Molecularly imprinted polymer for solid-phase extraction of oleanolic acid from Ligustrum lucidum fruit.

A molecularly imprinted polymer (MIP) was synthesized for the selective extraction of oleanolic acid (OA), employing OA as the template molecule, acrylamide as the functional monomer, ethylene glycol dimethacrylate as the cross-linking agent, azobisisobutyronitrile as the initiator, and chloroform as the porogenic solvent. The characterization of the obtained MIPs was evaluated by scanning electron microscopy, Fourier transform infrared spectroscopy, Brunauer-Emmett-Teller (BET) analysis and X-ray photoelectron spectroscopy. The MIPs reached adsorption equilibrium within 2 hours to OA, with high adsorption capacity of 124.

Discovery of pentacyclic triterpene conjugates as HBV polymerase/NTCP dual-targeting inhibitors with potent anti-HBV activities.

The inhibition of HBV DNA and elimination of HBsAg has already been established as an indicator for HBV clinic cure, and a novel dual-targeting inhibitors of HBV polymerase/entry are designed and synthesized in this study. Pentacyclic triterpenes (PTs) scaffold of exhibiting a high affinity to NTCP, including glycyrrhitinic acid (GA), oleanolic acid (OA), ursolic acid (UA), and betulinic acid (BA) were linked neatly with the nucleoside drug zidovudine (AZT) through a molecular hybrid strategy to synthesize twenty of PTs-AZT conjugates for targeting HBV polymerase as well as sodium taurocholate cotransporting polypeptide (NTCP). The conjugates showed significant inhibitory effects on the secretion of HBsAg and HBeAg in HepG2.

Kaempferol Improved Rheumatoid Arthritis by Regulating the Immune Imbalance of Treg/Th17.

Objective: The objective of this study was to explore the therapeutic effects of kaempferol (Kae) on rheumatoid arthritis (RA) and to elucidate the underlying mechanisms.

Methods: The collagen-induced arthritis (CIA) model was established using collagen II to induce RA. Mice were treated with Kae at a dose of 25 or 50 mg/kg/day via gavage.

Two C-Steroids and a New Isocoumarin Metabolite from Mangrove Sediment-Derived Fungus sp. SCSIO 41429.

Two new C-steroids derivatives, cyclocitrinoic acid A () and cyclocitrinoic acid B (), and a new isocoumarin metabolite, (3,4)-6,8-dihydroxy-3,4,5-trimethyl-7-carboxamidelisocoumarin (), together with 12 known compounds (-, -) were isolated from the mangrove-sediment fungus sp. SCSIO 41429. The structures of the new compounds were comprehensively characterized by 1D and 2D NMR, HRESIMS and ECD calculation.

Screening bioactive compounds from Fangji Huangqi decoction for treating rheumatoid arthritis via COX-2 magnetic ligand fishing combined with in vivo validation.

Ethnopharmacological Relevance: Fangji Huangqi Decoction (FHD) is a classical Chinese compound formula for treating rheumatoid arthritis (RA) with satisfactory effects. FHD is reputed for its ability to tonify qi with strengthening exterior, and dispel wind while removing dampness, but its mechanisms and bioactive compounds for treating RA remain unclear.

Aim Of The Study: The aim of this study was to explore the key target and bioactive compounds that were responsible for FHD-mediated improvements in RA.

Synthesis and evaluation of pentacyclic triterpenoids conjugates as novel HBV entry inhibitors targeting NTCP receptor.

Chronic liver diseases caused by hepatitis B virus (HBV) are the accepted main cause leading to liver cirrhosis, hepatic fibrosis, and hepatic carcinoma. Sodium taurocholate cotransporting polypeptide (NTCP), a specific membrane receptor of hepatocytes for triggering HBV infection, is a promising target against HBV entry. In this study, pentacyclic triterpenoids (PTs) including glycyrrhetinic acid (GA), oleanolic acid (OA), ursolic acid (UA) and betulinic acid (BA) were modified via molecular hybridization with podophyllotoxin respectively, and resulted in thirty-two novel conjugates.

Ru(II)-Catalyzed Carboamination of Olefins with α-Carbonyl Sulfoxonium Ylides.

The first ruthenium-catalyzed carboamination of olefins with α-carbonyl sulfoxonium ylides is reported. The utilization of an inexpensive ruthenium catalyst enables the concise synthesis of pharmaceutically important isoindolin-1-ones, which possess both a stereogenic center and β-carbonyl side chain. This method is mild, efficient, and scalable and allows for the coupling of a wide range of aryl-, heteroaryl-, alkenyl-, and alkyl-substituted sulfoxonium ylides.

Two New Sesquiterpenoids and a New Shikimic Acid Metabolite from Mangrove Sediment-Derived Fungus sp. SCSIO 41427.

Two new sesquiterpenoid derivatives, elgonenes M () and N (), and a new shikimic acid metabolite, methyl 5--acetyl-5--shikimate (), were isolated from the mangrove sediment-derived fungus sp. SCSIO 41427 together with fourteen known compounds (-). The planar structures were elucidated through nuclear magnetic resonance (NMR) and mass spectroscopic (MS) analyses.

Discovery of Enzyme Inhibitors from Mangrove Sediment Derived Fungus Trichoderma harzianum SCSIO 41051.

One new fatty acid derivative, (2E,4E)-6,7-dihydroxy-2-methylocta-2,4-dienoic acid (1), and 16 known compounds (2-17) were isolated from the mangrove sediment derived fungus Trichoderma harzianum SCSIO 41051. Their structures were established by spectroscopic methods, computational ECD, and Mo(OAc)-induced ECD experiment. All the compounds were evaluated for their acetylcholinesterase (AChE) and pancreatic lipase (PL) inhibition.

Marine-Fungi-Derived Gliotoxin Promotes Autophagy to Suppress Infection in Macrophage.

The (MTB) infection causes tuberculosis (TB) and has been a long-standing public-health threat. It is urgent that we discover novel antitubercular agents to manage the increased incidence of multidrug-resistant (MDR) or extensively drug-resistant (XDR) strains of MTB and tackle the adverse effects of the first- and second-line antitubercular drugs. We previously found that gliotoxin (), 12, 13-dihydroxy-fumitremorgin C (), and helvolic acid () from the cultures of a deep-sea-derived fungus, sp.

Gancao Fuzi decoction regulates the Th17/Treg cell imbalance in rheumatoid arthritis by targeting Foxp3 via miR-34a.

Ethnopharmacological Relevance: During the Eastern Han Dynasty, Zhang Zhongjing first recorded the Gancao Fuzi decoction (GCFZD) formula in the "Synopsis of the Golden Chamber", which is reportedly an effective and safe treatment for rheumatoid arthritis (RA). However, the mechanism underlying the observed improvement in the T helper 17 (Th17)/regulatory T (Treg) cell imbalance in RA obtained with GCFZD has not been reported.

Aim Of The Study: This study aimed to demonstrate whether GCFZD ameliorated RA by modulating the Th17/Treg imbalance in RA mice.

Aromatic Acids and Leucine Derivatives Produced from the Deep-Sea Actinomycetes SCSIO15079 with Antihyperlipidemic Activities.

Six new aromatic acids (-) and three new leucine derivatives containing an unusual oxime moiety (-) were isolated and identified from the deep-sea-derived actinomycetes strain SCSIO15079, together with two known compounds (-). The structures of - including absolute configurations were determined by detailed NMR, MS, and experimental and calculated electronic circular dichroism spectroscopic analyses. Compounds - were evaluated for their antimicrobial and cytotoxicity activities, as well as their effects on intracellular lipid accumulation in HepG2 cells.

Engineered polymer nanoparticles incorporating l-amino acid groups as affinity reagents for fibrinogen.

Synthetic polymer hydrogel nanoparticles (NPs) were developed to function as abiotic affinity reagents for fibrinogen. These NPs were made using both temperature-sensitive N-isopropyl acrylamide (NIPAm) and l-amino acid monomers. Five kinds of l-amino acids were acryloylated to obtain functional monomers: l-phenylalanine (Phe) and l-leucine (Leu) with hydrophobic side chains, l-glutamic acid (Glu) with negative charges, and l-lysine (Lys) and l-arginine (Arg) with positive charges.

Synthesis and antitumor activity of new tetrahydrocurcumin derivatives click reaction.

Three new derivatives of tetrahydrocurcumin , and have been prepared as potent antitumor agents using copper(II)-catalyzed 'click chemistry'. Their structures were identified using H-NMR, C-NMR and HRMS techniques. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay has been carried out to investigate the cytotoxicity against human cervical carcinoma (HeLa), human lung adenocarcinoma (A549), human hepatoma carcinoma (HepG2) and human colon carcinoma (HCT-116).

Effects of Sodium Phosphate and Sodium Nitrite on the Pitting Corrosion Process of X70 Carbon Steel in Sodium Chloride Solution.

In this paper, effects of sodium phosphate (NaPO) and sodium nitrite (NaNO) on the pitting corrosion of X70 carbon steel in 0.10 mol/L NaCl solution were investigated by potentiodynamic polarization technique, electrochemical impedance spectroscopy (EIS) method, scanning electron microscope (SEM) and scanning electrochemical microscope (SECM). The SECM equipment was used to observe the dynamic processes of the pitting corrosion in situ.

Design, synthesis and biological evaluation of seco-A-pentacyclic triterpenoids-3,4-lactone as potent non-nucleoside HBV inhibitors.

A series of seco-A-pentacyclic triterpenoids-3,4-lactone were synthesized and the anti-HBV activities were evaluated in vitro. Several compounds inhibited the secretion of HBV antigen and the replication of HBV DNA in micromolar level. Compounds D7 and D10, seco-A-oleanane-3,4-lactone, suppressed the HBeAg secretion with IC values of 0.

Molecularly imprinted nanoparticles and their releasing properties, bio-distribution as drug carriers.

Molecular imprinted nanoparticles (MINPs) can memorize the shape and functional group positions complementary to template, which account for the large drug loading capacity and slow drug release behavior as drug carriers. We synthesized MINPs via precipitation polymerization with vinblastine (VBL) as a model drug, and investigated the drug loading, releasing property and bio-distribution . The obtained MINPs, from 300 to 450 nm, had smooth surface and favorable dispersibility.

Molecularly imprinted polymers on a silica surface for the adsorption of tobacco-specific nitrosamines in mainstream cigarette smoke.

Tobacco-specific nitrosamines are one of the most important groups of carcinogens in tobacco products. Using adsorbents as filter additives is an effective way to reduce tobacco-specific nitrosamines in cigarette smoke. Molecularly imprinted polymers (MIPs) using nicotinamide as template were grafted on the silica gel surface to obtain MIP@SiO2 and employed as filter additives to absorb tobacco-specific nitrosamines in mainstream cigarette smoke.