1.Radiotracer labeled thymohydroquinyl gallate capped gold nanoparticles as a theranostic radiopharmaceutical for targeted antineoplastic and bioimaging.
Munaza BATOOL ; Batool FATIMA ; Dilshad HUSSAIN ; Rubaida MAHMOOD ; Muhammad IMRAN ; Saeed AKHTER ; Muhammad Saqib KHAN ; Saadat MAJEED ; Muhammad NAJAM-UL-HAQ
Journal of Pharmaceutical Analysis 2025;15(4):100965-100965
Thymoquinone (Tq) and gallic acid (GA) are known for counter-tumorigenic characteristics. GA inhibits cancer cell proliferation by interfering with many apoptotic signaling pathways, producing more reactive oxygen species (ROS), focusing on the cell cycle, and suppressing the expression of oncogenes and matrix metalloproteinases (MMPs). In this study, thymoquinone (after reducing to thymohydroquinone) and gallic acid are esterified to form thymohydroquinyl gallate (a prodrug). Thymohydroquinyl gallate (THQG) possesses enhanced antineoplastic efficacy and targeted delivery potential. The chemical and spectroscopic analysis confirms ester synthesis. Gold nanoparticles (AuNPs) are employed as nanocarriers due to their physicochemical and optical characteristics, biocompatibility, and low toxicity. As an efficient drug transporter, gold nanoparticles (AuNPs) shield conjugated drugs from enzymatic digestion. The prodrug acts as a reducing agent for Au metal atoms and is loaded onto it after reduction. The nano drug is radiolabeled with 99mTc and 131I to monitor the drug biodistribution in animals using a gamma camera and single-photon emission computerized tomography (SPECT). 131I is an antineoplastic that helps enhance the drug's efficiency. Chromatographic results reveal promising radiolabeling percentages. In vitro, drug release shows sustained release at pH⁓5.8. In vitro 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) cytotoxicity assay reveals drug potency on CAL 27 and MCF 7 cell lines.
2.Mitochondrial oxidative damage by co-exposure to bisphenol A and acetaminophen in rat testes and its amelioration by melatonin
Hina RASHID ; Mohammad Suhail AKHTER ; Saeed ALSHAHRANI ; Marwa QADRI ; Yousra NOMIER ; Maryam SAGEER ; Andleeb KHAN ; Mohammad F. ALAM ; Tarique ANWER ; Razan AYOUB ; Rana J. H. BAHKALI
Clinical and Experimental Reproductive Medicine 2023;50(1):26-33
Objective:
Human exposure to multiple xenobiotics, over various developmental windows, results in adverse health effects arising from these concomitant exposures. Humans are widely exposed to bisphenol A, and acetaminophen is the most commonly used over-the-counter drug worldwide. Bisphenol A is a well-recognized male reproductive toxicant, and increasing evidence suggests that acetaminophen is also detrimental to the male reproductive system. The recent recognition of male reproductive system dysfunction in conditions of suboptimal reproductive outcomes makes it crucial to investigate the contributions of toxicant exposures to infertility and sub-fertility. We aimed to identify toxicity in the male reproductive system at the mitochondrial level in response to co-exposure to bisphenol A and acetaminophen, and we investigated whether melatonin ameliorated this toxicity.
Methods:
Male Wistar rats were divided into six groups (n=10 each): a control group and groups that received melatonin, bisphenol A, acetaminophen, bisphenol A and acetaminophen, and bisphenol A and acetaminophen with melatonin treatment.
Results:
Significantly higher lipid peroxidation was observed in the testicular mitochondria and sperm in the treatment groups than in the control group. Levels of glutathione and the activities of catalase, glutathione peroxidase, glutathione reductase, and manganese superoxide dismutase decreased significantly in response to the toxicant treatments. Likewise, the toxicant treatments significantly decreased the sperm count and motility, while significantly increasing sperm mortality. Melatonin mitigated the adverse effects of bisphenol A and acetaminophen.
Conclusion
Co-exposure to bisphenol A and acetaminophen elevated oxidative stress in the testicular mitochondria, and this effect was alleviated by melatonin.
3.Intercomparison of environmental gamma doses measured with A NaI (Tl) survey meter and thermoluminescent dosimeters (TLDs) in the Poonch division of Azad Kashmir, Pakistan.
Muhammad RAFIQUE ; Kimberlee J KEARFOTT ; Khalil AHMAD ; Jabeen AKHTER ; Abdul Razzaq KHAN ; Raja Azhar SAEED ; Saeed Ur RAHMAN ; Matiullah ; Muhammad Usman RAJPUT
Biomedical and Environmental Sciences 2014;27(12):969-972
This study presents the intercomparison of the outdoor environmental gamma dose rates measured using a NaI (Tl) based survey meter along with thermoluminescent dosimeters (TLDs) and estimation of excess lifetime cancer risk (ELCR), for the inhabitants of Poonch division of the Azad Kashmir, Pakistan. CaF2: Dy (TLD-200) card dosimeters were installed at height of 1 m from ground at fifteen different locations covering the entire Poonch division comprising of three districts. During three distinct two month time periods within the six month study period, all the installed dosimeters were exposed to outdoor environmental gamma radiations, retrieved and read out at Radiation Dosimetry Laboratory, Health Physics Division, PINSTECH laboratory, Islamabad. The ambient outdoor gamma dose rate measurements were also taken with NaI (Tl) based portable radiometric instrument at 1 m above the ground. To estimate the annual gamma doses, NaI (Tl) based survey data were used for one complete year following the deployment of the dosimeters. The mean annual gamma dose rates measured by TLDs and survey meter were found as 1.47±0.10 and 0.862±0.003 mGy/y respectively. Taking into account a 29% outdoor occupancy factor, the annual average effective dose rate for individuals was estimated as 0.298±0.04 and 0.175±0.03 mSv/y by TLDs and survey meter, respectively. For outdoor exposure, the ELCR was calculated from the TLD and survey meter measurements. The environmental outdoor average annual effective dose obtained in present study are less than the estimated world average terrestrial and cosmic gamma ray dose rate of 0.9 mSv/y reported in UNSCEAR 2000. The possible origins of gamma doses in the area and incompatibilities of results obtained from the two different measurement techniques are also discussed.
Gamma Rays
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adverse effects
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Humans
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Neoplasms
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etiology
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Pakistan
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Radiation Monitoring
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instrumentation

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