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  1. Fulltext Assessment of practical science communication skills as a core competency of admission to undergraduate medical programmes: nationwide outcomes and associated factors
    Nicholas Pang, Jiann Lin Loo, Yusuf Ibrahim, Pasupuleti Visweswara Rao, Fairrul Kadir, Mohd Saffree Jeffree
    Malaysian Journal of Medicine and Health Sciences, 2019;15(106):14-14.
    MyJurnal
    Introduction: Interprofessional scientific communication skills are an essential part of the medical profession. Mul-tiple research suggests poor interprofessional communication has direct correlations with poor patient outcomes. As part of the inaugural Multiple Mini Interview (MMI) at Universiti Malaysia Sabah, a 5-minute station on science com-munication was introduced, assessed on three domains – logical thinking, communication skills, and general impres-sion. This station featured a panicky nurse calling a doctor to get them to calculate doses of a medication, using only upper primary school-level arithmetic and knowledge of ratios. Methods: 255 candidates, grouped into 3 separate geographical groups – Klang Valley, non-Klang Valley, and Borneo – participated in the MMI featuring a science communication station. Candidates were graded in the abovementioned three domains, and correlations were cal-culated between scores and various sociodemographic factors, with an objective written basic science test, and with overall scores. Also, quantitative analysis was done of the “red flag” comments for candidates deemed unsuitable for the practise of medicine. Results: The average scores for West Malaysia for logical thinking scores were higher than Borneo, with non-Klang Valley scores (4.1) significantly higher than Klang Valley (3.6). Communication scores were also significantly lower in Borneo compared to West Malaysia. General impression scores hence also showed a dis-crepancy between West Malaysian and Bornean scores. There were a total of 8 red flags, with reasons ranging from gross miscalculation with misplaced confidence, to nervous breakdowns while performing calculations. Conclusion: The present study showed that there is a distinct separation of science communication scores between geographic re-gions. Also it illustrates the yawning gap between academic knowledge and “translational” scientific knowledge. The results illustrate the need for medical curricula to boost resilience and translational computational skills in medical graduates who will be working in environments that demand usual abilities under unusual and trying circumstances.
  2. Balanced diets in food systems: Emerging trends and challenges for human health
    Sammugam L, Pasupuleti VR
    Crit Rev Food Sci Nutr, 2019;59(17):2746-2759.
    PMID: 29693412 DOI: 10.1080/10408398.2018.1468729
    Processed foods, generally known as modified raw foods produced by innovative processing technologies alters the food constituents such natural enzymes, fatty acids, micronutrients, macronutrients and vitamins. In contrast to fresh and unprocessed foods, processed foods are guaranteed to be safer, imperishable, long lasting and consist high level of nutrients bioactivity. Currently, the evolution in food processing technologies is necessary to face food security and safety, nutrition demand, its availability and also other global challenges in the food system. In this scenario, this review consists of information on two food processing technologies, which effects on processed foods before and after processing and the impact of food products on human health. It is also very well established that understanding the type and structure of foods to be processed can assist food processing industries towards advancement of novel food products. In connection with this fact, the present article also discusses the emerging trends and possible modifications in food processing technologies with the combination of conventional and modern techniques to get the suitable nutritional and safety qualities in food.
  3. A Mini Review on Emerging Targets and Approaches for the Synthesis of Anti-viral Compounds: In Perspective to COVID-19
    Gokada MR, Pasupuleti VR, Bollikolla HB
    Mini Rev Med Chem, 2021;21(10):1173-1181.
    PMID: 33397236 DOI: 10.2174/1389557521666210104165733
    The novel Coronavirus disease (COVID-19) is an epidemic disease that appeared at the end of the year 2019 with a sudden increase in number and came to be considered as a pandemic disease caused by a viral infection which has threatened most countries for an emergency search for new anti-SARS-COV drugs /vaccines. At present, the number of clinical trials is ongoing worldwide on different drugs i.e. Hydroxychloroquine, Remedisvir, Favipiravir that utilize various mechanisms of action. A few countries are currently processing clinical trials, which may result in a positive outcome. Favipiravir (FPV) represents one of the feasible treatment options for COVID-19, if the result of the trials turns out positive. Favipiravir will be one of the developed possibly authoritative drugs to warrant benefits to mankind with large-scale production to meet the demands of the current pandemic Covid-19 outbreak and future epidemic outbreaks. In this review, the authors tried to explore key molecules, which will be supportive for devising COVID-19 research.
  4. Fulltext Surface Thermo-Dynamic Characterization of Poly (Vinylidene Chloride-Co-Acrylonitrile) (P(VDC-co-AN)) Using Inverse-Gas Chromatography and Investigation of Visual Traits Using Computer Vision Image Processing Algorithms
    Kakani V, Kim H, Basivi PK, Pasupuleti VR
    Polymers (Basel), 2020 Jul 23;12(8).
    PMID: 32717780 DOI: 10.3390/polym12081631
    The Inverse Gas Chromatography (IGC) technique has been employed for the surface thermo-dynamic characterization of the polymer Poly(vinylidene chloride-co-acrylonitrile) (P(VDC-co-AN)) in its pure form. IGC attributes, such as London dispersive surface energy, Gibbs free energy, and Guttman Lewis acid-base parameters were analyzed for the polymer (P(VDC-co-AN)). The London dispersive surface free energy ( γ S L ) was calculated using the Schultz and Dorris-Gray method. The maximum surface energy value of (P(VDC-co-AN )) is found to be 29.93 mJ·m - 2 and 24.15 mJ·m - 2 in both methods respectively. In our analysis, it is observed that the γ S L values decline linearly with an increase in temperature. The Guttman-Lewis acid-base parameter K a , K b values were estimated to be 0.13 and 0.49. Additionally, the surface character S value and the correlation coefficient were estimated to be 3.77 and 0.98 respectively. After the thermo-dynamic surface characterization, the (P(VDC-co-AN)) polymer overall surface character is found to be basic. The substantial results revealed that the (P(VDC-co-AN)) polymer surface contains more basic sites than acidic sites and, hence, can closely associate in acidic media. Additionally, visual traits of the polymer (P(VDC-co-AN)) were investigated by employing Computer Vision and Image Processing (CVIP) techniques on Scanning Electron Microscopy (SEM) images captured at resolutions ×50, ×200 and ×500. Several visual traits, such as intricate patterns, surface morphology, texture/roughness, particle area distribution ( D A ), directionality ( D P ), mean average particle area ( μ a v g ) and mean average particle standard deviation ( σ a v g ), were investigated on the polymer's purest form. This collective study facilitates the researches to explore the pure form of the polymer Poly(vinylidene chloride-co-acrylonitrile) (P(VDC-co-AN )) in both chemical and visual perspective.
  5. Fulltext Honey, Propolis, and Royal Jelly: A Comprehensive Review of Their Biological Actions and Health Benefits
    Pasupuleti VR, Sammugam L, Ramesh N, Gan SH
    Oxid Med Cell Longev, 2017;2017:1259510.
    PMID: 28814983 DOI: 10.1155/2017/1259510
    BACKGROUND: There are several health benefits that honeybee products such as honey, propolis, and royal jelly claim toward various types of diseases in addition to being food.

    SCOPE AND APPROACH: In this paper, the effects of honey, propolis, and royal jelly on different metabolic diseases, cancers, and other diseases have been reviewed. The modes of actions of these products have also been illustrated for purposes of better understanding.

    KEY FINDINGS AND CONCLUSIONS: An overview of honey, propolis, and royal jelly and their biological potentials was highlighted. The potential health benefits of honey, such as microbial inhibition, wound healing, and its effects on other diseases, are described. Propolis has been reported to have various health benefits related to gastrointestinal disorders, allergies, and gynecological, oral, and dermatological problems. Royal jelly is well known for its protective effects on reproductive health, neurodegenerative disorders, wound healing, and aging. Nevertheless, the exact mechanisms of action of honey, propolis, and royal jelly on the abovementioned diseases and activities have not been not fully elucidated, and further research is warranted to explain their exact contributions.

  6. Hunig's base catalyzed synthesis of new 1-(2,3-dihydro-1H-inden-1-yl)-3-aryl urea/thiourea derivatives as potent antioxidants and 2HCK enzyme growth inhibitors
    Lachhi Reddy V, Avula VKR, Zyryanov GV, Vallela S, Anireddy JS, Pasupuleti VR, et al.
    Bioorg Chem, 2020 01;95:103558.
    PMID: 31911311 DOI: 10.1016/j.bioorg.2019.103558
    A series of 1-(2,3-dihydro-1H-indan-1-yl)-3-aryl urea/thiourea derivatives (4a-j) have been synthesized from the reaction of 2,3-dihydro-1H-inden-1-amine (2) with various aryl isocyanates/isothiocyanates (3a-j) by using N,N-DIPEA base (Hunig's base) catalyst in THF at reflux conditions. All of them are structurally confirmed by spectral (IR, 1H &13C NMR and MASS) and elemental analysis and screened for their in-vitro antioxidant activity against DPPH and NO free radicals and found that compounds 4b, 4i, 4h &4g are potential antioxidants. The obtained in vitro results were compared with the molecular docking, ADMET, QSAR and bioactivity study results performed for them and identified that the recorded in silico binding affinities were observed in good correlation with the in vitro antioxidant results. The Molecular docking analysis had unveiled the strong hydrogen bonding interactions of synthesized ligands with ARG 160 residue of protein tyrosine kinase (2HCK) enzyme and plays an effective role in its inhibition. Toxicology studies have assessed the potential risks of 4a-j and inferred that all of them were in the limits of potential drugs. The conformational analysis of 4a-j inferred that the urea/thiourea spacer linking 2,3-dihydro-1H-inden-1-amino and substituted aryl units has facilitated all these molecules to effectively bind with ARG 160 amino acid residue present on the α-helix of the protein tyrosine kinase (2HCK) enzyme specifically on chain A of hemopoetic cell kinase. Collectively this study has established a relationship between the antioxidant potentiality and ligands binding with ARG 160 amino acid residue of chain A of 2HCK enzyme to inhibit its growth as well as proliferation of reactive oxygen species in vivo.
  7. Synthesis, antioxidant activity and bioinformatics studies of L-3-hydroxytyrosine templated N-alkyl/aryl substituted urea/thioureas
    Kollu U, Avula VKR, Vallela S, Pasupuleti VR, Zyryanov GV, Neelam YS, et al.
    Bioorg Chem, 2021 06;111:104837.
    PMID: 33812281 DOI: 10.1016/j.bioorg.2021.104837
    A new series of urea/thiourea derivatives have been efficiently synthesized from the reaction of L-3-hydroxytyrosine with selective isocyanates/isothiocyanates and characterized by Infra-red, proton & carbon-13 nuclear magnetic resonance spectral and mass spectrometry studies. All the synthesized compounds have been screened for their antioxidant activity by 1,1-diphenyl1-2-picrylhydrazyl radical assay, ferric reducing antioxidant power assay and also studied their molecular docking interaction profiles against 1N8Q and 3NRZ enzymatic proteins. The in vitro antioxidant activity has further supported by quantitative structure activity relationship, absorption, distribution, metabolism, and excretion & toxicity studies, bioactivity studies & enzyme inhibition assay and identified that they were potentially bound to ASP490 & ASP361 aminoacid residue in chain A of 1N8Q protein and GLN1194 aminoacid residue in chain L of 3NRZ protein and are responsible for potential antioxidant activity. It is proved that urea derivatives linked with 4-fluoro & 4-nitro and thiourea derivatives linked with 3-chloro & 4-fluoro have exhibited promising antioxidant activity. In eventual synthesized compounds have been identified as potential blood-brain barrier penetrable compounds and proficient central nervous system active neuro-protective antioxidant agents as they have envisaged as easily penetrable to blood-brain barrier thresholds, a neuroprotective property.
  8. Gallocatechin‑silver nanoparticle impregnated cotton gauze patches enhance wound healing in diabetic rats by suppressing oxidative stress and inflammation via modulating the Nrf2/HO-1 and TLR4/NF-κB pathways
    Vendidandala NR, Yin TP, Nelli G, Pasupuleti VR, Nyamathulla S, Mokhtar SI
    Life Sci, 2021 Dec 01;286:120019.
    PMID: 34624322 DOI: 10.1016/j.lfs.2021.120019
    This study is designed to investigate the combination of gallocatechin (GC) and silver nanoparticles (AgNPs) for its wound healing ability in diabetic rats. Thirty male Sprague Dawley rats were randomly divided into 5 groups: 1. Normal control rats dressed with blank CGP1; 2. Diabetic rats dressed with blank CGP1; 3. Diabetic rats dressed with 13.06μM of GC; 4. Diabetic rats dressed with 26.12 μM of GC; 5. Diabetic rats dressed with 0.1% silver sulfadiazine patches. GC-AgNPs-CGP dressed diabetic rats showed significant FBG reduction, prevented the body weight losses and reduced the oxidative stress by lowering MDA content and elevated antioxidant enzymes such as SOD, CAT and GPx in wound healing skin of diabetic rats when compared to normal CGP. Besides, mRNA expression of Nrf2, Nqo-1, and Ho-1 was upregulated with downregulated expression of Keap-1 mRNA, which is supported by immunohistochemistry. Furthermore, GC-AgNPs-CGP dressing increased growth factors such as VEGF, EGF, TGF-β, and FGF-2 while decreasing MMP-2 in the skin of diabetic wound rats. In vitro permeation study demonstrated rapid GC release and permeation with a flux of 0.061 and 0.143 mg/sq.cm/h. In conclusion, the results indicated that GC-AgNPs-CGP dressing on diabetic wound rats modulated oxidative stress and inflammation with elevated growth factors; increased collagen synthesis thereby significantly improved the wound healing and could be beneficial for the management of diabetic wounds.
  9. Fulltext Multifaceted phytogenic silver nanoparticles by an insectivorous plant Drosera spatulata Labill var. bakoensis and its potential therapeutic applications
    Gaddam SA, Kotakadi VS, Subramanyam GK, Penchalaneni J, Challagundla VN, Dvr SG, et al.
    Sci Rep, 2021 11 09;11(1):21969.
    PMID: 34753977 DOI: 10.1038/s41598-021-01281-8
    The current investigation highlights the green synthesis of silver nanoparticles (AgNPs) by the insectivorous plant Drosera spatulata Labill var. bakoensis, which is the first of its kind. The biosynthesized nanoparticles revealed a UV visible surface plasmon resonance (SPR) band at 427 nm. The natural phytoconstituents which reduce the monovalent silver were identified by FTIR. The particle size of the Ds-AgNPs was detected by the Nanoparticle size analyzer confirms that the average size of nanoparticles was around 23 ± 2 nm. Ds-AgNPs exhibit high stability because of its high negative zeta potential (- 34.1 mV). AFM studies also revealed that the Ds-AgNPs were spherical in shape and average size ranges from 10 to 20 ± 5 nm. TEM analysis also revealed that the average size of Ds-AgNPs was also around 21 ± 4 nm and the shape is roughly spherical and well dispersed. The crystal nature of Ds-AgNPs was detected as a face-centered cube by the XRD analysis. Furthermore, studies on antibacterial and antifungal activities manifested outstanding antimicrobial activities of Ds-AgNPs compared with standard antibiotic Amoxyclav. In addition, demonstration of superior free radical scavenging efficacy coupled with potential in vitro cytotoxic significance on Human colon cancer cell lines (HT-29) suggests that the Ds-AgNPs attain excellent multifunctional therapeutic applications.
  10. Fulltext Bitter Gourd Honey Ameliorates Hepatic and Renal Diabetic Complications on Type 2 Diabetes Rat Models by Antioxidant, Anti-Inflammatory, and Anti-Apoptotic Mechanisms
    Arigela CS, Nelli G, Gan SH, Sirajudeen KNS, Krishnan K, Abdul Rahman N, et al.
    Foods, 2021 Nov 20;10(11).
    PMID: 34829154 DOI: 10.3390/foods10112872
    Honey has several pharmacological effects, including anti-diabetic activity. However, the effectiveness of bitter gourd honey (BGH) in the treatment of diabetes mellitus (DM) is unknown. The aim of this study was to determine the antioxidant, anti-inflammatory, and anti-apoptotic properties of BGH on the kidney and liver of a streptozotocin-induced diabetes rat model.

    METHODS: A single dose (nicotinamide 110 mg/kg, streptozotocin (STZ) 55 mg/kg, intraperitoneal (i.p.)) was used to induce DM in male rats. For 28 days, normal or diabetic rats were administered 1 g/kg/day and 2 g/kg/day of BGH orally. After the treatment, blood, liver, and kidney samples were collected and analysed for biochemical, histological, and molecular parameters. In addition, liquid chromatography-mass spectrometry (LC-MS) was used to identify the major bioactive components in BGH.

    RESULTS: The administration of BGH to diabetic rats resulted in significant reductions in alanine transaminase (ALT),aspartate aminotransferase (AST), creatinine, and urea levels. Diabetic rats treated with BGH showed lesser pathophysiological alterations in the liver and kidney as compared to non-treated control rats. BGH-treated diabetic rats exhibited reduced levels of oxidative stress (MDA levels), inflammatory (MYD88, NFKB, p-NFKB, IKKβ), and apoptotic (caspase-3) markers, as well as higher levels of antioxidant enzymes (SOD, CAT, and GPx) in the liver and kidney. BGH contains many bioactive compounds that may have antioxidative stress, anti-inflammatory, and anti-apoptotic effects.

    CONCLUSION: BGH protected the liver and kidney in diabetic rats by reducing oxidative stress, inflammation, and apoptosis-induced damage. As a result, BGH can be used as a potential therapy to ameliorate diabetic complications.

  11. Fulltext Medicinal plants in management of type 2 diabetes and neurodegenerative disorders
    Siew Hua G, Kamal MA, Lima MM, Khalil MI, Pasupuleti VR, Aliev G
    Evid Based Complement Alternat Med, 2015;2015:686872.
    PMID: 25873981 DOI: 10.1155/2015/686872
  12. Multiple molecular targets mediated antioxidant activity, molecular docking, ADMET, QSAR and bioactivity studies of halo substituted urea derivatives of α-Methyl-l-DOPA
    Vadabingi N, Avula VKR, Zyryanov GV, Vallela S, Anireddy JS, Pasupuleti VR, et al.
    Bioorg Chem, 2020 04;97:103708.
    PMID: 32146177 DOI: 10.1016/j.bioorg.2020.103708
    A series of novel α-methyl-l-DOPA urea derivatives viz., 3-(3,4-dihydroxyphenyl)-2-methyl-2-(3-halo/trifluoromethyl substituted phenyl ureido)propanoic acids (6a-e) have been synthesized from the reaction of α-methyl-l-DOPA (3) with various aryl isocyanates (4a-e) by using triethylamine (5, TEA) as a base catalyst in THF at reflux conditions. The synthesized compounds are structurally characterized by spectral (IR, 1H &13C NMR and MASS) and elemental analysis studies and screened for their in-vitro antioxidant activity against DPPH, NO and H2O2 free radical scavenging assays and identified compounds 6c &6d as potential antioxidants. The acquired in vitro results were correlated with the results of molecular docking, ADMET, QSAR and bioactivity studies performed for them and predicted that the recorded in silico binding affinities are in good correlation with the in vitro antioxidant activity results. The molecular docking analysis has comprehended the strong hydrogen bonding interactions of 6a-e with 1CB4, 1N8Q, 3MNG, 1OG5, 1DNU, 3NRZ, 2CDU, 1HD2 and 2HCK proteins of their respective SOD, LO, PRXS5, CP450, MP, XO, NO, PRY5 and HCK enzymes. This has sustained the effective binding of 6a-e and resulted in functional inhibition of selective aminoacid residues to be pronounced as multiple molecular targets mediated antioxidant potent compounds. In addition, the evaluated toxicology risks of 6a-e are identified with in the potential limits of drug candidates. The conformational analysis of 6c & 6d prominently infers that urea moiety uniting α-methyl-l-DOPA with halo substituted aryl units into a distinctive orientation to comply good structure-activity to inhibit the proliferation of reactive oxygen species in vivo.
  13. Fulltext A Review on Oxidative Stress, Diabetic Complications, and the Roles of Honey Polyphenols
    Pasupuleti VR, Arigela CS, Gan SH, Salam SKN, Krishnan KT, Rahman NA, et al.
    Oxid Med Cell Longev, 2020;2020:8878172.
    PMID: 33299532 DOI: 10.1155/2020/8878172
    Despite the availability of various antidiabetic drugs, diabetes mellitus (DM) remains one of the world's most prevalent chronic diseases and is a global burden. Hyperglycaemia, a characteristic of type 2 diabetes mellitus (T2DM), substantially leads to the generation of reactive oxygen species (ROS), triggering oxidative stress as well as numerous cellular and molecular modifications such as mitochondrial dysfunction affecting normal physiological functions in the body. In mitochondrial-mediated processes, oxidative pathways play an important role, although the responsible molecular mechanisms remain unclear. The impaired mitochondrial function is evidenced by insulin insensitivity in various cell types. In addition, the roles of master antioxidant pathway nuclear factor erythroid 2-related factor 2 (Nrf2)/Kelch-like ECH-associated protein 1 (Keap1)/antioxidant response elements (ARE) are being deciphered to explain various molecular pathways involved in diabetes. Dietary factors are known to influence diabetes, and many natural dietary factors have been studied to improve diabetes. Honey is primarily rich in carbohydrates and is also abundant in flavonoids and phenolic acids; thus, it is a promising therapeutic antioxidant for various disorders. Various research has indicated that honey has strong wound-healing properties and has antibacterial, anti-inflammatory, antifungal, and antiviral effects; thus, it is a promising antidiabetic agent. The potential antidiabetic mechanisms of honey were proposed based on its major constituents. This review focuses on the various prospects of using honey as an antidiabetic agent and the potential insights.
  14. Fulltext Ultrasonication-mediated nitrogen-doped multiwalled carbon nanotubes involving carboxy methylcellulose composite for solid-state supercapacitor applications
    Basivi PK, Ramesh S, Kakani V, Yadav HM, Bathula C, Afsar N, et al.
    Sci Rep, 2021 May 10;11(1):9918.
    PMID: 33972653 DOI: 10.1038/s41598-021-89430-x
    In this study, a novel nanohybrid composite containing nitrogen-doped multiwalled carbon nanotubes/carboxymethylcellulose (N-MWCNT/CMC) was synthesized for supercapacitor applications. The synthesized composite materials were subjected to an ultrasonication-mediated solvothermal hydrothermal reaction. The synthesized nanohybrid composite electrode material was characterized using analytical methods to confirm its structure and morphology. The electrochemical properties of the composite electrode were investigated using cyclic voltammetry (CV), galvanic charge-discharge, and electrochemical impedance spectroscopy (EIS) using a 3 M KOH electrolyte. The fabricated composite material exhibited unique electrochemical properties by delivering a maximum specific capacitance of approximately 274 F g-1 at a current density of 2 A g-1. The composite electrode displayed high cycling stability of 96% after 4000 cycles at 2 A g-1, indicating that it is favorable for supercapacitor applications.
  15. Fulltext Sonication-supported synthesis of cobalt oxide assembled on an N-MWCNT composite for electrochemical supercapacitors via three-electrode configuration
    Nare RK, Ramesh S, Basavi PK, Kakani V, Bathula C, Yadav HM, et al.
    Sci Rep, 2022 Feb 07;12(1):1998.
    PMID: 35132094 DOI: 10.1038/s41598-022-05964-8
    The Co3O4@N-MWCNT composite was synthesized by a sonication-supported thermal reduction process for supercapacitor applications. The structural and morphological properties of the materials were characterized via Raman, XRD, XPS, SEM-EDX, and FE-TEM analysis. The composite electrode was constructed into a three-electrode configuration and examined by using CV, GCD and EIS analysis. The demonstrated electrochemical value of ~ 225 F/g at 0.5 A/g by the electrode made it appropriate for potential use in supercapacitor applications.
  16. Fulltext Biogenic silver nanoparticles using Rhinacanthus nasutus leaf extract: synthesis, spectral analysis, and antimicrobial studies
    Pasupuleti VR, Prasad TN, Shiekh RA, Balam SK, Narasimhulu G, Reddy CS, et al.
    Int J Nanomedicine, 2013;8:3355-64.
    PMID: 24039419 DOI: 10.2147/IJN.S49000
    Nanotechnology is gaining momentum due to its ability to transform metals into nanoparticles. The synthesis, characterization, and applications of biologically synthesized nanomaterials have become an important branch of nanotechnology. Plant extracts are a cost-effective, ecologically friendly, and efficient alternative for the large-scale synthesis of nanoparticles. In this study, silver nanoparticles (AgNps) were synthesized using Rhinacanthus nasutus leaf extract. After exposing the silver ions to the leaf extract, the rapid reduction of silver ions led to the formation of AgNps in solution. The synthesis was confirmed by ultraviolet-visible spectroscopy, Fourier transform infrared spectroscopy, and transmission electron microscopy. The in vitro antimicrobial activity of the AgNps synthesized using R. nasutus leaf extract was investigated against Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumonia, Escherichia coli, Aspergillus niger, and Aspergillus flavus using a disc diffusion method. The AgNps showed potential activity against all of the bacterial strains and fungal colonies, indicating that R. nasutus has the potential to be used in the development of value-added products in the biomedical and nanotechnology-based industries.
  17. Fulltext Development of Protein Rich Pregelatinized Whole Grain Cereal Bar Enriched With Nontraditional Ingredient: Nutritional, Phytochemical, Textural, and Sensory Characterization
    Allai FM, Dar BN, Gul K, Adnan M, Ashraf SA, Hassan MI, et al.
    Front Nutr, 2022;9:870819.
    PMID: 35464008 DOI: 10.3389/fnut.2022.870819
    This study was aimed to use extrusion cooking as a pretreatment for non-conventional seeds (Indian horse chestnut flour) to blend them with whole grain flours (whole wheat flour, whole barley flour, and whole corn flour) for the development of a pregelatinized cereal bar (PCB). In this study, date paste (7.5-17.5%) and walnut grits (2.5-12.5%) were incorporated at varying levels to prepare PCB. The PCB was evaluated for its nutritional, color, textural (both three-point bending test and TPA), antioxidant activity, and sensory attributes. The flexural modulus, rupture stress, and fracture strain of PCB increased with the incorporation of a higher proportion of date paste. The protein and fiber content in PCB increased from 7.74 to 9.13% and 4.81 to 5.59% with the incorporation of walnut grits and date paste, respectively. The DPPH, total phenolic content, and water activity of PCB were determined, which progressively enhanced with increased levels of walnut grits and date paste. The correlation between sensory attributes and instrumental texture on PCB was also investigated. The correlation results showed a significant (p < 0.05) positive correlation between texture analysis and sensory hardness, springiness, adhesiveness, and negatively correlated to instrumental and sensory cohesiveness. For sensorial attributes, all PCB samples presented average scores of 7/10 and 4/5 for buying intention. Therefore, whole grain extrudates, date paste, and walnut grits can be efficiently used to develop PCB with improved nutritional, nutraceutical, and economic values.
  18. Fulltext Synthesis of novel cytotoxic tetracyclic acridone derivatives and study of their molecular docking, ADMET, QSAR, bioactivity and protein binding properties
    Veligeti R, Madhu RB, Anireddy J, Pasupuleti VR, Avula VKR, Ethiraj KS, et al.
    Sci Rep, 2020 11 26;10(1):20720.
    PMID: 33244007 DOI: 10.1038/s41598-020-77590-1
    Acridone based synthetic and natural products with inherent anticancer activity advancing the research and generating a large number of structurally diversified compounds. In this sequence we have designed, synthesized a series of tetracyclic acridones with amide framework viz., 3-(alkyloyl/ aryloyl/ heteroaryloyl/ heteroaryl)-2,3-dihydropyrazino[3,2,1-de]acridin-7(1H)-ones and screened for their in vitro anti-cancer activity. The in vitro study revealed that compounds with cyclopropyl-acetyl, benzoyl, p-hydroxybenzoyl, p-(trifluoromethyl)benzoyl, p-fluorobenzoyl, m-fluorobenzoyl, picolinoyl, 6-methylpicolinoyl and 3-nicotinoyl groups are active against HT29, MDAMB231 and HEK293T cancer cell lines. The molecular docking studies performed for them against 4N5Y, HT29 and 2VWD revealed the potential ligand-protein binding interactions among the neutral aminoacid of the enzymes and carbonyl groups of the title compounds with a binding energy ranging from - 8.1394 to - 6.9915 kcal/mol. In addition, the BSA protein binding assay performed for them has confirmed their interaction with target proteins through strong binding to BSA macromolecule. The additional studies like ADMET, QSAR, bioactivity scores, drug properties and toxicity risks ascertained them as newer drug candidates. This study had added a new collection of piperazino fused acridone derivatives to the existing array of other nitrogen heterocyclic fused acridone derivatives as anticancer agents.
  19. Green Synthesis, Antioxidant, and Plant Growth Regulatory Activities of Novel α-Furfuryl-2-alkylaminophosphonates
    Nadiveedhi MR, Nuthalapati P, Gundluru M, Yanamula MR, Kallimakula SV, Pasupuleti VR, et al.
    ACS Omega, 2021 Feb 02;6(4):2934-2948.
    PMID: 33553912 DOI: 10.1021/acsomega.0c05302
    A series of novel α-furfuryl-2-alkylaminophosphonates have been efficiently synthesized from the one-pot three-component classical Kabachnik-Fields reaction in a green chemical approach by addition of an in situ generated dialkylphosphite to Schiff's base of aldehydes and amines by using environmental and eco-friendly silica gel supported iodine as a catalyst by microwave irradiation. The advantage of this protocol is simplicity in experimental procedures and products were resulted in high isolated yields. The synthesized α-furfuryl-2-alkylaminophosphonates were screened to in vitro antioxidant and plant growth regulatory activities and some are found to be potent with antioxidant and plant growth regulatory activities. These in vitro studies have been further supported by ADMET (absorption, distribution, metabolism, excretion, and toxicity), quantitative structure-activity relationship, molecular docking, and bioactivity studies and identified that they were potentially bound to the GLN340 amino acid residue in chain C of 1DNU protein and TYR597 amino acid residue in chain A of 4M7E protein, causing potential exhibition of antioxidant and plant growth regulatory activities. Eventually, title compounds are identified as good blood-brain barrier (BBB)-penetrable compounds and are considered as proficient central nervous system active and neuroprotective antioxidant agents as the neuroprotective property is determined with BBB penetration thresholds.
  20. Fulltext Synthesis and Anti-Pancreatic Cancer Activity Studies of Novel 3-Amino-2-hydroxybenzofused 2-Phospha-γ-lactones
    Balam SK, Soora Harinath J, Krishnammagari SK, Gajjala RR, Polireddy K, Baki VB, et al.
    ACS Omega, 2021 May 04;6(17):11375-11388.
    PMID: 34056293 DOI: 10.1021/acsomega.1c00360
    A series of 3-amino-2-hydroxybenzofused 2-phosphalactones (4a-l) has been synthesized from the Kabachnik-Fields reaction via a facile route from a one-pot three-component reaction of diphenylphosphite with various 2-hydroxybenzaldehyes and heterocyclic amines in a new way of expansion. The in vitro anti-cell proliferation studies by MTT assay have revealed them as potential Panc-1, Miapaca-2, and BxPC-3 pancreatic cell growth inhibitors, and the same is supported by molecular docking, QSAR, and ADMET studies. The MTT assay of their SAHA derivatives against the same cell lines evidenced them as potential HDAC inhibitors and identified 4a, 4b, and 4k substituted with 1,3-thiazol, 1,3,4-thiadiazol, and 5-sulfanyl-1,3,4-thiadiazol moieties on phenyl and diethylamino phenyl rings as potential ones. Additionally, the flow cytometric analyses of 4a, 4b, and 4k against BxPC-3 cells revealed compound 4k as a lead compound that arrests the S phase cell cycle growth at low micromolar concentrations. The ADMET properties have ascertained their inherent pharmacokinetic potentiality, and the wholesome results prompted us to report it as the first study on anti-pancreatic cancer activity of cyclic α-aminophosphonates. Ultimately, this study serves as a good contribution to update the existing knowledge on the anticancer organophosphorus heterocyclic compounds and elevates the scope for generation of new anticancer drugs. Further, the studies like QSAR, drug properties, toxicity risks, and bioactivity scores predicted for them have ascertained the synthesized compounds as newer and potential drug candidates. Hence, this study had augmented the array of α-aminophosphonates by adding a new collection of 3-amino-2-hydroxybenzofused 2-phosphalactones, a class of cyclic α-aminophosphonates, to it, which proved them as potential anti-pancreatic cancer agents.
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