Chemicals and Drugs Commons^™

Pharmacological Aspects Of Resveratrol, Raisa Ramirez, Debasish Bandyopadhyay

School of Integrative Biological & Chemical Sciences (Formerly Dept. of Chemistry)

Resveratrol [(E)-5-(4-hydroxystyryl) benzene-1,3-diol], also known as 3,4′,5-trihydroxystilbene also known as resveratrol is classified as a phytoalexin in plants such as nuts, cocoa, berries and grapes for self-defense against injury and pathogenic attacks by bacteria and fungi. Research on this compound did not gain popularity until the 1990s when a published paper implied the relationship between resveratrol and the decrease in cardiovascular complications due to the consumption of grape fermented wine in French populations. This observation sparked research on resveratrol even though its concentration in wine is relatively low, leading to the realization that resveratrol has potential for benefits in other …

The Membrane-Active Phytopeptide Cycloviolacin O2 Simultaneously Targets Hiv-1-Infected Cells And Infectious Viral Particles To Potentiate The Efficacy Of Antiretroviral Drugs, Samantha L. Gerlach, Partha K. Chandra, Upal Roy, Sunithi Gunasekera, Ulf Göransson, William C. Wimley, Stephen E. Braun, Debasis Mondal

Health & Biomedical Sciences Faculty Publications

Background: Novel strategies to increase the efficacy of antiretroviral (ARV) drugs will be of crucial importance. We hypothesize that membranes of HIV-1-infected cells and enveloped HIV-1 particles may be preferentially targeted by the phytopeptide, cycloviolacin O2 (CyO2) to significantly enhance ARV efficacy.

Methods: Physiologically safe concentrations of CyO2 were determined via red blood cell (RBC) hemolysis. SYTOX-green dye-uptake and radiolabeled saquinavir (³H-SQV) uptake assays were used to measure pore-formation and drug uptake, respectively. ELISA, reporter assays and ultracentrifugation were conducted to analyze the antiviral efficacy of HIV-1 protease and fusion inhibitors alone and co-exposed to CyO2.

Results: CyO2 concentrations below …

Rapid Identification Of Phospholipase A2 Transcripts From Snake Venoms, Ying Jia, Pablo Olvera, Frida Rangel, Bianca Mendez, Samir Reddy

School of Integrative Biological & Chemical Sciences (Formerly Dept. of Biology)

Phospholipase A₂ (PLA₂) is a major component in snake venoms and it is found in many different isoforms. To identify transcripts encoding different PLA₂ isoforms, we developed a simple, rapid procedure. Total RNA was extracted from the venoms of three cottonmouth snakes and two diamondback rattlesnakes, and further reverse-transcribed into complementary DNA (cDNA). Using one pair of cottonmouth PLA₂-specific primers and Reverse Transcription Polymerase Chain Reaction (RT-PCR) technique, we identified 27 unique full-length PLA₂ transcripts, including nine sequences identical to the previously documented ones in the database and one novel GIII-like PLA_{2 …}

Antagonizing The Corticotropin Releasing Hormone Receptor 1 With Antalarmin Reduces The Progression Of Endometriosis, Annelyn Torres-Reveron, Leslie L. Rivera-Lopez, Idhaliz Flores, Caroline B. Appleyard

School of Medicine Publications

Endometriosis is a disorder in which endometrial tissue is found outside the uterus causing pain, infertility and stress. Finding effective, non-hormonal and long-term treatments for endometriosis still remains one of the most significant challenges in the field. Corticotropin releasing hormone (CRH) is one of the main signaling peptides within the hypothalamic pituitary adrenal (HPA) axis released in response to stress. CRH can affect nervous and visceral tissues such as the uterus and gut via activation of two types of CRH receptors: CRHR1 and CRHR2. Our aim was to determine if blocking CRHR1 with antalarmin will reduce endometriosis progression. In experiment …

Carglumic Acid Treatment Of A Patient With Recurrent Valproic Acid-Induced Hyperammonemia: A Rare Case Report, Yasar Sattar, Saad Wasiq, Waqas Yasin, Ali M. Khan, Mahwish Adnan, Shristi Shrestha, Nirav B. Patel, Sharaad Latchana

School of Medicine Publications

Valproic acid, first manufactured as an anticonvulsant, is commonly used to treat both neurological and psychiatric conditions. A rare and deadly side effect of this medication is hyperammonemia, presenting as lethargy, confusion, seizure, and, ultimately, coma. In rare circumstances, hyperammonemia can be recurrent and devastating, especially in patients with an underlying N-acetyl glutamate synthase (NAGS) deficiency, as the valproic acid can enhance this enzyme deficiency and inhibit the conversion of ammonia into urea in the liver. For these subtypes of patients, the United States Food and Drug Administration (US FDA) has recently approved carglumic acid, a medication that can act …

Glutathione: A Small Molecule With Big Sense, Cristina E. Raya, Debasish Bandyopadhyay

School of Integrative Biological & Chemical Sciences (Formerly Dept. of Chemistry)

Glutathione, a peptide found in microbes, plants and animals including human plays a key role in maintaining healthy cells. The peptide exists in both reduced and oxidized forms. Synthesis of GSH occurs in the cytosol of cells, and the extent of glutathione synthesis relies on various factors, such as amino acid availability, protein activity etc. Once synthesized, glutathione exists in both forms: oxidized (GSSG) and reduced (GSH). Oxidized glutathione characterized by its disulfide linkage. On the other hand, presence of a thiol group characterizes the reduced glutathione. This thiol makes the tripeptide an essential component of health; it makes glutathione …

Characterization Of Nanodiamondbased Anti-Hiv Drug Delivery To The Brain, Upal Roy, Vadym Drozd, Andriy Durygin, Jesse Rodriguez, Paul Barber, Venkata Atluri, Xiaohua Liu, Thomas G. Voss, Surendra Saxena, Madhavan Nair

Health & Biomedical Sciences Faculty Publications

Human Immunodefciency Virus Type 1 (HIV-1) remains one of the leading causes of death worldwide. Present combination antiretroviral therapy has substantially improved HIV-1 related pathology. However, delivery of therapeutic agents to the HIV reservoir organ like Central nervous system (CNS) remains a major challenge primarily due to the inefective transmigration of drugs through Blood Brain Barrier (BBB). The recent advent of nanomedicine-based drug delivery has stimulated the development of innovative systems for drug delivery. In this regard, particular focus has been given to nanodiamond due to its natural biocompatibility and non-toxic nature–making it a more efcient drug carrier than other …

Antibody-Drug Conjugates For Cancer Therapy: Chemistry To Clinical Implications, Nirnoy Dan, Saini Setua, Vivek K. Kashyap, Sheema Khan, Meena Jaggi, Murali M. Yallapu, Subhash C. Chauhan

School of Medicine Publications

Chemotherapy is one of themajor therapeutic options for cancer treatment. Chemotherapy is often associated with a low therapeutic window due to its poor specificity towards tumor cells/tissues. Antibody-drug conjugate (ADC) technology may provide a potentially new therapeutic solution for cancer treatment. ADC technology uses an antibody-mediated delivery of cytotoxic drugs to the tumors in a targeted manner, while sparing normal cells. Such a targeted approach can improve the tumor-to-normal tissue selectivity and specificity in chemotherapy. Considering its importance in cancer treatment, we aim to review recent efforts for the design and development of ADCs. ADCs are mainly composed of an …

Development Of Polyvinylpyrrolidone/Paclitaxel Self-Assemblies For Breast Cancer, Pallabita Chowdhury, Prashanth K.B. Nagesh, Sheema Khan, Bilal B. Hafeez, Subhash C. Chauhan, Meena Jaggi, Murali M. Yallapu

School of Medicine Publications

The goal of this investigation was to develop and demonstrate a polymer/paclitaxel self-assembly (PTX-SA) formulation. Polymer/PTX-SAs were screened based on smaller size of formulation using dynamic light scattering analysis. Additionally, fluorescence microscopy and flow cytometry studies exhibited that polyvinylpyrrolidone (PVP)-based PTX-SAs (PVP/PTX-SAs) had superior cellular internalization capability in MCF7 and MDA-MB-231 breast cancer cells. The optimized PVP/PTX-SAs exhibited less toxicity to human red blood cells indicating a suitable formulation for reducing systemic toxicity. The formation of PVP and PTX self-assemblies was confirmed using fluorescence quenching and transmission electron microscopy which indicated that the PVP/PTX-SAs were spherical in shape with an …

Gastrin Induces Nuclear Export And Proteasomal Degradation Of Menin In Enteric Glial Cells, Sinju Sundaresan, Cameron A. Meininger, Anthony J. Kang, Amanda L. Photenhauer, Michael M. Hayes, Nirakar Sahoo, Jolanda Lindenberg, Jolanta Grembecka, Tomasz Cierpicki, Lin Ding

School of Integrative Biological & Chemical Sciences (Formerly Dept. of Biology)

Background & aims: The multiple endocrine neoplasia, type 1 (MEN1) locus encodes the nuclear protein and tumor suppressor menin. MEN1 mutations frequently cause neuroendocrine tumors such as gastrinomas, characterized by their predominant duodenal location and local metastasis at time of diagnosis. Diffuse gastrin cell hyperplasia precedes the appearance of MEN1 gastrinomas, which develop within submucosal Brunner's glands. We investigated how menin regulates expression of the gastrin gene and induces generation of submucosal gastrin-expressing cell hyperplasia.

Methods: Primary enteric glial cultures were generated from the VillinCre:Men1FL/FL:Sst-/- mice or C57BL/6 mice (controls), with or without inhibition of gastric acid by omeprazole. Primary …

The Genetic Basis Of The Comorbidity Between Cannabis Use And Major Depression, Karen Hodgson, Laura Almasy, Emma E. M. Knowles, Jack W. Kent Jr., Joanne E. Curran, Thomas D. Dyer, Harald H. H. Goring, Rene L. Olvera, Mary D. Woolsey, Ravindranath Duggirala, Peter T. Fox, John Blangero, David C. Glahn

School of Medicine Publications

Background and aims—While the prevalence of major depression is elevated amongst cannabis users, the role of genetics in this pattern of comorbidity is not clear. This study aimed to estimate the heritability of cannabis use and major depression, quantify the genetic overlap between these two traits, and localize regions of the genome that segregate in families with cannabis use and major depression.

Design—Family-based univariate and bivariate genetic analysis.

Setting—San Antonio, Texas, USA

Participants—Genetics of Brain Structure and Function study (GOBS) participants: 1,284 Mexican-Americans from 75 large multi-generation families and an additional 57 genetically unrelated spouses.

Measurements …

Systematically Characterizing Dysfunctional Long Intergenic Noncoding Rnas In Multiple Brain Regions Of Major Psychosis, Jing Hu, Jinyuan Xu, Lin Pang, Hongying Zhao, Feng Li, Yulan Deng, Ling Liu, Yujia Lan, Xinxin Zhang, Chun Xu

Health & Biomedical Sciences Faculty Publications

Schizophrenia (SZ) and bipolar disorder (BD) are severe neuropsychiatric disorders with serious impact on patients, together termed “major psychosis”. Recently, long intergenic non-coding RNAs (lincRNAs) were reported to play important roles in mental diseases. However, little was known about their molecular mechanism in pathogenesis of SZ and BD. Here, we performed RNA sequencing on 82 postmortem brain tissues from three brain regions (orbitofrontal cortex (BA11), anterior cingulate cortex (BA24) and dorsolateral prefrontal cortex (BA9)) of patients with SZ and BD and control subjects, generating over one billion reads. We characterized lincRNA transcriptome in the three brain regions and identified 20 …

An Insight Into The Role Of Vitamins Other Than Vitamin D On Bone, Robert E. Salazar, Jameela Banu

Health & Biomedical Sciences Faculty Publications

Vitamins are essential micronutrients for normal development. Great emphasis has been placed on vitamin D for bone development and maintenance. However, other vitamins also influence bone health. While some of them are more beneficial to bone and increase bone mass by increasing bone formation, calcium deposition and stimulate osteoblastogenesis, higher concentrations of others have deleterious effects causing fragile bones and increasing the risk of fractures. Knowledge about the effects of these vitamins will help in better maintenance of bone. This review focuses on the information available on vitamins A,B,C,E and K on bone health. Existing information supports vitamin C and …

Curcumin: A Folklore Remedy From Kitchen On The Way To Clinic As Cancer Drug, Debasish Bandyopadhyay

School of Integrative Biological & Chemical Sciences (Formerly Dept. of Chemistry)

Numerous compounds are widely distributed in nature and many of these possess medicinal/biological/pharmacological activity. Curcumin, a polyphenol derived from the rhizomes (underground stems) of Curcuma longa Linn (a member of the ginger family, commonly known as turmeric) is a culinary spice and therapeutic used in India for thousands of years to induce color and flavor in food as well as to treat a wide array of diseases. The origin of turmeric as spice and folklore medicine is so old that it is lost in legend. Curcumin has many beneficial pharmacological effects which includes, but are not limited with, antimicrobial, anti-inflammatory, …

A Historical Analysis Of The Reasoning And Rationale Behind The Federal Prohibition Of Marijuana, Carlos Caro

Theses and Dissertations - UTB/UTPA

This thesis argues that the federal government first created and then maintained the prohibition of marijuana as a reflection of and reaction to, social, political and economic events happening at large in the U.S. and abroad. This thesis primarily compares and contrasts the treatment of marijuana by the federal government and society at large during the 1930s through the early 1980s by building upon scholars’ previous links to race, ethnicity, class and morality to display a pattern of change that was convenient to the federal government’s continued efforts to prohibit marijuana. This thesis demonstrates that changes in attitude and perception …