Hedansanqi Tiaozhi Tang extract (HTT) consists of Notoginseng, Danshen, Hawthorn and Lotus leaf from traditional Chinese medicine, which has significant therapeutic effects on hyperlipidemia in patients with non-alcoholic fatty liver disease (NAFLD). This study sought to evaluate the pharmacological effects and molecular mechanism of HTT for the treatment of hyperlipidemia in adipocytes and animal model with NAFLD. Quantitative phytochemical analysis of HTT was performed by HPLC. Antioxidant activity and the adipogenesis in 3T3-L1 cells were assessed. In the rat model induced by high-fat diet, lipid-related and antioxidant markers in serum and liver were detected. Moreover, the organ weights, non-alcoholic steatohepatitis (NASH) score and the levels of Nrf2 and HO-1 in liver sections were analyzed by tissue pathological techniques. 8 constituents were identified in HTT including saponins, flavonoids, alkaloids and others. HTT treatment enhanced antioxidant activities and promoted lipolysis in 3T3-L1 adipocytes. We also found that HTT inhibited weight gain, reduced the lipid profiles and improved the liver function and pathological characteristics induced by high-fat diet. In addition, HTT activated the Nrf2/HO-1 antioxidant pathway in the liver. HTT has protective effect against NAFLD in vitro and in vivo by activating the Nrf2/HO-1 antioxidant pathway.
Two new p-hydroxybenzoic acid glycosides, namely p-hydroxybenzoic acid-4-O-α-d-manopyranosyl-(1 → 3)-α-l-rhamnopyranoside (compound 1) and 4-O-α-l-rhamnopyran-osyl-(1 → 6)-α-d-manopyranosyl-(1 → 3)-α-l-rhamnopyranoside (compound 2), and seven known compounds, compound 3, 6, 7 (acid components), compound 8, 9 (flavonoids), compound 4 (a coumarin) and compound 5 (an alkaloid), were isolated from the 70% ethanol aqueous extract of the aerial parts of Melilotus officinalis (Linn.) Pall. The structures of all compounds were elucidated by use of extensive spectroscopic methods Infrared Spectroscopy (IR), High resolution electrospray ionization mass spectrometry (HR-ESI-MS), and 1H and 13C-NMR). Sugar residues obtained after acid hydrolysis were identified by high-performance liquid chromatography (HPLC). The antioxidant activity of all the compounds was evaluated by 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) and 1,1-diphenyl-2-picrylhydrazyl (DPPH). The anti-inflammatory effects of the compounds were also evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. All compounds were shown to inhibit LPS-induced nitric oxide (NO) and prostaglandin E 2 (PGE 2) production by suppressing the expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively, in LPS-stimulated RAW 264.7 cells. The inhibitory effect of all the compounds on MCF-7 cells was determined by Cell Counting Kit-8 (CCK-8) method. The results showed that compounds 1, 2, 7, 8, 9 exhibited better antioxidant activity compared to the other compounds. compounds 1–9 had different inhibitory effects on the release of NO, TNF-α and IL-6 in LPS-stimulated RAW264.7 cells by LPS, of which compound 7 was the most effective against inflammatory factors. compounds 1 and 2 have better antitumor activity compared to other compounds. Further research to elucidate the chemical composition and pharmacological effects of Melilotus officinalis (Linn.) Pall is of major importance towards the development and foundation of clinical application of the species.
Ziziphus jujuba var. spinosa (Bunge) Hu ex H.F.Chow [Rhamnaceae; Ziziphi Spinosae Semen (ZSS)] has attracted extensive attention as the first choice of traditional Chinese medicine in the treatment of insomnia. However, recent studies on the sleep-improving mechanism of ZSS have mainly focused on the role of single components. Thus, to further reveal the potential mechanism of ZSS, an assessment of its multiple constituents is necessary. In this study, ZSS extract (ZSSE) was obtained from ZSS via detailed modern extraction, separation, and purification technologies. The chemical constituents of ZSSE were analyzed by high-performance liquid chromatography–mass spectrometry (HPLC–MS). For in vivo experiments, a rat model of insomnia induced by p-chlorophenylalanine (PCPA) was established to investigate the potential effect and corresponding mechanism of ZSSE on improving sleep. Hematoxylin–eosin staining (HE) results revealed that the drug group showed prominent advantages over the model group in improving sleep. Moreover, the brain levels of γ-aminobutyric acid (GABA), glutamic acid (Glu), 5-hydroxytryptamine (5-HT), and dopamine (DA) were monitored via enzyme-linked immunosorbent assay (ELISA) to further study the sleep-improving mechanism of ZSSE. We found that sleep was effectively improved via upregulation of GABA and 5-HT and downregulation of Glu and DA. In addition, molecular mechanisms of ZSSE in improving sleep were studied by immunohistochemical analysis. The results showed that sleep was improved by regulating the expression levels of GABA receptor subunit alpha-1 (GABAARα1) and GABA acid receptor subunit gamma-2 (GABAARγ2) receptors in the hypothalamus and hippocampus tissue sections. Therefore, this work not only identified the active ingredients of ZSSE but also revealed the potential pharmacological mechanism of ZSSE for improving sleep, which may greatly stimulate the prospective development and application of ZSSE.
Whitening cosmetics have a large market scale and broad development prospects, while whitening products of traditional Chinese medicine have always been a research hotspot. In this study, the whitening active extract of Platycodon grandiflorum (PGE) was isolated and purified for the first time, and the whitening activity mechanism and chemical composition of PGE were elucidated. A total of 45 components were identified via high-performance liquid chromatography-mass spectrometry (HPLC-MS) analysis, including arbutin, syringin, chlorogenic acid, platycoside E, platycodin D3, baicalin, platycodin D, and luteolin. The scavenging rates of PGE toward DPPH and ABTS free radicals were 98.03% and 84.30%, respectively. The inhibition rate of PGE toward tyrosinase was up to 97.71%. The PGE had significant anti-inflammatory effects on RAW264.7 macrophages stimulated by lipopolysaccharide (LPS) and had significant inhibition effects on tyrosinase and melanin generation of B16F10 cells stimulated by α-MSH. The results showed that the PGE achieved a synergistic whitening effect by inhibiting the activation of oxygen free radicals on tyrosinase, antioxidation, anti-inflammatory effect, enzyme activity, and melanin generation. As a whitening agent extracted from natural plants, PGE has great potential in the research and development of plant whitening cosmetics, which lays a foundation for the further development and utilization of Platycodon grandiflorum resources and also provides a theoretical basis for the development of green and organic whitening cosmetics.
Semen Ziziphi Spinosae (Ziziphus jujuba Mill. var. spinosa (Bunge) Hu ex H. F. Chou) is a functional food and a traditional Chinese medicine (TCM) in China. Herein, Semen Ziziphi Spinosae protein (SZSP) was prepared by an alkaline extraction and acid precipitation method, of which the structural, physicochemical, functional and emulsion properties were investigated. Results showed that SZSP contained an ideal amino acid composition. The structural properties of the proteins were characterized using Fourier transform infrared spectroscopy (FTIR), relative fluorescence and circular dichroism (CD) spectroscopy analysis. The electrophoresis profiles showed that the main molecular weight of the protein components was about 10–40 kDa and contained some glycoproteins. Differential scanning calorimetry analysis indicated that the denaturation temperature of SZSP was 110.5 °C. The functional properties showed that SZSP has good water and oil absorption capacity, high emulsifying ability and foaming stability. The overall results suggest that SZSP is a promising protein source for the functional food industry.