Xingyun Chai

Coreosides A-D, C14-polyacetylene glycosides from the capitula of Coreopsis tinctoria and its anti-inflammatory activity against COX-2.

Four new C14-polyacetylene glycosides, namely coreosides A-D (1-4), were isolated from the capitula of Coreopsis tinctoria, a Snow chrysanthemum or Snow tea that is used as a folk tea for prevention of cardiovascular disease in southern Xinjiang, China. Coreosides A-D feature a long chain structure as its aglycon with two acetylenes on C-8 and C-10 and two olefinics on C-6 and C-12 sites, which construct a large conjugate system. The structures were elucidated on the basis of spectroscopic evidences and hydrolysis. Compounds 1-4 exhibited significant inhibition against cyclooxygenase-2 at the concentration of 1×10(-6) mol/L, with its IC50 values of 0.22-8.8×10(-2) μmol/L.

Phytochemical and pharmacological progress on the genus Syringa

AbstractGenus Syringa, belonging to the Oleaceae family, consists of more than 40 plant species worldwide, of which 22 species, including 18 endemic species, are found in China. Most Syringa plants are used in making ornaments and traditional medicines, whereas some are employed for construction or economic use. Previous studies have shown that extracts of Syringa plants mainly contain iridoids, lignans, and phenylethanoids that have antitumor, antihypertensive, anti-oxidant, and anti-inflammatory activities. This study reviews phytochemical and pharmacological progress on Syringa in the recent 20 years and discusses the future research prospects to provide a reference in further promotion and application of the genus. Graphical AbstractPhytochemical and pharmacological progress on the genus Syringa

Ilexpublesnins C-M, eleven new triterpene saponins from the roots of Ilex pubescens.

Eleven new triterpene saponins, ilexpublesnins C-M (1-11), along with ten known analogues were isolated from the roots of Ilex pubescens. Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D and 2D NMR experiments. Compounds 1, 2, 10, and 11 contain a 24-aldehyde, which is rare for triterpene saponins from Ilex. These compounds were evaluated in vitro for their cytotoxic effects on human cancer cell lines HepG2, HLE, BEL7402, BEL7403, BEL7405, MCF-7, and HeLa. Among them, only compounds 6 and 19 showed cytotoxicity against the MCF-7 cell line [inhibition (%): 33.14 and 34.03, respectively].

Triterpene saponins from the roots of Ilex pubescens.

Five new triterpene saponins, Ilexpublesnins N-R (1-5), along with seven known analogs were isolated from the root of Ilex pubescens. Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D and 2D NMR experiments. Ilexpublesnin N (1) possessed a rare 20-hydroxyursolic acid scaffold from natural resource. These compounds were evaluated in vitro for their cytotoxic effects on human cancer cell lines HepG2, HLE, BEL7402, BEL7403, BEL7405, MCF-7, HeLa. Among them, only compounds 5 and 10 showed cytotoxic potentiality against BEl-7403 and HEL cell lines [inhibition (%): 35.38 and 45.12, respectively].

Usnic Acid Derivatives with Cytotoxic and Antifungal Activities from the Lichen Usnea longissima

Eight usnic acid derivatives, that is, usenamines A-F (1-6), usone (7), and isousone (8), together with the known (+)-usnic acid (9), were isolated from the lichen Usnea longissima. Their structures were elucidated using 1D and 2D NMR and MS data, and the absolute configurations of compounds 1 and 2 were defined by single-crystal X-ray diffraction analyses. Compounds 1, 2, and 8 showed inhibitory effects on the growth of human hepatoma HepG2 cells with IC50 values of 6.0-53.3 μM compared with methotrexate as the positive control, which had an IC50 value of 15.8 μM. Furthermore, 1 induced apoptosis of HepG2 cells in a dose-dependent manner at concentrations of 0-15.0 μM. The isolated compounds were also evaluated for their antifungal and antibacterial activities, with 7 and 8 exhibiting weak inhibitory effects on fungal Trichophyton rubrum spp. with an MIC value of 41.0 μM.

The genus Casearia: a phytochemical and pharmacological overview

Casearia (Salicaceae sensu lato) species have been used as folk medicines in South American and Asian countries since ancient times. Previous phytochemical screenings demonstrated that the Casearia plants mainly contain clerodane diterpenoids, sesquiterpenoids, phenylpropanoids and other constituents from different chemical classes. The pharmacological studies confirmed that the crude extracts or individual compounds from the genus showed cytotoxic, hypoglycemic, antiulcer, and anti-inflammatory activities, as well as anti-snake venom property. In this review we presented a summary of the secondary metabolites isolated from Casearia species based on the published literatures through May 2013. In addition to the traditional medicinal use of Casearia plants and their taxonomic characteristics, we focused on the known biological activities of the plants and discussed them in detail here.

Alkaloids from the tribe Bocconieae (papaveraceae): a chemical and biological review.

The Bocconieae tribe, consisting of only the genera Macleaya and Bocconia, possesses significant economic and medicinal value and plays an important role in health management for people in developing countries. During the past decades, research on metabolites and relative pharmacology, including the isolation and identification of a variety of molecules, has shed light on the tribe. Among those molecules, isoquinoline alkaloids, and their antimicrobial, antifungal, and anti-inflammatory activities are especially noteworthy. This paper presents a comprehensive compilation of current research progress, with emphasis on the alkaloids and their distribution, phytochemical and pharmacological investigation, toxicity and side effects, related chemotaxonomy and future use prospects, and hopefully provides a valuable reference as an effort to promote further exploration and application of this tribe.

Chemical constituents with NO production inhibitory and cytotoxic activities from Litsea cubeba

A bioassay-guided fractionation of the roots and stems of Litsea cubeba led to the isolation of 14 constituents, including three new compounds, cubebanone (1), N-cis-3,4-methylenedioxycinnamoyl-3-methoxytyramine (2), and 9,9′-O-di-(E)-feruloyl-(+)-secoisolariciresinol (3), together with 11 known ones (4–14). Compounds 1, 4, and 8–11 showed obvious in vitro anti-inflammatory activities against NO production in LPS-induced murine microglial (BV-2) cell line and RAW 264.7 macrophages. A cytotoxic evaluation showed that 2, 3, and 5–8 exhibited considerable inhibition against the growth of hepatocyte carcinoma (HepG2) cell line. These findings are evidence, to some extent, for the traditional medicinal application of L. cubeba, especially as folk medicine in the treatment of inflammation-related diseases.

Investigation of Two Flacourtiaceae Plants: Bennettiodendron leprosipes and Flacourtia ramontchi

Investigations of two Flacourtiaceae plants, Bennettiodendron leprosipes and Flacourtia ramontchi, resulted in the isolation and structural elucidation of six new constituents including two phenolic glycosides ( 1 and 2), one lignan ( 3), two lignan glycosides ( 4 and 5), and a monoterpene glycoside ( 6), together with 22 known compounds ( 7- 28). The structures of the new compounds were elucidated by spectroscopic analysis and chemical methods. The selected isolates 1, 2, 8- 10, 22- 26, and some phenolic glycosides 29- 42 previously isolated from another Flacourtiaceae plant, Itoa orientalis, were tested against snake venom phosphodiesterase I (PDE I) activity. The result indicated that 22, 30, 32, 34, and 40 exhibited moderate inhibitory activities against PDE I with the values ranging from 13.15 to 20.86 %, and 1, 8, 10, 25, 31, 33, 35, 38, 39, and 41 showed weak inhibitory activity.

Lignans from the stem bark of Syringa pinnatifolia.

Four new lignans, alashinols A-D (1-4), a new hydrolysis product, alashinols E (5), and seven known analogues were isolated from the stem bark of Syringa pinnatifolia Hemsl. These new lignans were characterized using 1D and 2D NMR and MS data, and their absolute configurations were determined by experimental and calculated electronic circular dichroism and X-ray diffraction analyses. Alashinol B (2) exhibited two conformers that adopted an unusual unit cell packing. Anti-inflammatory evaluation revealed that compounds 1, 4, 6, and 8 showed moderate inhibition against NO production in lipopolysaccharide-induced macrophages RAW 264.7 cells with IC50 values range from 43.3-60.9μM, and 1 decreased the TNF-α and IL-6 level in a concentration-dependent manner at 40-160μM and exhibited considerable neuroprotective effect against the glutamate-induced injury in PC12 cell line. Analogues 3 and 9 showed protective effects against oxygen glucose deprivation/reoxygenation in H9c2 cells.