Lung cancer is one of the most common cancers worldwide, causing nearly one million deaths each year. Herein, we present the effect of 2-methoxyestradiol (2-ME), the endogenous metabolite of 17β-estradiol (E2), on non-small cell lung cancer (NSCLC) cells. We observed that 2-ME reduced the viability of lung adenocarcinoma in two-dimensional (2D) and three-dimensional (3D) spheroidal A549 cell culture models.
View Article and Find Full Text PDFCurrently, the world is facing the SARS-CoV-2 pandemic, coronavirus of acute respiratory distress syndrome 2, causes of COVID-19. Coronaviruses are RNA single-stranded viruses that have an envelope. In addition, coronaviruses are classified into four subfamilies: alpha, beta, gamma and delta coronaviruses.
View Article and Find Full Text PDFThe role of autophagy is to degrade damaged or unnecessary cellular structures. Both in vivo and in vitro studies suggest a dual role of autophagy in cancer-it may promote the development of neoplasms, but it may also play a tumor protective function. The mechanism of autophagy depends on the genetic context, tumor stage and type, tumor microenvironment, or clinical therapy used.
View Article and Find Full Text PDFInt J Environ Res Public Health
January 2021
Malignant neoplasms are among the most common diseases and are responsible for the majority of deaths in the developed world. In contrast to men, available data show a clear upward trend in the incidence of lung cancer in women, making it almost as prevalent as breast cancer. Women might be more susceptible to the carcinogenic effect of tobacco smoke than men.
View Article and Find Full Text PDFThe catechins derived from green tea possess antioxidant activity and may have a potentially anticancer effect. PTP1B is tyrosine phosphatase that is oxidative stress regulated and is involved with prooncogenic pathways leading to the formation of a.o.
View Article and Find Full Text PDFGreen tea () is widely known for its anticancer and anti-inflammatory properties. Among the biologically active compounds contained in , the main antioxidant agents are catechins. Recent scientific research indicates that the number of hydroxyl groups and the presence of characteristic structural groups have a major impact on the antioxidant activity of catechins.
View Article and Find Full Text PDFThe structure-activity relationship of the O-benzyl serine side chain was investigated based on the tetrazole-based growth hormone secretagogue BMS-317180 (2). The ortho position of the benzyl moiety was found to be favorable for introduction of substituents. A series of ortho-substituted compounds were synthesized with improved in-vitro and in-vivo activity.
View Article and Find Full Text PDFA tetrazole-based peptidomimetic 2 (BMS-317180) was discovered as a human growth hormone secretagogue (GHS). Compound 2 is a potent, novel, orally effective GHS that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development.
View Article and Find Full Text PDFA novel class of Growth Hormone Secretagogues (GHS), based on a tetrazole template, has been discovered. In vitro SAR and in vivo potency within this new class of GHS are described. The tetrazole 9q exhibits good oral bioavailability in rats and dogs as well as efficacy following an oral 10 mg/kg dose in dogs.
View Article and Find Full Text PDFBioorg Med Chem Lett
April 2005
Several novel series of tetrahydroisoquinoline 1-carboxamides were prepared and shown to be potent growth hormone (GH) secretagogues. Among them, carbamate 12a-E2 displays excellent in vivo activity by increasing plasma GH 10-fold in an anesthetized IV rat model.
View Article and Find Full Text PDFTwo cases of Histoplasma meningitis are presented, illustrating the difficulty in diagnosis and treatment. The first case occurred in a patient with acquired immunodeficiency syndrome as a relapse of disseminated histoplasmosis and resolved after prolonged treatment and ongoing antiretroviral therapy. The second case occurred in a cardiac allograft recipient as meningitis and focal brain lesions that responded to liposomal amphotericin B, but the patient died shortly after therapy was completed.
View Article and Find Full Text PDFA cross-sectional epidemiology study evaluated the role of sexual activity and sexually transmitted diseases (STDs) in the transmission of hepatitis G virus (HGV/GBV-C) and other hepatitis virus infections in 944 subjects. There was a statistically significant higher prevalence of HGV/GBV-C, hepatitis B virus, and hepatitis C virus exposure in the STD clinic group (i.e.
View Article and Find Full Text PDFPurpose: Stiripentol (STP) is a new antiepileptic drug (AED) that inhibits cytochrome P450, resulting in increased plasma concentrations of concomitant AEDs. The efficacy and tolerability of STP as an add-on therapy in children were assessed.
Methods: Two hundred twelve patients with refractory epilepsy, aged from 1 month to 20.
Patients with abetalipoproteinemia, a disease caused by defects in the microsomal triglyceride transfer protein (MTP), do not produce apolipoprotein B-containing lipoproteins. It was hypothesized that small molecule inhibitors of MTP would prevent the assembly and secretion of these atherogenic lipoproteins. To test this hypothesis, two compounds identified in a high-throughput screen for MTP inhibitors were used to direct the synthesis of a highly potent MTP inhibitor.
View Article and Find Full Text PDFA method is presented for estimating replicate polycyclic aromatic hydrocarbon (PAH) concentrations in American lobster (Homarus americanus) digestive gland tissue based on recoveries of added perdeuterated surrogates from a single satisfactory analysis. PAH concentrations demonstrated a large interanimal variance, even in specimens captured at the same time in the same place. Principal component analysis showed that the variability of the total system of biological variables (carapace length, lobster weight, and digestive gland weight) could be adequately summarized by the first principal component alone in each data set.
View Article and Find Full Text PDFA rapid, simple method for screening polychlorinated dibenzo-p-dioxin and dibenzofuran classes in shellfish tissue at pg g-1 wet mass concentrations is described. The method does not require a clean room facility and is based on saponification followed by extraction into hexane, clean-up using gel-permeation chromatography and sulfuric acid treatment, and measurement using capillary gas chromatography-low resolution mass spectrometry with selected ion monitoring. Selected ion monitoring using multiple ions eliminates interferences not removed by clean-up or chromatography.
View Article and Find Full Text PDFA laser scanning confocal microscope has been used to investigate the development of the sea urchin embryo. The samples were fixed in Carnoy's solution at various developmental stages, stained for DNA with the Feulgen reaction, and optically sectioned with a BioRad MRC-500 confocal microscope. Computer-generated stereographic projection images and a three-dimensional contour tracing and reconstruction system were employed to investigate the cleavage pattern during the 6th cleavage division.
View Article and Find Full Text PDFResults of antimicrobial susceptibility testing of anaerobic bacteria isolated at the Mayo Clinic were reviewed for 1982 through 1987 and compared with a previous survey during 1977 through 1981 at this institution. Between the earlier and the later period, clindamycin resistance increased in the Bacteroides fragilis group (from 4% of isolates to 8%). We noted continuing penicillin resistance among Bacteroides species other than B.
View Article and Find Full Text PDFCommercially available kits (Mycobacterium avium Complex Rapid Diagnostic System and Mycobacterium tuberculosis Complex Rapid Diagnostic System; Gen-Probe, Inc., San Diego, Calif.) utilizing nucleic acid hybridization for the rapid identification of members of the M.
View Article and Find Full Text PDFClin Microbiol Rev
October 1988
Fungal infections of the immunocompromised host are being seen with greater frequency than ever before. In addition, a growing list of unusual and unexpected etiologic agents presents a unique and difficult challenge to the clinician and microbiologist. The clinical manifestations of opportunistic fungal infections are often not characteristic and, in many instances, may prevent a rapid diagnosis from being made.
View Article and Find Full Text PDFBull Environ Contam Toxicol
May 1988
J Assoc Off Anal Chem
July 1988
Twenty-five laboratories were sent 2 materials, one an acetone powder of lobster digestive gland, the other, the oil which had been extracted during preparation of the powder. Each laboratory was requested to measure the levels of a suite of polycyclic aromatic hydrocarbons in both materials. The response was poor with only 10 laboratories submitting results.
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