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The rhizomes of Atractylodes macrocephala are used as both a food source and traditional Chinese medicine in China. A phytochemical investigation was carried out on wild A. macrocephala grown in Qimen County in eastern China, and yielded a novel bisesquiterpenoid lactone, namely, biatractylenolide II (1), along with two known compounds, atractylenolide II (2) and taraxeryl acetate (3). The structure and relative configuration of the new compound were elucidated mainly by 1D and 2D NMR spectroscopic methods in combination with HRESIMS experiments. This paper describes the isolation and structural elucidation of the new bisesquiterpenoid lactone (1).

Contrast-induced nephropathy (CIN) is a common complication in patients with coronary arteriography, and oxidative stress is involved in the CIN pathogenesis. Sargassum fusiforme (SF) is a brown seaweed with medicinal value, and its polysaccharides have good antioxidant activity. In this study, the crude polysaccharides (cSFP-C) were extracted by cold water, precipitated by ethanol, purified by CaCl2, and detected with high contents of sulfate radical and fucose. cSFP-C is composed of glucose, glucuronic acid, xylose, rhamnose, mannose, galactose, and fucose with a molar ratio of 1.0 : 0.4 : 5.6 : 1.2 : 1.7 : 12.3 : 56.1. The cSFP-C has the typical absorption of polysaccharides. Antioxidation assays in vitro showed that cSFP-C exhibited superoxide radical scavenging activity which was better than the hot water-extracted crude polysaccharides (cSFP-H). 20 rats were divided into 4 groups (n=5): sham group; CIN group; CIN+cSFP-C group, and cSFP-C group. The CIN+cSFP-C group and cSFP-C group were pretreated intragastrically with cSFP-C at a dose of 9.45 g/kg twice daily for 5 consecutive days. Then, the CIN group and CIN+cSFP-C group were given indomethacin to develop CIN. The in vivo results showed that cSFP-C could decrease blood creatinine and urea nitrogen, inhibiting pathological injury in the renal tissues. The MDA content of renal tissues was decreased, while the activity of SOD was increased. The crude sulfated polysaccharides extracted from S. fusiforme have a renoprotective effect on oxidative stress to alleviate the kidney injury in CIN rats.

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Background: Paeonol (Pae)， the main active compound of the root of Paeonia albiflora, is efficacious in treating atherosclerosis (AS). Endothelial dysfunction is throughout the pathological progression of AS. It is expected that inhibition of Endothelial-to-mesenchymal transition (EndMT) will be a key target for AS treatment. Objective: In this study, we investigated the molecular mechanism of the regulatory effect of Pae on EndMT in human umbilical vein endothelial cells (HUVECs). Methods: Cell cytotoxicity, proliferation, and migration were detected by CCK-8, the wound healing assay, and EdU staining, respectively. The protein expressions were measured by Western blot or immunofluorescence staining. Immunofluorescence staining was performed to indicate endothelial cells undergoing EndMT in ApoE-/- mice. In vitro TGF-β1-induced EndMT assays were performed in HUVECs and the effect of Pae was explored. Results: We demonstrated that Pae could improve induced TGF-β1-EndMT in vivo and in vitro. Mechanism study revealed that Pae directly bonds to the activin-like kinase 5 (ALK5, also known as TGFβ type I receptor), inhibited downstream Smad2/3 phosphorylation, and thus alleviated EndMT. Notably, overexpression of ALK5 significantly reversed the inhibitory effect of Pae on EndMT in HUVECs. Conclusion: Our results indicate that ALK5 is a promising druggable target for AS, and pharmacological regulation of ALK5-Smad2/3 signaling pathway with small-molecule holds great potential to benefit AS patients.

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A new phenylpropanoid, (+)-methyl 3-acetoxy-3-(7-methoxy-1,3-benzodioxol-5-yl) propanoate (1), was obtained from the 95% EtOH extract of entire plant of Peperomia tetraphylla. The structure was elucidated based on the spectral analysis (IR, 1-D and 2-D NMR and HRESIMS). The absolute configuration of 1 was determined as (3R) by referring to analogous compound's optical rotation. Cytotoxicity assays showed that compound 1 had a moderate inhibitory activity against the A549 cell line, weak inhibitory activity against the Hela and the HepG2 cell lines.