Novel sesquiterpenoids isolated from Chimonanthus praecox and their antibacterial activities.

In the present study, four new sesquiterpenoids, chimonols A-D (compounds 1-4), together with four known compounds (5-8) were isolated from the EtOAc extract of Chimonanthus praecox Link. The structures of these new compounds were elucidated on the basis of spectroscopic techniques (UV, IR, MS, and 1D and 2D NMR), and their absolute configurations were established by comparing experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 1-8 were evaluated for antimicrobial activities and the minimum inhibitory concentrations (MICs) were determined by the broth microdilution method in 96-well culture plates.

A novel synthesized 3', 5'-diprenylated chalcone mediates the proliferation of human leukemia cells by regulating apoptosis and autophagy pathways.

Leukemia is a hematologic malignancy with poor prognosis in humans and chemotherapy is the main strategy for treating leukemia patients. Novel drugs with better selectivity and lower toxicity are required for the treatment of patients. A novel 3',5'-diprenylated chalcone, (E)-1-(2-hydroxy-4-methoxy-3,5-diprenyl) phenyl-3-(3- pyridinyl)-propene-1-one (C10) is a potential new anti-leukemia agent.

Novel 3',5'-diprenylated chalcones inhibited the proliferation of cancer cells in vitro by inducing cell apoptosis and arresting cell cycle phase.

A double Claisen rearrangements synthetic strategy was established for the total synthesis of 4,4'-dimethyl medicagenin (compound 6c). A series of its analogs also were prepared, including two novel 3',5'-diprenylated chalcones, in which ring B was replaced by azaheterocycle. The structures of the twenty-two newly synthesized compounds were confirmed by H NMR, C NMR and ESI-MS.

Metabolite identification of bentysrepinine (Y101), a novel anti-HBV agent in rats using a five-step strategy based on a combined workflow with two different platforms of liquid chromatography-tandem mass spectrometry.

Bentysrepinine (Y101), a derivative of repensine (a compound isolated from Dichondrarepens Forst), is a novel phenyalanine dipeptide inhibiting DNA-HBV and cccDNA activities and is currently under development for the treatment of hepatitis B virus (HBV)-infected hepatitis. Our previous study implied that there might be an existence of extensive metabolism of Y101 in rats. Therefore, it is necessary to perform metabolic profiling study to further evaluate its safety and drug-like properties.

[The in vitro transport mechanism of bentysrepinine: a novel anti-hepatitis B virus drug candidate].

Bentysrepinine (Y101), a derivative of phenylalanine dipeptide, is a novel drug candidate for the treatment of hepatitis B virus (HBV) infection. Our previous preclinical pharmacokinetic study showed that its in vivo absorption and distribution characteristics were probably related to transmembrane transport after Y101 was administered intragastically in rats. In this study, Caco-2 and MDCK-MDR1 cell models were used to investigate interactions between Y101 and P-gp through the apparent permeation coefficient (P(app)) and efflux ratio (RE); the results showed that Y101 was a substrate of P-gp.

Synthesis and Biological Evaluation of Matijin-Su Derivatives as Potential Antihepatitis B Virus and Anticancer Agents.

A series of Matijin-Su (MTS, (2S)-2-{[(2S)-2-benzamido-3-phenylpropanoyl]amino}-3-phenylpropyl acetate) derivatives were synthesized and evaluated for their anti-HBV and cytotoxic activities in vitro. Six compounds (4g, 4j, 5c, 5g, 5h and 5i) showed significant inhibition against HBV DNA replication with the IC values in range of 2.18 - 8.

[Studies on flavonoids from Derris eriocarpa].

Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before.

Synthesis and anti-tumor activity evaluation of Matijin-Su derivatives.

A series of Matijin-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-l-phenylalanol) derivatives was synthesized and evaluated for their anti-tumor activities in hepatocellular carcinoma cells. The IC50 of compounds 1, 3, 4, 11, 13 were less than 20μM, and compound 1 and 3 showed an IC50 value of less than 9μM. Expansion inhibition could be found significantly in compound 1 and 3-treated human hepatoma cell HepG2 and PLC/PRF/5, while both compounds exhibit lower toxicity to human hepatocyte cell line L-02.

Vulgarisin A, a new diterpenoid with a rare 5/6/4/5 ring skeleton from the Chinese medicinal plant Prunella vulgaris.

Vulgarisin A (1), a new diterpenoid with an unprecedented 5/6/4/5 fused tetracyclic ring skeleton, has been isolated from the medicinal plant Prunella vulgaris Linn. Its structure was characterized by extensive spectroscopic methods, and the absolute configuration was secured by single crystal X-ray diffraction analysis. Compound 1 showed weak cytotoxicity against human lung carcinoma A549 cells with an IC50 value of 57.

[Chemical constituents from rhizome of Daphne papyracea var. crassiuscula].

Objective: To study chemical constituents from rhizome of Daphne papyracea var. crassiuscula.

Method: Ethyl acetate fraction of 75% ethanol extracts from rhizome of D.

A novel franchetine type norditerpenoid isolated from the roots of Aconitum carmichaeli Debx. with potential analgesic activity and less toxicity.

Further investigation on the phytochemistry of the plant Aconitum carmichaeli Debx. led to isolate a new franchetine type C(19)-diterpenoid alkaloid, guiwuline 1. Its structure was established on the basis of the spectroscopic data (1D and 2D NMR, HRESIMS, UV, IR).

Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents.

A series of Matijing-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-L-phenylalanol) derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity in 2.2.15 cells.

Fangchinoline induces autophagic cell death via p53/sestrin2/AMPK signalling in human hepatocellular carcinoma cells.

Background And Purpose: Fangchinoline is a novel anti-tumour agent with little known of its cellular and molecular mechanisms of action. Here we have investigated the mode of cell death induced by fangchinoline and its underlying mechanism in two human hepatocellular carcinoma cell lines, HepG2 and PLC/PRF/5.

Experimental Approach: Apoptosis and autophagy were monitored in fangchinoline-treated HepG2 and PLC/PRF/5 cells by histological methods.

Aporphine alkaloids from the roots of Stephania viridiflavens.

Further investigation on the phytochemistry of the medicinal plant Stephania viridiflavens led to the isolation of a new naturally occurring aporphine alkaloid, (+)-6R, 6aS-isocorydine N(beta)-oxide (1), together with three known aporphine alkaloids: (+)-6R, 6aS-corydine N(beta)-oxide (2), (+)-N-methyl-laurotetanine (3) and (+)-stepharine (4). The structure and stereochemistry of 1 were determined on the basis of spectroscopic methods and confirmed by synthesis. Alkaloids 2-4 were isolated for the first time from this species.

[Study on the chemical constituents of Humulus scandens].

Objective: To study the chemical constituents of Humulus scandens.

Methods: The compounds were isolated by column chromatography on silica gel and Sephadex LH-20. The structures were identified by means of IR, 1H-NMR,13C-NMR and MS analyses.

Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives.

A series of derivatives of Matijing-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) was synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells.

A novel iridoid from Torricellia angulata var intermedia.

A new iridoid, named torricellate, was isolated from root bark of Torricellia angulata var intermedia, a Chinese folk medicinal plant used to treat bone fracture, tonsillitis and asthma. Its structure was elucidated by NMR, MS, IR and UV, and confirmed by X-ray diffraction studies.

[Studies on factors influencing on ephedrine contents in Maxing Shigan decoction].

Objective: To investigate the factors influencing on the ephedrine contents in different compositions of Maxingshigan decoction.

Method: Adopt mixed uniform design to dismantle recipes, employ the stepping regression analysis to deal with experimental statistics, use the partial correlational analysis to analyze the correlation coefficients and the results were validated.

Result: The regressive equation was of significance, that is Y = 4.

[Determination of contents of amygdalin in traditional and granular decoctions of Maxingshigan decoction by HPLC].

Objective: To determine the contents of amygdalin in traditional and granular decoctions of Maxingshigan decoction.

Methods: The determination was carried out by HPLC with an ODS column and a mobile phase of water-methanol (23:77) at 215 nm.

Results: The content of amygdalin in traditional decoction of Maxingshigan Decoction was 17.

Diastereoselective synthesis of aminobacteriohopanetetrol, a biomarker for methanotrophic bacteria: confirmation of the absolute configuration.

A short and convenient strategy was developed for the first stereoselective chemical synthesis of aminobacteriohopanetetrol (= (1R,2R,3S,4S)-5-amino-1-[(22R)-hopan-30-yl]pentane-1,2,3,4-tetrol; 1), a typical biomarker for methanotrophic bacteria. Comparison of the NMR spectra of the synthetic and natural (peracetylated) product enabled us to unambiguously corroborate the absolute configuration of the functionalized pentyl side chain of 1.

[Determination of glycyrrhizic acid in different decoctions of sanaotang by HPLC and comparison with antifugal effects in vitro].

Objective: To investigate the contents of glycyrrhizic acid in hejian decoction (mixed the traditional Chinese herbs together, then boiling them with water) and the fenjian decoction (boiling the single traditional Chinese herb with water separately, then mixed the abstracts) of Sanaotang (composed of Ephedra sinica, Prunus armeniaca and Glycyrrhiza uralensis) and to compare with their anti-bacterial activities in vitro.

Method: A HPLC method was established with a Agilent Zorbax SB-C18 column (4. 6 mm x 250 mm, 5 microm), a mobile phase of acetonitrile-0.

[Comparative study on transdermal osmosis in vitro of Aconitum brachypodium liniment, gel and patcher].

Objective: To study the transdermal osmosis process of Aconitum brachypodum's liniment, gel and patcher to provide basis for selecting dosage form and controlling the quality.

Method: Taking the cumulate rate of transdermal as index, a imitated Fick's diffusion device was used for the investigating the transdermal osmosis course of the three preparations. The best transdermal mathematics models are obtained and the relations between the transdermal course and the release course are analysed.

Two new naturally occurring optical polyacetylene compounds from Torricellia angulata var intermedia and the determination of their absolute configurations.

Four compounds were isolated from Torricellia angulata var intermedia (Harms.) Hu (Torricelliaceae), followed by formation of derivatives, which gave two new polyacetylene compounds 3 and 4 with respectively a chiral carbon center whose absolute configurations were determined unambiguously by the recently developed extended Mosher's method. This is the first time to obtain natural polyacetylenes possessing a chiral hydroxyl group.

Complex biohopanoids synthesis: efficient anchoring of ribosyl subunits onto a C(30) hopane.

Bacteriohopanoids represent a particularly important series of triterpenoids, widely distributed in bacteria. One of the common features of these pentacyclic hopanepolyols is the presence of an extended non-terpenoid and polyhydroxylated side chain attached to the triterpenic moiety through a C--C bond. The biological function of biohopanoids also has to be addressed when one considers the broad diversity in both structures and functionalities found in the side chain.

Analysis of volatile components of Curcuma sichuanensis X. X. Chen by gas chromatography-mass spectrometry.

Volatile components of Curcuma sichuanensis X. X. Chen growing in Sichuan, China, were extracted by steam distillation and analyzed by using gas chromatography and gas chromatography-mass spectrometry.