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Three new pregnane alkaloids, named terminamines H–J (1–3), together with two known alkaloids (4 and 5), were isolated from the ethanol extract of Pachysandra terminalis. The structures of isolated compounds were elucidated by spectroscopic methods, including 1H and 13C NMR, 2D NMR, and HR-ESI-MS. Compounds 1, 4, and 5 revealed significant anti-metastasis activities. In addition, compound 1 inhibited the expression of p-PKCζ in MDA-MB-231 cells, and compound 4 inhibited the expressions of p-PKCζ in MDA-MB-231 and A549 cells. [ABSTRACT FROM AUTHOR]

Preclinical Research The preparation of novel E ‐ salignone derivatives and their biological evaluation as potential antimetastatic agents is described. The E ‐ salignone amide derivatives were prepared from epiandrosterone and androsterone, and characterized by analytical 1H NMR, 13C NMR, and mass spectrometry. The derivatives were evaluated for antimetastatic activity in MDA ‐ MB ‐ 231 cells by using a transwell assay. Comparing with the positive control, LY294002, compounds 19b, 19d, and 19e exhibited significant inhibitory effects on the EGF ‐ induced invasion of MB ‐ MDA ‐ 231 cells. Moreover, compound 19b also had antimigration effects in wound ‐ healing assay. Compound 19b may represent a novel antimetastatic agent for treating breast cancer. [ABSTRACT FROM AUTHOR]

Abstract: A series of new tiliroside derivatives were synthesized and characterized by analytical 1H NMR, 13C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cells. Compounds 3c, 3d, and 3i–l caused significant enhancements in glucose consumption by insulin-resistant HepG2 cells compared with control cells and cells that were exposed to metformin (an anti-diabetic drug). Moreover, compound 3l significantly activated adenosine 5′-monophosphate-activated protein kinase activity and reduced acetyl-CoA carboxylase activity. Thus, the tiliroside derivative 3l offers potential to be developed as a new approach for treating type II diabetes. [Copyright &y& Elsevier]

Fraxinifolines A-F (1 – 6), six new B- seco limonoids, together with four known A,D-di- seco ones, were isolated from the twigs with leaves of Tetradium fraxinifolium. Their structures with absolute configurations were elucidated on the basis of analysis of MS, NMR, single-crystal X-ray diffraction and biogenetic pathway. An anti-inflammatory bioassay in vitro showed limonoids 1 – 3 had significant immunosuppressive effect against the production of pro-inflammatory cytokines (IL-1 β and/or TNF-α) in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. [Display omitted] • Ten limonoids were isolated from the twigs with leaves of Tetradium fraxinifolium. • Fraxinifolines A-F are the first examples of B- seco limonoids from Rutaceae plant. • Fraxinifolines A-D are unusal 7,8- seco -7,8-epoxide type limonoids. • Fraxinifolines A, B and C had significant immunosuppressive effect. [ABSTRACT FROM AUTHOR]

A pair of new enantiomeric indolopyridoquinazoline-type alkaloids, (+)-1,7 S ,8 R - and (−)-1,7 R ,8 S -trihydroxyrutaecarpine (3a and 3b), and a new limonoid-tyrosamine hybrid, austrosinin (8), along with six known alkaloids and limonoids, were isolated from the stems with leaves of Tetradium austrosinense. Their structures were elucidated on the basis of analysis of MS, NMR, ECD and time-dependent density functional theory-based electronic circular dichroism (TDDFT-ECD) calculations, as well as proposed biosynthetic pathway. An anti-inflammatory bioassay in vitro showed 8 had significant immunosuppressive effect against the production of pro-inflammatory cytokine TNF-α in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. [Display omitted] • Six alkaloids and three limonoids were isolated from Tetradium austrosinense. • A pair of enantiomeric indolopyridoquinazoline-type alkaloids were isolated and resolved. • Austrosinin is the first example of limonoid-tyrosamine hybrid from the nature source. • Austrosinin displayed significant immunosuppressive effect. [ABSTRACT FROM AUTHOR]

Whitmania pigra Whitman (Whitmania pigra , WP), firstly recorded in the Shennong's Herbal Classic and officially listed in the Chinese Pharmacopoeia, is a well-used cardiovascular protective traditional Chinese medicine derived from leeches. Traditional Chinese physicians prefer to prescribe the dried whole body of leech processed under high temperatures. It has been reported that dried WP remains clinically effective. However, the therapeutic mechanism has yet not be clearly elucidated. This study was designed to investigate the protective activity of the extract of WP in a high-molecular-weight dextran-induced blood hyperviscosity rat model, and to explore the role of WP in improving blood hyperviscosity related metabolic disorders and to clarify the possible mechanism of metabolic regulation. The hemorheological parameters were measured with an automated blood rheology analyzer. Hematoxylin-eosin staining was used to observe the pathological changes in aortic tissues samples. Further, a liquid chromatography-mass-spectrometry (LC-MS)-based untargeted metabolomics approach was applied to characterize the metabolic alterations. WP has evident attenuating effects on blood hyperviscosity and related metabolic disorders, and the influences are distinct from those of aspirin. The results showed that WP had good effects in reducing blood viscosity and ameliorating histopathological changes in the thoracic aorta in a high molecular weight dextran-induced blood hyperviscosity rat model. The middle dose (2.5 g raw material/kg body weight) of WP exhibited effects equivalent to aspirin (100 mg/kg) on hemorheological and histopathological parameters (P > 0.05). However, when using metabolomics profiling, we found that WP could significantly improve blood hyperviscosity-related metabolic disorders and restore metabolites to normal levels; while aspirin showed little effect. With principal component analysis and orthogonal partial least-squares discriminant analysis, WP regulated many more endogenous metabolites than aspirin. With pathway enrichment analysis, the differential endogenous metabolites were involved in cysteine and methionine metabolism, TCA cycle, arachidonic acid metabolism, etc., highlighting the metabolic reprogramming potential of WP against blood hyperviscosity-induced metabolic disorders. The study suggest that WP has a more potent effect, but a different mechanism, than aspirin in improving either blood hyperviscosity or related metabolic disorders associated with cardio- and cerebrovascular diseases. Image 1 [ABSTRACT FROM AUTHOR]