Dehydroepiandrosterone-α-2-Deoxyglucoside Exhibits Enhanced Anticancer Effects in MCF-7 Breast Cancer Cells and Inhibits Glucose-6-Phosphate Dehydrogenase Activity.

In the pentose phosphate pathway, dehydroepiandrosterone (DHEA) uncompetitively inhibits glucose-6-phosphate dehydrogenase (G6PD), reducing NADPH production and increasing oxidative stress, which can influence the onset and/or progression of several diseases, including cancer. 2-Deoxy-D-glucose (2-DG), a glucose mimetic, competes with glucose for cellular uptake, inhibiting glycolysis and competing with glucose-6-phosphate (G-6-P) for G6PD activity. In this study, we report that DHEA-α-2-DG (5), an α-covalent conjugate of DHEA and 2-DG, exhibits better anticancer activity than DHEA, 2-DG, DHEA +2-DG, and polydatin in MCF-7 cells, and reduces NADPH/NADP ratio in cellular assays.

Quinazolinone-Peptido-Nitrophenyl-Derivatives as Potential Inhibitors of SARS-CoV-2 Main Protease.

The severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2-M) plays an essential role in viral replication, transcription, maturation, and entry into host cells. Furthermore, its cleavage specificity for viruses, but not humans, makes it a promising drug target for the treatment of coronavirus disease 2019 (COVID-19). In this study, a fragment-based strategy including potential antiviral quinazolinone moiety and glutamine- or glutamate-derived peptidomimetic backbone and positioned nitro functional groups was used to synthesize putative M inhibitors.

GSK-3 inhibitors enhance TRAIL-mediated apoptosis in human gastric adenocarcinoma cells.

Resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis has been reported in some cancer cells, including AGS human gastric adenocarcinoma cells. Reducing this resistance might shed light on the treatment of human gastric adenocarcinoma. In this study, we examined whether glycogen synthase kinase-3 (GSK-3) inhibitors can restore TRAIL responsiveness in gastric adenocarcinoma cells.

Promoted Angiogenesis Associated With Modified MMP-2/TIMP-2 Balance and Activation of VEGF Ligand/Receptors Expression.

J. Sm (), known as Gu-Sui-Bu, is used in traditional Chinese medicine to treat common injuries, including bone fractures and bruising. The specific functional mechanisms of the angiogenic and endothelial cell migration properties of are currently unclear.

The characteristics and prescription patterns of Chinese herbal medicine in clinical practice for the treatment of anemia.

Objective: Chinese herbal medicine (CHM) is frequently applied to patients to improve the symptoms and signs associated with anemia. The aim of this study is to use the claims data from the National Health Insurance Research Database (NHIRD) in Taiwan to analyze CHM prescription patterns and to identify the frequency and combinations of CHM commonly used to treat anemia.

Materials And Methods: A total of 41,028 patients were diagnosed with anemia in Taiwan within the defined study period.

Radix Paeoniae Rubra stimulates osteoclast differentiation by activation of the NF-κB and mitogen-activated protein kinase pathways.

Background: Radix Paeoniae Rubra (RPR), a traditional Chinese herb, has anti-inflammatory and immuno-regulatory properties. This study explored the effects of RPR on stimulation of osteoclast differentiation in RAW264.7 cells and peripheral blood mononuclear cells (PBMC)s.

Hepatoprotective effect of the ethanol extract of Polygonum orientale on carbon tetrachloride-induced acute liver injury in mice.

Polygonum orientale L. (Polygonaceae) fruits have various medicinal uses, but their hepatoprotective effects have not yet been studied. This study investigated the hepatoprotective activity of the ethanolic extract of P.

Hirsutane-Type Sesquiterpenes with Inhibitory Activity of Microglial Nitric Oxide Production from the Red Alga-Derived Fungus Chondrostereum sp. NTOU4196.

The marine red alga Pterocladiella capillacea is an economic alga for the food industry in Taiwan, and its associated highly diversified fungi have not been investigated meticulously thus far. The EtOAc extract of the fermented broth of Chondrostereum sp. NTOU4196, a fungal strain isolated from P.

Development of a new type of multifunctional fucoidan-based nanoparticles for anticancer drug delivery.

Fucoidan, a sulfated marine polysaccharide, has many potential biological functions, including anticancer activity. Recently, fucoidan has been reported to target P-selectin expressed on metastatic cancer cells. Increasing research attention has been devoted to the developments of fucoidan-based nanomedicine.

Piceatannol Exerts Anti-Obesity Effects in C57BL/6 Mice through Modulating Adipogenic Proteins and Gut Microbiota.

Obesity is a global health concern. Piceatannol (Pic), an analog of resveratrol (Res), has many reported biological activities. In this study, we investigated the anti-obesity effect of Pic in a high-fat diet (HFD)-induced obese animal model.

Nanoparticle Targeting CD44-Positive Cancer Cells for Site-Specific Drug Delivery in Prostate Cancer Therapy.

Prostate cancer is one of the leading causes of cancer death in adult men and is a multistage disease with therapeutic challenges of local recurrent advanced tumors and distant metastatic disease. CD44 is a multifunctional and multistructural cell surface glycoprotein that is involved in cell-cell interactions, cell proliferation, and cell migration. In the study, we produced negatively charged and biocompatible hyaluronic acid-based nanoparticles as a therapeutic system for targeting CD44-positive cancer cells.

Genistein suppresses leptin-induced proliferation and migration of vascular smooth muscle cells and neointima formation.

Obesity is a strong risk factor for the development of cardiovascular diseases and is associated with a marked increase in circulating leptin concentration. Leptin is a peptide hormone mainly produced by adipose tissue and is regulated by energy level, hormones and various inflammatory mediators. Genistein is an isoflavone that exhibits diverse health-promoting effects.

Berberine-loaded targeted nanoparticles as specific Helicobacter pylori eradication therapy: in vitro and in vivo study.

Aim: The aim of this work was to develop fucose-conjugated nanoparticles and control the release of berberine, and demonstrate that these particles come into contact with Helicobacter pylori and enhance the suppressive effect of berberine on H. pylori growth.

Materials & Methods: Fucose-chitosan/heparin nanoparticle-encapsulated berberine was prepared and delivery efficiency was monitored by confocal laser scanning microscopy.

Antiviral activity of chemical compound isolated from Artemisia morrisonensis against hepatitis B virus in vitro.

The compound p-hydroxyacetophenone (PHAP) isolated from Artemisia morrisonensis was found to have potential anti-HBV effects in HepG2 2.2.15 cells.

Analgesic and Anti-Inflammatory Activities of the Ethanolic Extract of Artemisia morrisonensis Hayata in Mice.

The aim of this study was to investigate the possible analgesic and anti-inflammatory mechanisms of the ethanolic extract of A. morrisonensis Hayata (AM(EtOH)). Two models were employed for evaluation of the analgesic effects: acetic acid-induced writhing response and formalin-induced paw licking.

Quantitative analysis of fructo-oligosaccharides in Gynura divaricata subsp. formosana by high performance anion exchange chromatography-pulsed amperometric detection.

High performance anion exchange chromatography-pulsed amperometric detection was employed in this study to conduct quantitative analysis of the inulin-related fructo-oligosaccharides present in Gynura divaricata subsp. formosana. Result obtained for the 1-kestose (GF2), nystose (GF3) and 1F-beta-fructofuranosyl-nystose (GF4) contents were 146.

Hypoglycemic constituents of Gynura divaricata subsp. formosana.

Gynura divaricata Kitam. subsp. formosana is a folk medicine used as a hypoglycemic agent for diabetes patients in Taiwan.

Antihepatitis B virus constituents of Solanum erianthum.

Eleven compounds were isolated from the methanolic extract of the leaves of Solanum erianthum D. Don, including five alpha-linolenic acid analogs, alpha-linolenic acid (1), 13S-hydroxy-9(Z),11(E)-octadecadienoic acid (2), 9S-hydroxy-10(E),12(Z), 15(Z)-octadectrienoic acid (3), 9(Z),11(E)-octadecadienoic acid (4), and octadecanoic acid (5); two benzofuran-type lactones, loliolide (6) and dihydroactinidiolide (7); two steroidal alkaloids, solasonine (8) and solamargine (9); a flavonol glycoside, camelliaside C (10); and a flavone, 5-methoxy-(3,4"-dihydro-3",4"-diacetoxy)-2",2'-dimethylpyrano-(7,8:5",6")-flavone (11). Among these isolated compounds, 9 showed the most potent activity against HBsAg, with an IC50 of 1.

Oleanane-type triterpenoids from the leaves and twigs of Fatsia polycarpa.

Seven new oleanane-type triterpenoids (1-7), named fatsicarpains A-G, and the known compounds 3α-hydroxyolean-11,13(18)-dien-28-oic acid (8) and 3α-hydroxyolean-11-en-28,13β-olide (9) were isolated from the leaves and twigs of Fatsia polycarpa on the basis of bioassay-guided fractionation. The structures of compounds 1-7 were elucidated through spectroscopic analyses and single-crystal X-ray crystallography of 1, 8, and 9. Cytotoxicity against HepG2 2.

Influence of gallate esterification on the activity of procyanidin B2 in androgen-dependent human prostate carcinoma LNCaP cells.

Purpose: Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compound B2, all isolated from grape seed extract (GSE).

Materials And Methods: Study compounds were isolated from GSE by several chromatographic steps and structures determined by a combination of enzymatic hydrolysis, mass spectrometry and comparisons with standards. Cells, treated with these compounds, were assessed for viability and apoptosis and examined by western blotting.

Hydrophobic metabolites from Rhododendron formosanum and their allelopathic activities.

Eighteen components were isolated from the methanolic extract of leaves of Rhododendron formosanum Hemsl. (Ericaceae), an endemic species in Taiwan, and evaluated for their allelopathic properties. Of the isolated compounds, 3beta-friedelinol, 5,6beta-epoxy-5beta-stigmastan-3beta-ol, 5,6alpha-epoxy-5alpha-stigmastan-3beta-ol, lupeol and ursolic acid revealed inhibitory effects at 10(-4) M or above, whereas alpha-tocopherol, friedelin and beta-amyrin acetate exhibited stimulatory effects on the radicle growth of the test plants at the same concentration or above.

Cloning and characterization of the biosynthetic gene cluster for tomaymycin, an SJG-136 monomeric analog.

Tomaymycin produced by Streptomyces achromogenes is a naturally produced pyrrolobenzodiazepine (PBD). The biosynthetic gene cluster for tomaymycin was identified and sequenced. The gene cluster analysis reveals a novel biosynthetic pathway for the anthranilate moiety of PBDs.

Biosynthesis of sibiromycin, a potent antitumor antibiotic.

Pyrrolobenzodiazepines, a class of natural products produced by actinomycetes, are sequence selective DNA alkylating compounds with significant antitumor properties. Among the pyrrolo[1,4]benzodiazepines (PBDs) sibiromycin, one of two identified glycosylated PBDs, displays the highest affinity for DNA and the most potent antitumor properties. Despite the promising antitumor properties clinical trials of sibiromycin were precluded by the cardiotoxicity effect in animals attributed to the presence of the C-9 hydroxyl group.

The structural diversity of phthalides from the Apiaceae.

Phthalides, and their corresponding dihydro and tetrahydro analogues, are components of several genera of the plant family Apiaceae. These taxa have been reported as exhibiting a wide range of bioactivities against experimental models of several illnesses and physiological conditions, including microbial and viral infections, stroke, tuberculosis, and vasoconstriction. Many of these genera are purported to possess medicinal values, and of these several are considered to be traditional herbal medicines.

Fungicidal activities of dihydroferulic acid alkyl ester analogues.

The natural product dihydroferulic acid (DFA, 1) and the synthesized DFA methyl (4a), ethyl (4b), propyl (4c), hexyl (4d), octyl (4e), and decyl (4f) esters were examined for antifungal activity. Test fungi included Saccharomyces cerevisiae (wild type, and deletion mutants slt2 Delta and bck1 Delta), Aspergillus fumigatus, and A. flavus.