zygophyllaceae were found to be infected with these rust fungi. The phylogenetic analysis based on LSU and ITS sequence data revealed the polyphyletic nature of the genus. A table of 248 species of this genus is also provided with all information of host, distribution and cited reference that can be helpful for mycologists to find all information at one place. Future perspectives for the advancement of this genus are also discussed. Full article
(This article belongs to the Section Fungal Pathogens)
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14 pages, 1512 KiB  
Article
Assessment of Enterovirus Excretion and Identification of VDPVs in Patients with Primary Immunodeficiency in India: Outcome of ICMR–WHO Collaborative Study Phase-I
by Madhu Chhanda Mohanty, Mukesh Desai, Ahmad Mohammad, Amita Aggarwal, Geeta Govindaraj, Sagar Bhattad, Harsha Prasada Lashkari, Liza Rajasekhar, Harish Verma, Arun Kumar, Unnati Sawant, Swapnil Yashwant Varose, Prasad Taur, Reetika Malik Yadav, Manogat Tatkare, Mevis Fernandes, Umair Bargir, Sanjukta Majumdar, Athulya Edavazhippurath, Jyoti Rangarajan, Ramesh Manthri and Manisha Ranjan Madkaikaradd Show full author list remove Hide full author list
Vaccines 2023, 11(7), 1211; https://doi.org/10.3390/vaccines11071211 - 6 Jul 2023
Cited by 2 | Viewed by 2638
Abstract
The emergence of vaccine-derived polioviruses (VDPVs) in patients with Primary Immunodeficiency (PID) is a threat to the polio-eradication program. In a first of its kind pilot study for successful screening and identification of VDPV excretion among patients with PID in India, enteroviruses were [...] Read more.
The emergence of vaccine-derived polioviruses (VDPVs) in patients with Primary Immunodeficiency (PID) is a threat to the polio-eradication program. In a first of its kind pilot study for successful screening and identification of VDPV excretion among patients with PID in India, enteroviruses were assessed in stool specimens of 154 PID patients across India in a period of two years. A total of 21.42% of patients were tested positive for enteroviruses, 2.59% tested positive for polioviruses (PV), whereas 18.83% of patients were positive for non-polio enteroviruses (NPEV). A male child of 3 years and 6 months of age diagnosed with Hyper IgM syndrome was detected positive for type1 VDPV (iVDPV1) with 1.6% nucleotide divergence from the parent Sabin strain. E21 (19.4%), E14 (9%), E11 (9%), E16 (7.5%), and CVA2 (7.5%) were the five most frequently observed NPEV types in PID patients. Patients with combined immunodeficiency were at a higher risk for enterovirus infection as compared to antibody deficiency. The high susceptibility of PID patients to enterovirus infection emphasizes the need for enhanced surveillance of these patients until the use of OPV is stopped. The expansion of PID surveillance and integration with a national program will facilitate early detection and follow-up of iVDPV excretion to mitigate the risk for iVDPV spread. Full article
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68 pages, 12431 KiB  
Review
Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective
by Adarsh Kumar, Ankit Kumar Singh, Harshwardhan Singh, Veena Vijayan, Deepak Kumar, Jashwanth Naik, Suresh Thareja, Jagat Pal Yadav, Prateek Pathak, Maria Grishina, Amita Verma, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas and Pradeep Kumar
Pharmaceuticals 2023, 16(2), 299; https://doi.org/10.3390/ph16020299 - 14 Feb 2023
Cited by 178 | Viewed by 14785
Abstract
Cancer is one of the major healthcare challenges across the globe. Several anticancer drugs are available on the market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there is a dire need to develop [...] Read more.
Cancer is one of the major healthcare challenges across the globe. Several anticancer drugs are available on the market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there is a dire need to develop safer and target-specific anticancer drugs. More than 85% of all physiologically active pharmaceuticals are heterocycles or contain at least one heteroatom. Nitrogen heterocycles constituting the most common heterocyclic framework. In this study, we have compiled the FDA approved heterocyclic drugs with nitrogen atoms and their pharmacological properties. Moreover, we have reported nitrogen containing heterocycles, including pyrimidine, quinolone, carbazole, pyridine, imidazole, benzimidazole, triazole, β-lactam, indole, pyrazole, quinazoline, quinoxaline, isatin, pyrrolo-benzodiazepines, and pyrido[2,3-d]pyrimidines, which are used in the treatment of different types of cancer, concurrently covering the biochemical mechanisms of action and cellular targets. Full article
(This article belongs to the Special Issue Nitrogen Containing Scaffolds in Medicinal Chemistry)
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11 pages, 967 KiB  
Article
Durability of ChAdOx1 nCoV-19 (Covishield®) Vaccine Induced Antibody Response in Health Care Workers
by Alka Verma, Amit Goel, Harshita Katiyar, Prachi Tiwari, Mayank, Asari Sana, Dheeraj Khetan, Dharmendra Singh Bhadauria, Ajay Raja, Neelam Khokher, Shalimar, Ratendra Kumar Singh and Amita Aggarwal
Vaccines 2023, 11(1), 84; https://doi.org/10.3390/vaccines11010084 - 30 Dec 2022
Cited by 7 | Viewed by 2149
Abstract
(i) Background: ChAdOx1 nCoV-19 (Covishield®) vaccine is widely used in India. We studied the Covishield® induced antibody response and its durability among health care workers (HCWs) (ii) Method: HCWs received two doses (0.5 mL) four weeks apart. Blood specimens, collected [...] Read more.
(i) Background: ChAdOx1 nCoV-19 (Covishield®) vaccine is widely used in India. We studied the Covishield® induced antibody response and its durability among health care workers (HCWs) (ii) Method: HCWs received two doses (0.5 mL) four weeks apart. Blood specimens, collected before each dose, day (D)60, D150 and D270 after second dose, were tested for anti-spike antibody (ASAb) titre and neutralising antibody (%) (NAb) using Elecsys Anti-SARS-CoV-2 S (Roche) and SARS-CoV-2 NAb ELISA Kit (Invitrogen), respectively. Data are expressed as proportions and median (interquartile range) and compared using non-parametric (iii) Result: Among 135 HCWs (83 males; age 45 (37–53); 36 had pre-existing ASAb), 29 (21.5%) acquired COVID-19 after 60 (39–68) days of vaccination. ASAb titre before second dose and at D60, D150, D270 were 77.2 (19.4–329.4), 512 (114.5–9212), 149 (51.6–2283) and 2079 (433.9–8644) U/mL, respectively. Compared to those without pre-existing ASAb, titres were significantly higher before second dose (5929 vs. 41, p < 0.001), D60 (3395 vs. 234, p = 0.007) and D150 (1805 vs. 103, p < 0.001) in participants with pre-existing ASAb; NAb were also higher (80 vs. 18, p < 0.001) before second dose. Between those who acquired infection or not after vaccination, ASAb titres were comparable before second dose (77 vs. 78, p = 0.362) but significantly higher at D60 (14,019 vs. 317, p < 0.001) and D150 (2062 vs. 121, p = 0.002) in the former group, though NAb percentage were higher at D60 (87 vs. 27, p < 0.001) and D150 (79 vs. 25, p = 0.007) only (iv) Conclusions: Covishield® induces a higher antibody titre in those with pre-existing ASAb. The vaccine induced antibody starts falling 5 months after vaccination. Full article
(This article belongs to the Special Issue COVID-19 Vaccines and Immune Response)
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16 pages, 2320 KiB  
Article
Guava Leaf Essential Oil as a Potent Antioxidant and Anticancer Agent: Validated through Experimental and Computational Study
by Ashok Kumar Mandal, Samrat Paudel, Anisha Pandey, Parasmani Yadav, Prateek Pathak, Maria Grishina, Mariusz Jaremko, Abdul-Hamid Emwas, Habibullah Khalilullah and Amita Verma
Antioxidants 2022, 11(11), 2204; https://doi.org/10.3390/antiox11112204 - 7 Nov 2022
Cited by 20 | Viewed by 6651
Abstract
Several drugs now employed in cancer therapy were discovered as a result of anticancer drug research based on natural products. Here, we reported the in vitro antioxidant and anticancer activity followed by in silico anticancer and estrogen-like activity of Psidium guajava L. essential [...] Read more.
Several drugs now employed in cancer therapy were discovered as a result of anticancer drug research based on natural products. Here, we reported the in vitro antioxidant and anticancer activity followed by in silico anticancer and estrogen-like activity of Psidium guajava L. essential oil against ER-α receptors which lead to potential inhibitory action against breast cancer pathways. Methods: The bioactive compounds in guava essential oil were screened using gas chromatography–mass spectrometry (GC-MS). Similarly, the antioxidant properties of the extracted oil were evaluated using 2,2-Diphenyl-1-picrylhydrazyl scavenging assay. Furthermore, the in vitro anticancer activity of guava oil was observed through the MTT assay and an in silico molecular docking experiment was also carried out to ensure that they fit into the estrogen receptors (ERs) and possess anticancer potential. Results: The GC–MS profile of the essential oil revealed the presence of 17 chemicals, with limonene (51.3%), eucalyptol (21.3%), caryophyllene oxide (6.2%), caryophyllene (5.6%), and nerolidol (4.5%) occupying more than one-third of the chromatographic spectrum zone. Guava leaves’ essential oil (EO) inhibited DPPH (2,2-diphenyl-1-picrylhydrazyl) radicals and exhibited concentration dependent free radical scavenging activity, acting as a potent antioxidant with an IC50 value of 29.3 ± 0.67 µg/mL. The outcome of the MTT assay showed that the extracted guava oil had nearly the same efficacy against breast and liver cancer cells at a low concentration (1 µg/mL), giving 98.3 ± 0.3% and 98.5 ± 0.4% cell viability against HepG2 at 1 µg/mL, respectively. When the concentration of essential oil was increased, it showed a small reduction in the percentage of viable cells. While conducting an in silico study of all the screened compounds, the potential for hydroxycaryophyllene, caryophyllene, caryophyllene oxide, humulene, terpineol, and calamenene to inhibit tumor growth was bolstered due to a resemblance to 4-hydroxytamoxifen, thereby implying that these compounds may act as selective estrogen receptor modulators (SERMs). The ADME analysis of the compounds indicated above revealed that they exhibit excellent drug likeness properties and follow the Lipinski rule of five. Conclusions: Consequently, they have a substantial anticancer therapeutic potential and can be used for novel drug discovery in the effort to minimize the global burden of breast cancer. Full article
(This article belongs to the Special Issue Antioxidant Potential of Extracts from Foods and Plants)
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30 pages, 2760 KiB  
Review
Application of Nanotechnology in COVID-19 Infection: Findings and Limitations
by Ibrahim A. Shehu, Muhammad K. Musa, Aparna Datta and Amita Verma
J. Nanotheranostics 2022, 3(4), 203-232; https://doi.org/10.3390/jnt3040014 - 2 Nov 2022
Cited by 2 | Viewed by 4715
Abstract
There is an urgent need to address the global mortality of the COVID-19 pandemic, as it reached 6.3 million as of July 2022. As such, the experts recommended the mass diagnosis of SARS-CoV-2 infection at an early stage using nanotechnology-based sensitive diagnostic approaches. [...] Read more.
There is an urgent need to address the global mortality of the COVID-19 pandemic, as it reached 6.3 million as of July 2022. As such, the experts recommended the mass diagnosis of SARS-CoV-2 infection at an early stage using nanotechnology-based sensitive diagnostic approaches. The development of nanobiosensors for Point-of-Care (POC) sampling of COVID-19 could ensure mass detection without the need for sophisticated laboratories or expert personnel. The use of Artificial Intelligence (AI) techniques for POC detection was also proposed. In addition, the utilization of various antiviral nanomaterials such as Silver Nanoparticles (AgNPs) for the development of masks for personal protection mitigates viral transmission. Nowadays, nano-assisted vaccines have been approved for emergency use, but their safety and effectiveness in the mutant strain of the SARS-CoV-2 virus remain challenging. Methodology: Updated literature was sourced from various research indexing databases such as PubMed, SCOPUS, Science Direct, Research Gate and Google Scholars. Result: We presented the concept of novel nanotechnology researched discovery, including nano-devices, electrochemical biosensing, nano-assisted vaccine, and nanomedicines, for use in recent times, which could be a formidable step for future management of COVID-19. Full article
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10 pages, 800 KiB  
Article
Serological Immune Response Following ChAdOx1 nCoV-19 Vaccine (Covishield®) in Patients with Liver Cirrhosis
by Amit Goel, Alka Verma, Prachi Tiwari, Harshita Katiyar, Amita Aggarwal, Dheeraj Khetan, Mayank, Ravi V. Krishna Kishore, Pankaj Kumar, Thakur Prashant Singh, Sabreena Sheikh, Manas Vaishnav, Piyush Pathak and Shalimar
Vaccines 2022, 10(11), 1837; https://doi.org/10.3390/vaccines10111837 - 30 Oct 2022
Cited by 9 | Viewed by 2503
Abstract
Introduction: Data are limited on antibody response to the ChAdOx1 nCoV-19 vaccine (AZD1222; Covishield®) in cirrhosis. We studied the antibody response following two doses of the ChAdOx1 vaccine, given 4–12 weeks apart, in cirrhosis. Methods: Prospectively enrolled, 131 participants (71% males; [...] Read more.
Introduction: Data are limited on antibody response to the ChAdOx1 nCoV-19 vaccine (AZD1222; Covishield®) in cirrhosis. We studied the antibody response following two doses of the ChAdOx1 vaccine, given 4–12 weeks apart, in cirrhosis. Methods: Prospectively enrolled, 131 participants (71% males; age 50 (43–58); alcohol-related etiology 14, hepatitis B 33, hepatitis C 46, cryptogenic 21, autoimmune 9, others 8; Child–Turcott–Pugh class A/B/C 52/63/16). According to dose intervals, the participants were grouped as ≤6 weeks (group I), 7–12 weeks (group II), and 13–36 weeks (group III). Blood specimens collected at ≥4 weeks after the second dose were tested for anti-spike antibody titre (ASAb; positive ≥ 0.80 U/mL) and neutralizing antibody (NAb; positive ≥20% neutralization) using Elecsys Anti-SARS-CoV-2 S (Roche) and SARS-CoV-2 NAb ELISA Kit (Invitrogen), respectively. Data are expressed as number (proportion) and median (interquartile range) and compared using non-parametric tests. Results: Overall, 99.2% and 84% patients developed ASAb (titre 5440 (1719–9980 U/mL)) and NAb (92 (49.1–97.6%)), respectively. When comparing between the study groups, the ASAb titres were significantly higher in group II than in group I (2613 (310–7518) versus 6365 (2968–9463), p = 0.027) but were comparable between group II and III (6365 (2968–9463) versus 5267 (1739–11,653), p = 0.999). Similarly, NAb was higher in group II than in group I (95.5 (57.6–98.0) versus 45.9 (15.4–92.0); p < 0.001), but not between the groups II and III (95.5 (57.6–98.0) versus 92.4 (73.8–97.5); p = 0.386). Conclusion: Covishield® induces high titres of ASAb and NAb in cirrhosis. A higher titre is achieved if two doses are given at an interval of more than six weeks. Full article
(This article belongs to the Section COVID-19 Vaccines and Vaccination)
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9 pages, 883 KiB  
Article
Antibody Response to ChAdOx1 nCoV-19 (AZD1222) Vaccine in Kidney Transplant Recipients
by Dharmendra S. Bhadauria, Harshita Katiyar, Amit Goel, Prachi Tiwari, Ravi V. Krishna Kishore, Amita Aggarwal, Alka Verma, Dheeraj Khetan, Anupma Kaul, Monika Yachha, Manas Ranjan Behera, Brijesh Yadav and Narayan Prasad
Vaccines 2022, 10(10), 1693; https://doi.org/10.3390/vaccines10101693 - 11 Oct 2022
Cited by 7 | Viewed by 7807
Abstract
Kidney transplant recipients (KTRs) are at a much higher risk of complications and death following COVID-19 and are poor vaccine responders. The data are limited on the immune response to Covishield® in KTRs. We prospectively recruited a cohort of 67 KTRs aged [...] Read more.
Kidney transplant recipients (KTRs) are at a much higher risk of complications and death following COVID-19 and are poor vaccine responders. The data are limited on the immune response to Covishield® in KTRs. We prospectively recruited a cohort of 67 KTRs aged >18 between April 2021 and December 2021. Each participant was given two intramuscular doses of Covishield®, each of 0.5 mL, at an interval of 12 weeks. A blood specimen of 5.0 mL was collected from each participant at two points within a few days before administering the first dose of the vaccine and at any time between 4–12 weeks after administering the second dose. The sera were tested for anti-RBD antibody (ARAb) titre and neutralising antibody (NAb). An ACE2 competition assay was used as a proxy for virus neutralization. According to the prior COVID-19 infection, participants were grouped as (i) group A: prior symptomatic COVID-19 infection, (ii) group B: prior asymptomatic COVID-19 infection as evidenced by detectable ARAb in the prevaccination specimen, (iii) Group C: no prior infection with COVID-19, (iv) group D: Unclassified, i.e., participants had no symptoms suggestive of COVID-19, but their prevaccination specimen was not available for ARAb testing before vaccination. Fifty of sixty-seven participants (74.6%) provided paired specimens (group A 14, group B 27, and group C 9) and 17 participants (25.4%) provided only postvaccination specimens (group D). In the overall cohort (n = 67), 91% and 77.6% of participants developed ARAb and NAb, respectively. Their ARAb titre and NAb proportion were 2927 (520–7124) U/mL and 87.9 (24.4–93.2) %, respectively. Their median ARAb titre increased 65.6 folds, from 38.2 U/mL to 3137 U/mL. Similarly, the proportion of participants with NAb increased from 56% to 86%, and the NAb proportion raised 2.7 folds, from 23% to 91%. A comparison of vaccine response between the study groups showed that all those with or without prior COVID-19 infection showed a significant rise in ARAb titre (p < 0.05) and NAb proportion (p < 0.05) after the two doses of vaccine administration. The median value of folds rise in anti-RBD and NAb between groups A and B were comparable. Hence, ARAb is present in more than 3/4th of KTRs before the ChAdOx1 vaccine in India. The titer of ARAb and the proportion of NAb significantly increased after the two doses of the ChAdOx1 vaccine in KTRs. Full article
(This article belongs to the Section COVID-19 Vaccines and Vaccination)
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93 pages, 41287 KiB  
Review
Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids
by Ankit Kumar Singh, Adarsh Kumar, Harshwardhan Singh, Pankaj Sonawane, Harshali Paliwal, Suresh Thareja, Prateek Pathak, Maria Grishina, Mariusz Jaremko, Abdul-Hamid Emwas, Jagat Pal Yadav, Amita Verma, Habibullah Khalilullah and Pradeep Kumar
Pharmaceuticals 2022, 15(9), 1071; https://doi.org/10.3390/ph15091071 - 28 Aug 2022
Cited by 135 | Viewed by 10005
Abstract
Cancer is a complex disease, and its treatment is a big challenge, with variable efficacy of conventional anticancer drugs. A two-drug cocktail hybrid approach is a potential strategy in recent drug discovery that involves the combination of two drug pharmacophores into a single [...] Read more.
Cancer is a complex disease, and its treatment is a big challenge, with variable efficacy of conventional anticancer drugs. A two-drug cocktail hybrid approach is a potential strategy in recent drug discovery that involves the combination of two drug pharmacophores into a single molecule. The hybrid molecule acts through distinct modes of action on several targets at a given time with more efficacy and less susceptibility to resistance. Thus, there is a huge scope for using hybrid compounds to tackle the present difficulties in cancer medicine. Recent work has applied this technique to uncover some interesting molecules with substantial anticancer properties. In this study, we report data on numerous promising hybrid anti-proliferative/anti-tumor agents developed over the previous 10 years (2011–2021). It includes quinazoline, indole, carbazole, pyrimidine, quinoline, quinone, imidazole, selenium, platinum, hydroxamic acid, ferrocene, curcumin, triazole, benzimidazole, isatin, pyrrolo benzodiazepine (PBD), chalcone, coumarin, nitrogen mustard, pyrazole, and pyridine-based anticancer hybrids produced via molecular hybridization techniques. Overall, this review offers a clear indication of the potential benefits of merging pharmacophoric subunits from multiple different known chemical prototypes to produce more potent and precise hybrid compounds. This provides valuable knowledge for researchers working on complex diseases such as cancer. Full article
(This article belongs to the Special Issue Hybrid Drugs: Design and Applications)
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13 pages, 2551 KiB  
Article
Debelalactone Prevents Hepatic Cancer via Diminishing the Inflammatory Response and Oxidative Stress on Male Wistar Rats
by Prateek Pathak, Vikas Kumar, Habibullah Khalilullah, Maria Grishina, HariOm Singh and Amita Verma
Molecules 2022, 27(14), 4499; https://doi.org/10.3390/molecules27144499 - 14 Jul 2022
Cited by 5 | Viewed by 2035
Abstract
The current study was conducted to exemplify the effect of debelalactone on tissue protection, chronic hepatic inflammation, hepatic protection and oxidative stress induced by diethyl nitrosamine in Wistar rats. Therefore, DEN (200 mg/kg) was used for the induction the hepatocellular carcinoma (HCC) and [...] Read more.
The current study was conducted to exemplify the effect of debelalactone on tissue protection, chronic hepatic inflammation, hepatic protection and oxidative stress induced by diethyl nitrosamine in Wistar rats. Therefore, DEN (200 mg/kg) was used for the induction the hepatocellular carcinoma (HCC) and the level of serum alpha fetoprotein was used for the estimation and confirmation of HCC. The study illustrated that debelalactone (DL) significantly downregulated the hepatic, non-hepatic parameters such as aspartate aminotransferase, alanine aminotransferase, alpha fetoprotein, NO levels, total protein, albumin, blood urea nitrogen, total bilirubin, and direct bilirubin in dose dependent manner, as well as noticeably improving the body weight, of treated animals. The macroscopically observation of DEN-induced rat liver showed the formation of informalities in liver tissue, which was reduced with treatment of DL at dose dependent manner. However, antioxidant markers and inflammatory mediators such as lipid peroxidation, catalase, superoxide dismutase, glutathione peroxidase and transferase, TNF-α, IL-1β, IL-6, and NF-kB restored up to the normal level by DL. The histopathology studies showed that the treated group of animals returned to a normal status. Collectively, it can be concluded that debelalactone mediated chemoprevention in the DEN-induced rats via an increase in the activities of endogenous enzymes and/or inhibition the precancerous cells. Full article
(This article belongs to the Section Natural Products Chemistry)
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33 pages, 5765 KiB  
Article
Synthesis and Evaluation of Anti-HIV Activity of Mono- and Di-Substituted Phosphonamidate Conjugates of Tenofovir
by Aaminat Qureshi, Louise A. Ouattara, Naglaa Salem El-Sayed, Amita Verma, Gustavo F. Doncel, Muhammad Iqbal Choudhary, Hina Siddiqui and Keykavous Parang
Molecules 2022, 27(14), 4447; https://doi.org/10.3390/molecules27144447 - 12 Jul 2022
Cited by 2 | Viewed by 3323
Abstract
The activity of nucleoside and nucleotide analogs as antiviral agents requires phosphorylation by endogenous enzymes. Phosphate-substituted analogs have low bioavailability due to the presence of ionizable negatively-charged groups. To circumvent these limitations, several prodrug approaches have been proposed. Herein, we hypothesized that the [...] Read more.
The activity of nucleoside and nucleotide analogs as antiviral agents requires phosphorylation by endogenous enzymes. Phosphate-substituted analogs have low bioavailability due to the presence of ionizable negatively-charged groups. To circumvent these limitations, several prodrug approaches have been proposed. Herein, we hypothesized that the conjugation or combination of the lipophilic amide bond with nucleotide-based tenofovir (TFV) (1) could improve the anti-HIV activity. During the current study, the hydroxyl group of phosphonates in TFV was conjugated with the amino group of L-alanine, L-leucine, L-valine, and glycine amino acids and other long fatty ester hydrocarbon chains to synthesize 43 derivatives. Several classes of derivatives were synthesized. The synthesized compounds were characterized by 1H NMR, IR, UV, and mass spectrometry. In addition, several of the synthesized compounds were evaluated as racemic mixtures for anti-HIV activity in vitro in a single round infection assay using TZM-bl cells at 100 ng/mL. TFV (1) was used as a positive control and inhibited HIV infection by 35%. Among all the evaluated compounds, the disubstituted heptanolyl ester alanine phosphonamidate with naphthol oleate (69), pentanolyl ester alanine phosphonamidate with phenol oleate (62), and butanolyl ester alanine phosphonamidate with naphthol oleate (87) ester conjugates of TFV were more potent than parent drug TFV with 79.0%, 76.5%, 71.5% inhibition, respectively, at 100 ng/mL. Furthermore, two fatty acyl amide conjugates of tenofovir alafenamide (TAF) were synthesized and evaluated for comparative studies with TAF and TFV conjugates. Tetradecanoyl TAF conjugate 95 inhibited HIV infection by 99.6% at 100 ng/mL and showed comparable activity to TAF (97–99% inhibition) at 10–100 ng/mL but was more potent than TAF when compared at molar concentration. Full article
(This article belongs to the Special Issue Antiviral Agents for RNA-Virus Infection)
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34 pages, 5815 KiB  
Review
Phytochemistry, Pharmacology, and Nutraceutical Profile of Carissa Species: An Updated Review
by Jyoti Dhatwalia, Amita Kumari, Rachna Verma, Navneet Upadhyay, Ishita Guleria, Sohan Lal, Shabnam Thakur, Kasahun Gudeta, Vikas Kumar, Jane C.-J. Chao, Somesh Sharma, Ashwani Kumar, Amanda-Lee Ezra Manicum, José M. Lorenzo and Ryszard Amarowicz
Molecules 2021, 26(22), 7010; https://doi.org/10.3390/molecules26227010 - 20 Nov 2021
Cited by 40 | Viewed by 7376
Abstract
Carissa, a genus of the Apocynaceae family, consists of evergreen species, such as shrubs as well as small trees that are native to Asia, Africa, and Oceania’s subtropical and tropical regions. Most of the Carissa species are traditionally used to treat various [...] Read more.
Carissa, a genus of the Apocynaceae family, consists of evergreen species, such as shrubs as well as small trees that are native to Asia, Africa, and Oceania’s subtropical and tropical regions. Most of the Carissa species are traditionally used to treat various diseases, such as chest pain, headaches, gonorrhoea, rheumatism, syphilis, oedema, rabies, stomach pain, hepatitis, cardiac diseases, and asthma. The pharmacological studies on Carissa species revealed its antioxidant, antimicrobial, anticancer, cardioprotective, antipyretic, analgesic, wound healing, anticonvulsant, antiarthritic, adaptogenic, anti-inflammatory, and antidiabetic activities, thus validating its use in indigenous medicine systems. The review article summarised the comprehensive literature available, including morphology, indigenous uses, bioactive composition, nutraceutical, and pharmacological activities of Carissa species. A total of 155 research papers were cited in this review article. The Carissa fruits are rich in dietary fibre, lipids, proteins, carbohydrates, vitamin C, and macro- and micro-elements. A total of 121 compounds (35 polyphenols (flavonoids and phenolic acids), 30 lignans, 41 terpenoids, 7 steroids, 2 coumarins, and 6 cardiac glycosides) have been extracted from C. spinarum, C. carandas, and C. macrocarpa. Among all chemical constituents, lupeol, carissol, naringin, carisssone, scopoletin, carissaeduloside A, D, J, carandinol, sarhamnoloside, carissanol, olivil, carinol, 3β-hydroxyolean-11-en-28,13β-oilde, ursolic acid, and carissone are the key bioactive constituents responsible for pharmacological activities of genus Carissa. The gathered ethnopharmacological information in the review will help to understand the therapeutic relevance of Carissa as well as paving a way for further exploration in the discovery of novel plant-based drugs. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources (2020, 2021))
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13 pages, 1903 KiB  
Article
An Epidemiological Analysis of SARS-CoV-2 Genomic Sequences from Different Regions of India
by Pragya D. Yadav, Dimpal A. Nyayanit, Triparna Majumdar, Savita Patil, Harmanmeet Kaur, Nivedita Gupta, Anita M. Shete, Priyanka Pandit, Abhinendra Kumar, Neeraj Aggarwal, Jitendra Narayan, Neetu Vijay, Usha Kalawat, Attayur P. Sugunan, Ashok Munivenkatappa, Tara Sharma, Sulochna Devi, Tapan Majumdar, Subhash Jaryal, Rupinder Bakshi, Yash Joshi, Rima Sahay, Jayanti Shastri, Mini Singh, Manoj Kumar, Vinita Rawat, Shanta Dutta, Sarita Yadav, Kaveri Krishnasamy, Sharmila Raut, Debasis Biswas, Biswajyoti Borkakoty, Santwana Verma, Sudha Rani, Hirawati Deval, Disha Patel, Jyotirmayee Turuk, Bharti Malhotra, Bashir Fomda, Vijaylakshmi Nag, Amita Jain, Anudita Bhargava, Varsha Potdar, Sarah Cherian, Priya Abraham, Anjani Gopal, Samiran Panda and Balram Bhargavaadd Show full author list remove Hide full author list
Viruses 2021, 13(5), 925; https://doi.org/10.3390/v13050925 - 17 May 2021
Cited by 30 | Viewed by 7143
Abstract
The number of Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) cases is increasing in India. This study looks upon the geographic distribution of the virus clades and variants circulating in different parts of India between January and August 2020. The NPS/OPS from representative positive [...] Read more.
The number of Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) cases is increasing in India. This study looks upon the geographic distribution of the virus clades and variants circulating in different parts of India between January and August 2020. The NPS/OPS from representative positive cases from different states and union territories in India were collected every month through the VRDLs in the country and analyzed using next-generation sequencing. Epidemiological analysis of the 689 SARS-CoV-2 clinical samples revealed GH and GR to be the predominant clades circulating in different states in India. The northern part of India largely reported the ‘GH’ clade, whereas the southern part reported the ‘GR’, with a few exceptions. These sequences also revealed the presence of single independent mutations—E484Q and N440K—from Maharashtra (first observed in March 2020) and Southern Indian States (first observed in May 2020), respectively. Furthermore, this study indicates that the SARS-CoV-2 variant (VOC, VUI, variant of high consequence and double mutant) was not observed during the early phase of virus transmission (January–August). This increased number of variations observed within a short timeframe across the globe suggests virus evolution, which can be a step towards enhanced host adaptation. Full article
(This article belongs to the Special Issue Genomic Epidemiology of Viral Infections)
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Article
Validating Anti-Infective Activity of Pleurotus Opuntiae via Standardization of Its Bioactive Mycoconstituents through Multimodal Biochemical Approach
by Aprajita Tiwari Pandey, Ishan Pandey, Anurag Kanase, Amita Verma, Beatriz Garcia-Canibano, Sarada Prasad Dakua, Shidin Balakrishnan and Mohan Prasad Singh
Coatings 2021, 11(4), 484; https://doi.org/10.3390/coatings11040484 - 20 Apr 2021
Cited by 9 | Viewed by 4192
Abstract
Mushrooms produce a variety of bioactive compounds that are known to have anti-pathogenic properties with safer and effective therapeutic effects in human disease prognosis. The antibacterial activity of ethanol and methanol extracts of Pleurotus opuntiae were checked against pathogenic microorganisms viz. Pseudomonas aeruginosa [...] Read more.
Mushrooms produce a variety of bioactive compounds that are known to have anti-pathogenic properties with safer and effective therapeutic effects in human disease prognosis. The antibacterial activity of ethanol and methanol extracts of Pleurotus opuntiae were checked against pathogenic microorganisms viz. Pseudomonas aeruginosa ATCC 27853, Proteus mirabilis NCIM 2300, Proteus vulgaris NCIM 5266, Serratia marcescens NCIM 2078, Shigella flexeneri NCIM 5265, Moraxella sp. NCIM 2795, Staphylococcus aureus ATCC 25923 by agar well diffusion method at different concentrations of the extracts. Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of the extracts was determined by INT (Iodonitrotetrazolium chloride) colorimetric assay. Extracts were standardized by thin layer chromatography (TLC) in different solvent systems. The Retention factors (Rf) of different compounds were calculated by high performance TLC (HPTLC) fingerprinting at UV 254, 366, and 540 nm before and after derivatization. The ethanol and methanol extracts of P. opuntiae showed bactericidal activity against all the test pathogens at MIC values of 15.6 to 52.08 mg/mL and 20.81 to 52.08 mg/mL respectively. Whereas the MBC values for ethanol and methanol extract of P. opuntiae against all pathogens were recorded as 26.03 to 62.5 mg/mL and 125 mg/mL respectively. Preliminary mycochemical screening of both the extracts revealed high contents of bioactive compounds. Amongst all the solvent systems used in TLC, the best result was given by chloroform + hexane (8:2) which eluted out 5 different compounds (spots). HPTLC results revealed spots with different Rf values for all the 24 compounds present. Thus, it can be inferred from the present investigation that the mycoconstituents could be an alternative medication regimen and could play a role in new drug discoveries against different infections. Further, the antimicrobial components of these mushrooms can be transformed to bioengineered antimicrobial coatings for surfaces, drug and other hybrid systems for public health implications in combating persistent infections. Full article
(This article belongs to the Special Issue Antiviral Coating as Sustainable Measure to Fight Viral Pandemic)
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