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  1. Article: Effects of dapagliflozin against streptozotocin and isoproterenol-induced heart failure via investigating NLRP3 and PPAR-γ signaling.

    Ijaz, Khadija / Khan, Arif-Ullah / Kamal, Yousaf / Irshad, Nadeem

    Pakistan journal of pharmaceutical sciences

    2024  Volume 37, Issue 2, Page(s) 337–347

    Abstract: Heart failure is a condition in which the heart's one or both ventricles are unable to either receive an adequate amount of blood or eject an adequate amount of blood. Diabetes is considered one of the major risk factors for cardiovascular diseases. The ... ...

    Abstract Heart failure is a condition in which the heart's one or both ventricles are unable to either receive an adequate amount of blood or eject an adequate amount of blood. Diabetes is considered one of the major risk factors for cardiovascular diseases. The current research is designed to evaluate the cardioprotective effects of dapagliflozin in streptozotocin and isoproterenol-induced comorbid rats. The COX-2, TNF-α, NF-КB, NLRP3, PPAR-γ, CKMB, TROP-I, AR, GP and SGLT were docked against dapagliflozin, propranolol and metformin. Dapagliflozin restored adequate blood flow and halted myofibril damage. Moreover, it's evident from this study that dapagliflozin significantly decreased serum concentration of various blood markers, decreased relative growth rate and QT interval prolongation, as compared to the negative control group. However, it improved the ventricular ejection fraction in rats of the treatment group. The GST, GSH and CAT levels were increased, as compared to normal. On the contrary, a decrease in LPO concentrations was observed. Evaluation of the coronal section of heart tissues showed the anti-inflammatory expressions evaluated through H & E staining and immunohistochemical techniques and with ELISA and PCR. In a nutshell, dapagliflozin reverses myocardial necrosis and apoptosis.
    MeSH term(s) Animals ; Glucosides/pharmacology ; Isoproterenol/toxicity ; Heart Failure/chemically induced ; Heart Failure/drug therapy ; Heart Failure/metabolism ; Benzhydryl Compounds/pharmacology ; NLR Family, Pyrin Domain-Containing 3 Protein/metabolism ; PPAR gamma/metabolism ; Rats ; Streptozocin ; Signal Transduction/drug effects ; Male ; Rats, Wistar ; Diabetes Mellitus, Experimental/drug therapy ; Cardiotonic Agents/pharmacology ; Apoptosis/drug effects ; Sodium-Glucose Transporter 2 Inhibitors/pharmacology ; Myocardium/metabolism ; Myocardium/pathology
    Chemical Substances dapagliflozin ; Nlrp3 protein, rat
    Language English
    Publishing date 2024-05-20
    Publishing country Pakistan
    Document type Journal Article
    ZDB-ID 885131-1
    ISSN 1011-601X
    ISSN 1011-601X
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Blood pressure lowering effect of selected pyrimidine derivatives mediated through inhibition of calcium channel: A computational approach.

    Irshad, Nadeem / Khan, Arif-Ullah / Kamal, Yousaf / Iqbal, Muhammad Nasir

    Pakistan journal of pharmaceutical sciences

    2023  Volume 35, Issue 6, Page(s) 1513–1522

    Abstract: Pyrimidine 2, 4, 6-trione derivatives are known to have L-type calcium channel blockade activity due to which they are quite effective in cardiovascular diseases along with cancer, epilepsy and inflammatory disorders. The chemoinformatics prediction for ... ...

    Abstract Pyrimidine 2, 4, 6-trione derivatives are known to have L-type calcium channel blockade activity due to which they are quite effective in cardiovascular diseases along with cancer, epilepsy and inflammatory disorders. The chemoinformatics prediction for test compounds: 5-(3-Hydroxybenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-5), 5-(4-Hydroxybenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-8), 5-(3-Chlorobenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-9) and 5-(4-Chlorobenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-10) was investigated. The drug likeliness and pharmacokinetic properties (PKs) of test compounds calculated using Molinspiration & Swiss ADME online servers. These test drugs subjected to molecular docking analysis and molecular dynamic (MD) simulation to calculate their binding energies with hypertensive and platelet aggregatory proteinaceous targets and their stability against calcium channel. The druggability and PKs of selected compounds exhibited that these compounds could be represented as potential candidates for further development into antihypertensive-like agents. The docking results indicated that binding energies ranged between -5 and -8.8 kcal/mol. Compounds showed good binding energies against calcium channels (CC) and subjected to molecular dynamic simulation to assess the stability of protein-ligand complex. The results showed that all the ligands form stable complexes with the CC, though SR-9 and SR-10 had enhanced stability when compared to SR-5 and SR-8.
    MeSH term(s) Calcium Channels ; Antihypertensive Agents/pharmacology ; Molecular Docking Simulation ; Blood Pressure ; Pyrimidines/pharmacology
    Chemical Substances Calcium Channels ; Antihypertensive Agents ; Pyrimidines
    Language English
    Publishing date 2023-02-15
    Publishing country Pakistan
    Document type Journal Article
    ZDB-ID 885131-1
    ISSN 1011-601X
    ISSN 1011-601X
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Assessment of cytotoxic potential of newly isolated Betulinic triterpenes from the Bark of Bauhinia variegata Linn. (Caesalpiniaceae)

    Kamal, Yousaf / Khan, Taous / Fatima, Nighat / Shahzadi, Irum / ul-Haq, Ihsan / Anaya-Eugenio, Gerardo D. / Arellano, Eric Daniel Salinas / Bashir, Kashif / Carcache de Blanco, Esperanza J.

    South African Journal of Botany. 2023 Aug., v. 159 p.419-424

    2023  

    Abstract: The present study focuses on the evaluation of the cytotoxic potential of isolated compounds from the bark of Bauhinia variegata L. (Caesalpiniaceae). Different chromatographic procedures led to the isolation of four compounds (1-4), with betulin type ... ...

    Abstract The present study focuses on the evaluation of the cytotoxic potential of isolated compounds from the bark of Bauhinia variegata L. (Caesalpiniaceae). Different chromatographic procedures led to the isolation of four compounds (1-4), with betulin type triterpene 1 (BVBH1) being reported as new compound along with three known compounds, 3-α-hydroxy-urs-12, 15-diene 2 (BVBH2), cholesta-5-en-3,7-diol amine 3 (BVBH3), N, N’, N''- (cyclopropane-1,2,3-triylidene) trihexanamide 4 (BVBH4) from n-hexane extract of B. variegata bark. The structure elucidation of isolated compounds was carried out using ¹H NMR, ¹³C NMR, 2D NMR and mass spectrometric data. Compound 3 displayed cytotoxic activity against DU-145, PC-3, MCF-7, and HT-29 human cancer cell lines, while compound 4 showed cytotoxic activity against HT-29 and MCF-7 human cancer cell lines, whereas compound 1 and compound 2 did not exhibit any cytotoxic effect against four tested cell lines. The current study suggested that isolated compounds from B. variegata bark have cytotoxic potential and may further be used for the detailed anticancer investigations.
    Keywords Bauhinia variegata ; bark ; betulin ; chromatography ; cytotoxicity ; hexane ; humans ; mass spectrometry ; neoplasm cells ; Bauhinia variegata bark ; SRB cytotoxicity assay ; 1H, 13C NMR and 2D NMR ; Mass spectrometry, chromatographic procedures ; Nuclear magnetic resonance
    Language English
    Dates of publication 2023-08
    Size p. 419-424.
    Publishing place Elsevier B.V.
    Document type Article ; Online
    ZDB-ID 2126918-X
    ISSN 0254-6299
    ISSN 0254-6299
    DOI 10.1016/j.sajb.2023.05.026
    Database NAL-Catalogue (AGRICOLA)

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  4. Article: In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid

    Rashid, Aisha / Irfan, Muhammad / Kamal, Yousaf / Asghar, Sajid / Khalid, Syed Haroon / Hussain, Ghulam / Alshammari, Abdulrahman / Albekairi, Thamer H / Alharbi, Metab / Khan, Hafeez Ullah / Chauhdary, Zunera / Vandamme, Thierry F / Khan, Ikram Ullah

    Pharmaceutics

    2024  Volume 16, Issue 2

    Abstract: Flurbiprofen (FBP), a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to treat the pain of rheumatoid arthritis, but in prolonged use it causes gastric irritation and ulcer. To avoid these adverse events of NSAIDs, the simultaneous ... ...

    Abstract Flurbiprofen (FBP), a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to treat the pain of rheumatoid arthritis, but in prolonged use it causes gastric irritation and ulcer. To avoid these adverse events of NSAIDs, the simultaneous administration of H
    Language English
    Publishing date 2024-01-24
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics16020164
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Obesity and tooth wear among American adults: the role of sugar-sweetened acidic drinks.

    Kamal, Yousaf / O'Toole, Saoirse / Bernabé, Eduardo

    Clinical oral investigations

    2019  Volume 24, Issue 4, Page(s) 1379–1385

    Abstract: Background: To explore the association between obesity and tooth wear among American adults and the role of sugar-sweetened acidic drinks consumption in explaining that association.: Methods: We analyzed data from 3541 adult participants in the ... ...

    Abstract Background: To explore the association between obesity and tooth wear among American adults and the role of sugar-sweetened acidic drinks consumption in explaining that association.
    Methods: We analyzed data from 3541 adult participants in the National Health and Nutrition Examination Survey. Obesity was determined using the body mass index and tooth wear was assessed using the modified tooth wear index. Daily intake of four categories of drinks was estimated as the average (drinks/day) of two consecutive 24-h dietary recalls. The association between obesity and number of surfaces with moderate-to-severe tooth wear was assessed in hurdle models adjusting for sociodemographic factors, acid reflux medication, and dental insurance.
    Results: Overweight and obese adults had more surfaces with moderate-to-severe tooth wear than those with normal body size, after adjusting for confounders. The consumption of sugar-sweetened acidic drinks explained part, but not all the above association. More specifically, the estimate for obesity was fully attenuated, whereas the estimate for overweight was slightly attenuated but remained significant.
    Conclusion: Obesity was positively associated with tooth wear in American adults. This association was only partially accounted for by the consumption of sugar-sweetened acidic drinks, a common risk factor for both conditions.
    Practical implications: Dentists must be aware of the health consequences of sugar-sweetened acidic drinks and advocate for reduction in consumption and/or substitution with healthier alternatives.
    MeSH term(s) Acids ; Adolescent ; Adult ; Aged ; Dietary Sucrose ; Female ; Humans ; Male ; Middle Aged ; Nutrition Surveys ; Obesity/epidemiology ; Sugar-Sweetened Beverages/adverse effects ; Tooth Wear/epidemiology ; United States ; Young Adult
    Chemical Substances Acids ; Dietary Sucrose
    Language English
    Publishing date 2019-10-27
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 1364490-7
    ISSN 1436-3771 ; 1432-6981
    ISSN (online) 1436-3771
    ISSN 1432-6981
    DOI 10.1007/s00784-019-03079-5
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Ameliorative Effect of Structurally Divergent Oleanane Triterpenoid, 3-Epifriedelinol from

    Majid, Muhammad / Farhan, Anam / Baig, Muhammad Waleed / Khan, Muhammad Tariq / Kamal, Yousaf / Hassan, Syed Shams Ul / Bungau, Simona / Haq, Ihsan-Ul

    Molecules (Basel, Switzerland)

    2022  Volume 28, Issue 1

    Abstract: The pentacyclic triterpenoids (PTs) of plant origin are reputed to restrain prostate cancer (PCa) cell proliferation. This study aims to assess 3-epifriedelinol (EFD) isolated from aerial part of Ipomoea batatas against PCa and its potential mechanism, ... ...

    Abstract The pentacyclic triterpenoids (PTs) of plant origin are reputed to restrain prostate cancer (PCa) cell proliferation. This study aims to assess 3-epifriedelinol (EFD) isolated from aerial part of Ipomoea batatas against PCa and its potential mechanism, in vitro and in vivo. Molecular docking affirms good binding affinity of the compound with target proteins exhibiting binding energy of −7.9 Kcal/mol with BAX, −8.1 Kcal/mol (BCL-2), −1.9 Kcal/mol (NF-κB) and −8.5 Kcal/mol with P53. In the MTT assay, EFD treatment (3−50 µM) showed a significant (p < 0.05 and p < 0.01) dose and time dependent drop in the proliferative graph of DU145 and PC3, and an upsurge in apoptotic cell population. EFD displayed substantial IC50 against DU145 (32.32 ± 3.72 µM) and PC3 (35.22 ± 3.47 µM). According to Western blots, EFD administration significantly enhanced the cleavage of caspases and PARP, elevated BAX and P53 and decreased BCL-2 and NF-κB expression, thereby triggering apoptosis in PCa cells. When male Sprague Dawley rats were intoxicated with Bisphenol A (BPA), an apparent increase in prostate mass (0.478 ± 0.08 g) in comparison to control (0.385 ± 0.03 g) indicates prostatitis. Multidose treatment of EFD (10 mg/kg) significantly reduced prostate size (0.404 ± 0.05 g). EFD exhibited substantial curative potential in vivo, as hematological, hormonal and histopathological parameters have been significantly improved. Reduced peroxidation (TBARS), and suppression of inflammatory markers i.e., NO, IL-6 and TNF-α, signposts substantial antiinflammatory potential of the compound. Overall, EFD has shown better binding affinity with target molecules, acceptable ADMET profile, potent antiproliferative and apoptotic nature and significant reduction in inflamed prostate mass of rats. The present study demonstrates acceptable physicochemical and pharmacokinetic properties of the compound with excellent drugable nature, hence EFD in the form of standardized formulation can be developed as primary or adjuvant therapy against PCa and toxins-induced gonadotoxicity.
    MeSH term(s) Animals ; Male ; Rats ; Apoptosis ; bcl-2-Associated X Protein/metabolism ; Cell Line, Tumor ; Ipomoea batatas/chemistry ; Molecular Docking Simulation ; NF-kappa B/metabolism ; Poly(ADP-ribose) Polymerase Inhibitors/pharmacology ; Prostatic Neoplasms/pathology ; Proto-Oncogene Proteins c-bcl-2/metabolism ; Rats, Sprague-Dawley ; Triterpenes/pharmacology ; Triterpenes/therapeutic use ; Tumor Suppressor Protein p53
    Chemical Substances bcl-2-Associated X Protein ; bisphenol A (MLT3645I99) ; NF-kappa B ; oleanane ; Poly(ADP-ribose) Polymerase Inhibitors ; Proto-Oncogene Proteins c-bcl-2 ; Triterpenes ; Tumor Suppressor Protein p53
    Language English
    Publishing date 2022-12-29
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules28010290
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article: Development and evaluation of pH sensitive semi-interpenetrating networks: assessing the impact of itaconic acid and aloe vera on network swelling and cetirizine release.

    Ajaz, Nyla / Bukhsh, Munnaza / Kamal, Yousaf / Rehman, Fauzia / Irfan, Muhammad / Khalid, Syed Haroon / Asghar, Sajid / Rizg, Waleed Y / Bukhary, Sahar M / Hosny, Khaled M / Alissa, Mohammed / Safhi, Awaji Y / Sabei, Fahad Y / Khan, Ikram Ullah

    Frontiers in bioengineering and biotechnology

    2023  Volume 11, Page(s) 1173883

    Abstract: Hydrogels are crosslinked three-dimensional networks, and their properties can be easily tuned to target the various segments of the gastrointestinal tract (GIT). Cetirizine HCl (CTZ HCl) is an antihistaminic drug, which when given orally can upset the ... ...

    Abstract Hydrogels are crosslinked three-dimensional networks, and their properties can be easily tuned to target the various segments of the gastrointestinal tract (GIT). Cetirizine HCl (CTZ HCl) is an antihistaminic drug, which when given orally can upset the stomach. Moreover, this molecule has shown maximum absorption in the intestine. To address these issues, we developed a pH-responsive semi-interpenetrating polymer network (semi-IPN) for the delivery of CTZ HCl to the lower part of the GIT. Initially, 10 different formulations of itaconic acid-grafted-poly (acrylamide)/aloe vera [IA-g-poly (AAm)/aloe vera] semi-IPN were developed by varying the concentration of IA and aloe vera using the free radical polymerization technique. Based on swelling and sol-gel analysis, formulation F5 containing 0.3%w/w aloe vera and 6%w/w IA was chosen as the optimum formulation. The solid-state characterization of the optimized formulation (F5) revealed a successful incorporation of CTZ HCl in semi-IPN without any drug-destabilizing interaction. The
    Language English
    Publishing date 2023-05-09
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2719493-0
    ISSN 2296-4185
    ISSN 2296-4185
    DOI 10.3389/fbioe.2023.1173883
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article: Rural industrialization

    Kamal, Yousaf

    Pakistan essays on economic problems . Publ. by Raza Mehdi , p. 1-28

    a Maoist model

    1979  , Page(s) 1–28

    Author's details Yousaf Kamal
    Keywords Entwicklungstheorie ; Industrialisierung ; China
    Publisher Progressive Publ.
    Publishing place Lahore
    Document type Article
    Database ECONomics Information System

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