Acid-promoted intra- and intermolecular [2+2] cycloaddition of indoles to aryl alkynes to access cyclobutene-fused indolines.

Herein, we have reported the first example of both intra- and intermolecular [2+2] cycloaddition of the electron-rich indoles and unactivated aryl alkynes promoted by the combination of Fe(NO) and HNO, which highlights efficient and selective access to several different types of functionalized cyclobutene-fused indolines from readily available starting materials with cheap catalysts and simple operations.

Modular and scalable synthesis of nematode pheromone ascarosides: implications in eliciting plant defense response.

A highly efficient and modular synthesis of nematode pheromone ascarosides was developed, which highlights a 4-step scalable synthesis of the common intermediate 10 in 23% yield from commercially available l-rhamnose by using orthoesterification/benzylation/orthoester rearrangement as the key step. Six diverse ascarosides were synthesized accordingly. Notably, biological investigations revealed that ascr#1 and ascr#18 treatment resulted in enhanced callose accumulation in Arabidopsis leaves.

Divergent Reactivity in Cu-Catalyzed Oxidative Coupling between Indole/Tryptamine Derivatives and β-Arylacrylic Acids.

Condition-controlled divergent oxidative coupling reactions between indole/tryptamine derivatives and β-arylacrylic acids with the catalysis of copper(II) have been developed. Specifically, a formal Michael addition/dehydration sequence between indoles and β-arylacrylic acids occurred in the presence of catalytic CuBr in CHCN under air, thus affording highly functionalized 2,3-dihydro-1-pyrrolo[1,2-]indoles. In contrast, upon changing the oxidant to BuOOH and the solvent to DCM, the reaction course switched to the unprecedented oxidative coupling/cyclization cascade to give the tetracyclic pyrrolo[2,3-]indolines selectively.

Dual-targeting Rutaecarpine-NO donor hybrids as novel anti-hypertensive agents by promoting release of CGRP.

CGRP, known as the most potent vasodilator substance, plays an important role in hypertension initiation and development. TRPV1 and TRPA1 are critical in promoting the synthesis and release of CGRP, thereby regulating the cardiovascular tone. Rutaecarpine exhibits potent vasodilator and hypertensive effects by stimulating CGRP synthesis and release via activation of TRPV1.

Alpha-glucosidase inhibitor 1-Deoxynojirimycin promotes beige remodeling of 3T3-L1 preadipocytes via activating AMPK.

Obesity is a serious health challenge in the world, and searching effective drugs to cure obesity is of great importance. 1-Deoxynojirimycin (DNJ) is extracted from mulberry leaves and acts as an α-glucosidase inhibitor to lower blood glucose. Recent studies demonstrated that it also has anti-obesity effect, but the mechanisms remain unknown.

Identification of anti-nociceptive constituents from the pollen of L. using effect-directed fractionation.

The pollen of , also known as in Chinese, has been used for treatment of stranguria, hematuria, dysmenorrhea, metrorrhagia and injuries in China for a long time. Extensive efforts have been directed toward its phytochemical and biological aspects. However, little is known about its anti-nociceptive implication and material basis.

Access to 3a-Benzoylmethyl Pyrrolidino[2,3- b]indolines via Cu-Catalyzed Radical Annulation/C3-Functionalization Sequence.

A Cu-catalyzed radical annulation/C3-functionalization cascade of tryptamine derivatives with aryl ethylene is reported. The mild catalytic system enables the facile construction of 3a-benzoylmethylpyrrolidino[2,3- b]indolines with excellent chemo- and regioselectivities. Remarkably, this novel method utilizes earth-abundant and inexpensive cupric salt as the catalyst and air as the co-oxidant, rendering the process highly environmentally friendly and atom economic.

Five macrocyclic glycosides from Schoenoplectus tabernaemontani.

Macrocyclic glycosides with unique 22-membered dimeric lactone skeleton, are rare occurring natural products. There are only ten compounds reported so far. Herein we reported the isolation and characterisation of five macrocyclic glycosides from Schoenoplectus tabernaemontani, including three new compounds (Schoenopolide A-C, 1-3) and two known ones, Berchemolide (4) and Clemoarmanoside B (5).

Phytochemicals of Pogostemon Cablin (Blanco) Benth. aqueous extract: Their xanthine oxidase inhibitory activities.

Bioassay-guided fractionation of the aerial part of P. cablin revealed that fraction A3 of the water extract exhibited significant xanthine oxidase inhibitory activities (IC=85.42±1.

Polyphenolic glycosides isolated from Pogostemon cablin (Blanco) Benth. as novel influenza neuraminidase inhibitors.

Background: Influenza is historically an ancient disease that causes annual epidemics and, at irregular intervals, pandemics. At present, the first-line drugs (oseltamivir and zanamivir) don't seem to be optimistic due to the spontaneously arising and spreading of oseltamivir resistance among influenza virus. Pogostemon cablin (Blanco) Benth.

Design, synthesis, and biological evaluation of crenatoside analogues as novel influenza neuraminidase inhibitors.

Natural products, especially derived from TCMH, have been found to exert antiviral effects against influenza virus. Crenatoside, a phenylethanoid glycoside from Pogostemon cablin Benth, which has been shown as a novel effective NA inhibitor previously, is considered as the leading compound for our further SARs studies. This work presented design, synthesis of novel crenatoside analogues from readily available d-Glucose and l-rhamnose in a convergent manner.

Chemical constituents of Morus alba L. and their inhibitory effect on 3T3-L1 preadipocyte proliferation and differentiation.

Mulberry leaf, an important traditional Chinese medicine, possesses many biological activities, including effects of anti-obesity. However, which constituents of mulberry leaf are responsible for its anti-adipogenic action is unclear. This study primarily investigated the chemical constituents from mulberry leaf and their bioactivity on the proliferation and differentiation of 3T3-L1 preadipocytes.

Purified vitexin compound 1 inhibits growth and angiogenesis through activation of FOXO3a by inactivation of Akt in hepatocellular carcinoma.

Vitexins, isolated from the seeds of the Chinese herb Vitex negundo, is known to exert antitumor activity in cancer xenograft models and cell lines. The aim of the current study was to examine whether the Akt/forkhead box protein O3a (FOXO3a) pathway mediates the biological effects of purified vitexin compound 1 (VB-1) in hepatocellular carcinoma (HCC) cells. The effect of VB-1 on the viability of the HCC cell lines HepG2, Hep3B, Huh-7 and the human embryonic liver cells L-02 was investigated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.

Purified vitexin compound 1 induces apoptosis through activation of FOXO3a in hepatocellular carcinoma.

We previously reported that purified vitexin compound 1 (VB1, a neolignan from the seed of Chinese herb Vitex negundo) exhibited antitumor activity in cancer cell lines and xenograft models. In the present study, we examined the molecular mechanisms by which activation of the FOXO3a transcription factor mediated VB1-induced apoptosis in hepatocellular carcinoma (HCC) cells. The effects of VB1 on the proliferation of HCC cell lines HepG2, Hep3B, Huh-7 and human embryo liver L-02 cells were investigated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.

Lipophilic components from Fructus Viticis Negundo and their anti-tumor activities.

Two new triterpenoids, (24R/S)-24-hydroxy-3α 10α-epoxy-9-eip-cucurbita-25-ene (1a, b), as well as six known compounds (3-8), were isolated from the extraction of Fructus Viticis Negundo. Their structures were established on the basis of spectral analysis. In addition, all the compounds were tested for inhibitory effect against K-562 and A-549 cell lines.

Purified vitexin compound 1 suppresses tumor growth and induces cell apoptosis in a mouse model of human choriocarcinoma.

Objective: In our previous study, we had isolated a series of lignan compounds, termed vitexins, from the seed of Chinese herb Vitex negundo and found broad antitumor activities of these compounds in many cancer xenograft models and cell lines. This study was aimed to determine the antitumor effect of purified vitexin compound 1 (VB1) on choriocarcinoma in vitro and in vivo.

Materials And Methods: The severe combined immunodeficiency mouse model of choriocarcinoma was established to investigate the in vivo effect of VB1.

Two acylated flavonoid glycosides from the leaves of Quercus dentata.

Two new acylated flavonoid glycosides have been isolated from the leaves of Quercus dentata Thunb. On the basis of chemical and spectral data, the structures of the compounds have been elucidated as kaempferol 3-O-(2", 4"-diacetyl-3"-cis-p-coumaroyl-6"-trans-p-coumaroyl)-beta-D-glucopyranoside (1), and kaempferol 3-O-(2"-trans-p-coumaroyl-3", 4"-diacetyl-6"-cisp-coumaroyl)-beta-D-glucopyranoside (2).

Vitexins, nature-derived lignan compounds, induce apoptosis and suppress tumor growth.

Purpose: Lignans such as secoisolariciresinol diglucoside in flaxseed, are metabolizes to bioactive mammalian lignans of END and ENL. Because mammalian lignans have chemical structural similarity to the natural estrogen, they are thought to behave like selective estrogen receptor modulators and therefore have anticancer effect against hormone-related cancers. We isolated a series of lignan compounds, named as Vitexins, from the seed of Chinese herb Vitex Negundo.

[Studies on flavonoid glycosides of Sarcandra glabra].

Objective: To in vestigate the chemical constituents of Sarcandra glabra and obtain a more comprehensive understanding on its effective components.

Method: The constituents were isolated by various column chromatographic method and their structures were elucidated by physico-chemical properties and spectroscopic analysis.

Result: Five flavonoid glycosides were isolated and identified as kaempferol-3-O-beta-D-glucuronide (1), quercetin-3-O-alpha-D-glucuronide (2), quercetin-3-O-beta-D-glucuronopyranoside methyl ester (3), 5, 7, 4'-trihydroxy-8-C-beta-D-glucopyranosyl flavanone (4), neoastilbin (5), 5-O-caffeoylquinic acid methyl ester (6), 3, 4-dihydroxybenzoic acid (7), isofraxidin (8).

[Studies on constituents of Oldenlandia diffusa].

Objective: To investigate the chemical constituents of Oldenlandia diffusa.

Method: The column chromatography with polyamide Sephadex LH -20, silica gel as packing materials and HPLC, were used to separate and purify the chemical components. The structures were elucidated on the basis of physicochemical properties and spectral data.

[Water-soluble chemical constituents of Swertia davidi Franch].

Aim: To study the active constituents of Swertia davidi Franch.

Methods: Column chromatographies on silica gel, Sephadex LH-20 and Diaion-201 et al. were used to isolate and purify the chemical components.