Chaoying Ma

Natural fatty acid synthase inhibitors as potent therapeutic agents for cancers: A review

Abstract Context Fatty acid synthase (FAS) is the only mammalian enzyme to catalyse the synthesis of fatty acid. The expression level of FAS is related to cancer progression, aggressiveness and metastasis. In recent years, research on natural FAS inhibitors with significant bioactivities and low side effects has increasingly become a new trend. Herein, we present recent research progress on natural fatty acid synthase inhibitors as potent therapeutic agents. Objective This paper is a mini overview of the typical natural FAS inhibitors and their possible mechanism of action in the past 10 years (2004–2014). Method The information was collected and compiled through major databases including Web of Science, PubMed, and CNKI. Results Many natural products induce cancer cells apoptosis by inhibiting FAS expression, with fewer side effects than synthetic inhibitors. Conclusion Natural FAS inhibitors are widely distributed in plants (especially in herbs and foods). Some natural products (mainly phenolics) possessing potent biological activities and stable structures are available as lead compounds to synthesise promising FAS inhibitors.

Essential oil composition and antibacterial activity of Lindera nacusua (D. Don) Merr.

Abstract This study represents the first report on the chemical composition and biological activity of the essential oils from the leaves of Lindera nacusua (D. Don) Merr. Twenty-two compounds were identified and quantified, and the major components of the oil were Caryophyllene oxide (8.79%), Hexahydrofarnesyl acetone (6.83%), β-Selinene (5.02%), Neophytadiene (4.53%), Palmitic acid (4.42%), Phytol (4.36%), α-Copaene (3.89%), 4a,5,8,8a-β-Tetrahydro-2,4,5-trimethyl-1,4-naphthalindione (3.83%), α-Cadinol (3.17%), Bulnesol (2.65%) and 1,4-Dimethyl-7-(1-methylethyl) azulene (2.38%). The in vitro antibacterial activities of the essential oils were evaluated by the disc diffusion method. The inhibition zones against Staphylococcus aureus and Candida albicans were 23.7 and 23 mm. So the essential oil of L. nacusua showed potent antibacterial activity and potential high selectivity against S. aureus and C. albicans. Graphical abstract

Antitumor constituents from Anthriscus sylvestris (L.) Hoffm.

Bioassay-guided chemical investigation of the roots of Anthriscus sylvestris (L.) Hoffm. resulted in the isolation of nine compounds, whose structures were determined by spectroscopic methods. Compound 1 was isolated from this plant for the first time and compounds 3 and 9 were first found from this genus. Different polar fractions of A. sylvestris extract and compounds 1, 6-8 and 9 were evaluated for antitumor activities against HepG2 (human hepatocellular carcinoma), MG-63 (human osteosarcoma cells), B16 (melanoma cells) and HeLa (human cervical carcinoma cells) lines by the MTT method. The petroleum ether fraction of A. sylvestris extract exhibited excellent inhibitory activity with an IC50 value of 18.3 μg/ml. Among the isolates from the petroleum ether fraction, compound 7 showed significant inhibition against the growth of the four tumor cells with IC50 values ranging from 12.2-43.3 μg/ml.

Flavones and lignans from the stems of Wikstroemia scytophylla diels

Background: The genus Wikstroemia has about 70 species, but only a limited number of species have been studied chemically. Wikstroemia indica has long been used as a traditional crude drug in China. However, there is no report about the bioactivity of Wikstroemia scytophylla. Objective: This paper reports the chemical investigation and biological evaluation of the W. scytophylla. Materials and Methods: The EtOAc extraction of W. scytophylla was isolated using chromatographic methods, and the compounds were analyzed by spectroscopic methods. The in vitro antitumor activities against five human cancer cell lines were performed according to the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method. Results: The chemical investigation of the stems of W. scytophylla resulted in the isolation of 12 compounds mainly including one biflavone (1), five flavones (2-6) compounds, and six lignans (7-12), in which compound 8 was a new natural product. Compounds 1 and 7-12 were evaluated for their antitumor activities while these compounds showed weak cytotoxicity with the half maximal inhibitory (IC50) values more than 40 μM. Conclusion: All of these compounds were isolated from this plant for the first time, and compounds 2-12 were first reported from genus Wikstroemia, in which compound 8 was a new natural product. Compounds 1 and 7-12 exhibited weak antitumor activities (IC50>40 μM). The chemotaxonomic significance of all the isolations was summarized. Abbreviations used: MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; IC50: Half maximal inhibitory; HL-60: Human leukemia cell line; SMMC-7721: Human hepatocellular carcinoma cell line; A549: Human lung tumor cell line; MCF-7: Human breast cancer cell line; SW480: Human colon cancer cell line; MS: Mass spectrometry; NMR: Nuclear Magnetic Resonance.

A new phenolic glycoside from Lindera nacusua

Abstract The present study was designed to investigate the chemical constituents of Lindera nacusua and their antitumor activities. A new phenolic glycoside, namely 1-O-3-hydroxyphenyl-5-methoxyphenol-(6′-O-vanilloyl)-β-d-glucopyranoside (1), together with five known phenolic glycosides (2–6), two anthraquinones (7, 8) and two γ-butanolides (9, 10), was isolated, and its structure was elucidated by spectroscopic and chemical methods. Compounds 1–10 were screened for their in vitro cytotoxicities against HL-60, SMMC-7721, A549, MCF-3 and SW480 cell lines by the MTS method. Compounds 9 and 10 showed moderate cytotoxicities with IC50 values ranging from 17.40 to 35.21 μM.

Anxiolytic potency of iridoid fraction extracted from Valeriana jatamansi Jones and its mechanism: a preliminary study

Abstract Valeriana jatamansi Jones (V. jatamansi) has been widely used for treating anxiety and its mechanism involves many aspects including GABA level. This study aimed to evaluate the anxiolytic potency of an iridoid fraction extracted from the radix and rhizomes of V. jatamansi. The iridoid fraction was extracted by using D101 resin; its major components were analysed preliminarily by thin layer chromatography, ultraviolet spectrophotometry and high-performance liquid chromatography; and its anxiolytic effects at 6 mg/kg (low-dose), 9 mg/kg (medium-dose) and 12 mg/kg (high-dose) were evaluated using the elevated plus maze test, the light–dark box test, the Vogel’s drinking conflict test, and the open field drink test. Its action mechanism was investigated using the ELISA. This study provided evidence on the anxiolytic potency of the iridoid fraction from V. jatamansi and revealed its action mechanism of regulating the GABA level.