Activity Components from Gynostemma pentaphyllum for Preventing Hepatic Fibrosis and of Its Molecular Targets by Network Pharmacology Approach.

Hepatic fibrosis would develop into cirrhosis or cancer without treating. Hence, it is necessary to study the mechanism and prevention methods for hepatic fibrosis. Gynostemma pentaphyllum is a traditional medicinal material with a high medicinal and health value. In this study, nineteen compounds obtained from G. pentaphyllum were qualitative and quantitative by HPLC-FT-ICR MS and HPLC-UV, respectively. Among them, the total content of 19 gypenosides accurately quantified reaches 72.21 mg/g and their anti-proliferation against t-HSC/Cl-6 cells indicated compound 19 performed better activity (IC50: 28.1 ± 2.0 µM) than the other compounds. Further network pharmacology study demonstrated that compound 19 mainly plays an anti-fibrosis role by regulating the EGFR signaling pathway, and the PI3K-Akt signaling pathway. Overall, the verification result indicated that compound 19 appeared to be nontoxic to LO2, was able to modulate the PI3K/Akt signal, led to subG1 cells cycle arrest and the activation of mitochondrial-mediated apoptosis of t-HSC/Cl-6 cells for anti-hepatic fibrosis.

Anti-inflammatory and analgesic activity based on polymorphism of cedrol in mice.

Alternate forms of drug crystals display different physicochemical properties. These include stability, dissolution rate, bioavailability and solubility, which can affect pharmacokinetics and pharmacodynamics. It is therefore important to compare the crystal forms of cedrol to obtain optimal anti-inflammatory and analgesic effects. This study, for the first time, obtained and reports three novel forms (I-III) of cedrol polymorphs. The three forms of cedrol were recrystallized from seven organic solvents by slow cooling or volatilization and identified by thermal analysis, fourier transform infrared spectroscopy, scanning electron microscopy and powder X-ray diffraction analysis. Form I originated from acetone and cyclohexane. Form II was obtained from ethanol, ethyl acetate, acetonitrile and n-hexane. Form III was recrystallized from methanol. The anti-inflammatory and analgesic activities of the three crystalline forms were evaluated by acetic acid induced writhing in mice, the hot plate method, carrageenan induced mouse paw edema models, Xylene-induced mouse ear edema models and cotton pellet-induced mouse granuloma models. Experimental results revealed that the highest performance was achieved from Form I. These findings are of great significance during the early research study of cedrol polymorphs.

Tailor-Made Boronic Acid Functionalized Magnetic Nanoparticles with a Tunable Polymer Shell-Assisted for the Selective Enrichment of Glycoproteins/Glycopeptides.

Biomedical sciences, and in particular biomarker research, demand efficient glycoproteins enrichment platforms. In this work, we present a facile and time-saving method to synthesize phenylboronic acid and copolymer multifunctionalized magnetic nanoparticles (NPs) using a distillation-precipitation polymerization (DPP) technique. The polymer shell is obtained through copolymerization of two monomers-affinity ligand 3-acrylaminophenylboronic acid (AAPBA) and a hydrophilic functional monomer. The resulting hydrophilic Fe3O4@P(AAPBA-co-monomer) NPs exhibit an enhanced binding capacity toward glycoproteins by an additional functional monomer complementary to the surface presentation of the target protein. The effects of monomer ratio of AAPBA to hydrophilic comonomers on the binding of glycoproteins are systematically investigated. The morphology, structure, and composition of all the synthesized microspheres are characterized by transmission electron microscopy (TEM), X-ray powder diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), and vibrating sample magnetometer (VSM). The hydrophilic Fe3O4@P(AAPBA-co-monomer) microspheres show an excellent performance in the separation of glycoproteins with high binding capacity; And strong magnetic response allows them to be easily separated from solution in the presence of an external magnetic field. Moreover, both synthetic Fe3O4@P(AAPBA) and copolymeric NPs show good adsorption to glycoproteins in physiological conditions (pH 7.4). The Fe3O4@P(AAPBA-co-monomer) NPs are successfully utilized to selectively capture and identify the low-abundance glycopeptides from the tryptic digest of horseradish peroxidase (HRP). In addition, the selective isolation and enrichment of glycoproteins from the egg white samples at physiological condition is obtained by Fe3O4@P(AAPBA-co-monomer) NPs as adsorbents.

Insecticidal Potential of Clove Essential Oil and Its Constituents on Cacopsylla chinensis (Hemiptera: Psyllidae) in Laboratory and Field.

Cacopsylla chinensis (Yang and Li) (Hemiptera: Psyllidae) is an important pest of pear in China. As an alternative to conventional chemical pesticides, botanicals including essential oils and their constituents could provide an eco-friendly and nonhazardous control method. In this study, the essential oil of clove buds (Syzygium aromaticum) was obtained by hydrodistillation. Five constituents, accounting for 99.89% of the oil, were identified by gas chromatography-mass spectrometry, and the major constituents were eugenol (88.61%) and eugenol acetate (8.89%), followed by ß-caryophyllene (1.89%). In a laboratory bioassay, clove essential oil, commercial eugenol (99.00%) and ß-caryophyllene (98.00%) exhibited strong contact toxicity against the summerform adults of C. chinensis with LD50 values of 0.730, 0.673, and 0.708 µg/adult, and against the nymphs with LD50 values of 1.795, 1.668, and 1.770 µg/nymph, respectively. In contrast, commercial eugenol acetate (98%) had LD50 values of 9.266 µg/adult and 9.942 µg/nymph. In a field trial, clove essential oil caused significant population reductions of 73.01% (4.80 mg/ml), 66.18% (2.40 mg/ml) and 46.56% (1.20 mg/ml), respectively. Our results demonstrated that clove essential oil and its constituents have potential as a source of natural insecticides.