Astragaloside IV Derivative (LS-102) Alleviated Myocardial Ischemia Reperfusion Injury by Inhibiting Drp1 Phosphorylation-Mediated Mitochondrial Fission.

Our previous studies showed that Astragaloside IV derivative (LS-102) exhibited potent protective function against ischemia reperfusion (I/R) injury, but little is known about the mechanisms. Mitochondrial fission regulated by dynamin-related protein1 (Drp1) is a newly recognized determinant of mitochondrial function. This study aimed to investigate the protection of LS-102 on mitochondrial structure and function by regulating the activity of Drp1 using models of H9c2 cardiomyocyte injury induced by hypoxia-reperfusion (H/R), and rat heart injury induced by I/R.

Dendrobine-type alkaloids and bibenzyl derivatives from Dendrobium findlayanum.

Five previously undescribed compounds, including two dendrobine-type alkaloids (1 and 2), three bibenzyl derivatives (3-5), along with six known compounds were isolated from orchids Dendrobium findlayanum. The structures and absolute configurations of the undescribed compounds were elucidated on the basis of HR-ESIMS, NMR spectroscopy, optical rotation value, as well as electronic circular dichroism (ECD) calculations. The cytotoxic effects of the isolated compounds on three human tumour cell lines (A172, SHSY5Y, and Hela) were evaluated by the MTT assay.

A new strategy for the preparation of antibody against natural glycoside: With astragaloside IV as an example.

A new strategy for the hapten design of natural glycoside and application for the preparation of antibody is reported in this work. With astragaloside IV (AGS-IV) as an example, C6"-CHOH on a glucosyl group was selectively oxidized by 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) oxidation to C6"-COOH, which was subsequently condensed with -NH on bovine serum albumin to get artificial antigen. Then, the successful preparation of artificial antigen was verified by TCL, SDS-PAGE, UV, and MALDI-TOF-MS.

Antifungal Halogenated Cyclopentenones from the Endophytic Fungus of by the One Strain-Many Compounds Strategy.

Phytopathogenic fungi have been considered as being an enormous threat in the agricultural system. In our search of new antifungal natural products, nine new halogenated cyclopentenones, bicolorins A-I (, and ), along with three known cyclopentenones (, , and ) were isolated from the endophytic fungus of by the one strain-many compounds strategy. Their structures and absolute configurations were elucidated based on extensive spectroscopic analysis, X-ray crystallographic analysis, and time-dependent density functional theory-equivalent circulating density calculations.

Competitive Protein Binding Assay of Naproxen by Human Serum Albumin Functionalized Silicon Dioxide Nanoparticles.

We have developed a new competitive protein binding assay (CPBA) based on human serum albumin functionalized silicon dioxide nanoparticles (nano-SiO-HSA) that can be used for naproxen determination in urine. Compared with a conventional multi-well reaction plate, nano-SiO with a high surface-area-to-volume ratio could be introduced as a stationary phase, markedly improving the analytical performance. Nano-SiO-HSA and horseradish peroxidase-labeled-naproxen (HRP-naproxen) were prepared for the present CPBA method.

Reusable Xerogel Containing Quantum Dots with High Fluorescence Retention.

Although various analytical methods have been established based on quantum dots (QDs), most were conducted in solution, which is inadequate for storage/transportation and rapid analysis. Moreover, the potential environmental problems caused by abandoned QDs cannot be ignored. In this paper, a reusable xerogel containing CdTe with strong emission is established by introducing host⁻guest interactions between QDs and polymer matrix.

β-Cyclodextrin based air filter for high-efficiency filtration of pollution sources.

Airborne particulate matter (PM) pollution has become a serious environmental problem. Thus, there is a need for the development of air filters with satisfactory overall performance. In this paper, we develop a kind of β-cyclodextrin (β-CD) based air filter with high strength, which has not only high filtration efficiency (about 99%) but also good air permeability (the pressure drop is only 45Pa).

Determination of a astragaloside IV derivative LS-102 in plasma by ultra-performance liquid chromatography-tandem mass spectrometry in dog plasma and its application in a pharmacokinetic study.

Background: Astragalosidic acid (LS-102) is a new water-soluble derivative of astragaloside IV - a major effective component isolated from the Chinese herb Astragali Radix. Our previous study showed that LS-102 exhibited potent cardiovascular activity.

Purpose: The objective of this study was to investigate the pharmacokinetic properties of LS-102 after single-dose, oral administration in beagle dogs by developing and validating an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method.

Two new lignans from .

A new dibenzocyclooctdiene (), and a new eupodienone () type lignans were isolated along with five known analogues from the whole plant of Pei. The structures of the new compounds were elucidated on the basis of detailed spectroscopic analysis. Bioassay results showed that compounds and exhibited no antimicrobial activity against four Gram-positive bacterial strains and four Gram-negative bacteria at the concentration of 1 mg/mL.

Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).

Background And Objectives: Astragaloside IV (AGS IV) is the most important bioactive constituent of Radix Astragali. However, its disappointing clinical application is mainly caused by its very low solubility in biologic fluids, resulting in poor bioavailability after oral administration. We recently obtained a novel water-soluble derivative of AGS IV (astragalosidic acid, LS-102) that displayed significant cardioprotective potential against hypoxia-induced injury.

A efficient method to identify cardioprotective components of Astragali Radix using a combination of molecularly imprinted polymers-based knockout extract and activity evaluation.

Although herb medicines have become the major source for new drug discovery, many of them are largely under-explored due to the purity-activity relationship. Efficient identification of bioactive compounds in conventional stepwise separation and isolation has not yet been elucidated. Therefore, we proposed a new separation strategy for holism understanding of herb pharmacology using molecularly imprinted polymers (MIPs).

Antiproliferative Sesquiterpenoids from Ligularia rumicifolia with Diverse Skeletons.

Twenty-two new sesquiterpenoids with four skeletal types and 15 known analogues were isolated from the whole plants of Ligularia rumicifolia. The structures of the isolates were elucidated based on comprehensive spectroscopic data analysis. Compound 1 is a C nor-sesquiterpenoid featuring a 6/6/6 tricyclic skeleton with a 9,13-ether bridge.

Bioactive halogenated dihydroisocoumarins produced by the endophytic fungus Lachnum palmae isolated from Przewalskia tangutica.

Guided by the UPLC-ESIMS profile, seven previously undescribed halogenated dihydroisocoumarins, palmaerones A-G, along with eleven known dihydroisocoumarins, were isolated from Lachnum palmae, an endophytic fungus from Przewalskia tangutica by exposure to a histone deacetylase inhibitor SAHA. Structures of the isolates were elucidated by analysis of their NMR, MS and optical rotation values. The antimicrobial, anti-inflammatory and cytotoxic activities of palmaerones A-G were evaluated.

Effective Formaldehyde Capture by Green Cyclodextrin-Based Metal-Organic Framework.

A kind of metal-organic framework made from γ-cyclodextrin (γ-CD) and potassium ions were explored as excellent formaldehyde (HCHO) absorbents. The adsorption capacity and speed of γ-CD-MOF-K are both about 9 times higher than those of activated carbon, which are attributed to the porous structure and synergistic effect of hydrogen bonding and host-guest interactions.

Astragalosidic Acid: A New Water-Soluble Derivative of Astragaloside IV Prepared Using Remarkably Simple TEMPO-Mediated Oxidation.

There is an urgent need for a water-soluble derivative of astragaloside IV for drug R&D. In the present study, a remarkably simple method for the preparation of such a water-soluble derivative of astragaloside IV has been developed. This protocol involves oxidative 2,2,6,6-tetramethylpiperidine-1-oxyl free radical (TEMPO)-mediated transformation of astragaloside IV to its carboxylic acid derivative, which is a new compound named astragalosidic acid.

An efficient direct competitive nano-ELISA for residual BSA determination in vaccines.

A simple, fast, and highly sensitive direct competitive enzyme-linked immunosorbent assay (ELISA) based on bovine serum albumin (BSA) antigen labeled amine-terminated silicon dioxide (SiO-NH-BSA) nanoparticles was developed to determine residual BSA in vaccines. As nano-ELISA using nanomaterials with a very high surface-to-volume ratio has emerged as a promising strategy, SiO-NH-BSA nanoparticles were prepared in this study by the coupling of BSA to SiO nanoparticles modified with amidogen, followed by the quantification of BSA via a direct competitive binding of BSA-antigen-labeled SiO nanoparticles to anti-BSA antibody conjugated with horseradish peroxidase. The validation study showed that the linear range of this method was from 1 to 90 ng/mL (r = 0.

Development of a nano-SiO based enzyme-linked ligand binding assay for the determination of ibuprofen in human urine.

The application domains of classic enzyme-linked ligand binding assay (ELBA) is relatively narrow due to the high cost and hardly available binding receptor. In here, we described for the first time the possibility of developing a new ELBA based on silica nanoparticles (nano-SiO) to assess the ibuprofen in human urine. Nano-SiO with a large surface area was introduced as stationary phase to improve the analytical performance.

Reactive Oxygen Species and Glutathione Dual Redox-Responsive Supramolecular Assemblies with Controllable Release Capability.

A dual redox and biorelevant triggered supramolecular system is developed through noncovalent supramolecular inclusion interactions between the ferrocene (Fc) modified on camptothecin (CPT) and β-cyclodextrin (β-CD) at the end of methoxy polyethylene glycol (mPEG). With these two segments, a stable noncovalent supramolecular structure, i.e.

6-TIPS-β-Cyclodextrin-Modified Fe O for Facile Enantioseparation of 1-(1-Naphthyl)ethylamine.

A new type of chiral magnetic nanoparticle was prepared from covalently linked magnetic nanoparticles (Fe O ) and heptakis-(6-O-triisopropylsilyl)-β-cyclodextrin (6-TIPS-β-CD). The resulting selectors (TIPS-β-CD-MNPs) combined the good magnetic properties Fe O and efficient chiral recognition ability of 6-TIPS-β-CD. The enantioselectivity of TIPS-β-CD-MNPs towards 1-(1-naphthyl)ethylamine was six times higher than that of the parent β-CD modified Fe O particles.

Cytotoxic triterpenoid saponins from Clematis tangutica.

Eight previously undescribed oleanane-type triterpenoid saponins, clematangoticosides A-H, together with eight known saponins, were isolated from the whole plants of Clematis tangutica (Maxim.) Korsh. Their structures were elucidated by extensive spectroscopic analysis, in combination with chemical methods (acid hydrolysis and mild alkaline hydrolysis).

Three new oxazoline alkaloids from Gymnotheca chinensis.

Three novel oxazoline alkaloids, 1-oxa-3-azaspiro [4.5] dec-2-ene-8-one (1), 1-oxa-3-azaspiro [4.5] dec-2, 6-diene-8-one (2), and 1-oxa-3-azaspiro [4.

[Chemical Constituents of n-Butanol Extract of Myrothecium verrucaria].

Objective: To study the chemical constituents of n-butanol extract in the broth of Myrothecium verrucaria.

Methods: The chemical constituents were isolated,purified and identified by various chromatographic and spectral techniques.

Results: 14 compounds were isolated and identified from n-butanol extracts of Myrothecium verrucaria broth.

A Rapid Study of Botanical Drug-Drug Interaction with Protein by Re-ligand Fishing using Human Serum Albumin-Functionalized Magnetic Nanoparticles.

A great many active constituents of botanical drugs bind to human serum albumin (HSA) reversibly with a dynamic balance between the free- and bound-forms in blood. The curative or side effect of a drug depends on its free-form level, which is always influenced by other drugs, combined dosed or multi-constituents of botanical drugs. This paper presented a rapid and convenient methodology to investigate the drug-drug interactions with HSA.

Cyclic Lipopeptides with Herbicidal and Insecticidal Activities Produced by Bacillus clausii DTM1.

Seven cyclic lipopeptide biosurfactants (1-7) were isolated for the first time from the fermentation broth of endophytic Bacillus clausii DTM1 and were identified as anteisoC13[Val7] surfactin-(L-Glu)-O-methyl-ester (1), anteisoC12[Val7] surfactin (2), anteisoC15[Val7] surfactin (3), isoC14[Leu7] surfactin (4), anteisoC12[Leu7] surfactin (5), nC13[Leu7] surfactin (6), and anteisoC14[Leu7] surfactin-(L-Glu)-O-methyl-ester (7); 1 has not been isolated before as a natural product from any source. Plate-based herbicide and insecticide bioassays showed that all compounds exhibited interesting insecticidal and herbicidal activities.