Purified Phlorizin from DocynIa Indica (Wall.) Decne by HSCCC, Compared with Whole Extract, Phlorizin and Non-Phlorizin Fragment Ameliorate Obesity, Insulin Resistance, and Improves Intestinal Barrier Function in High-Fat-Diet-Fed Mice

Abstract

Natural products generally contain complex and multiple bioactive compounds that are responsible for the effects on health through complicated synergistic and/or suppressive actions. As an important raw material of local ethnic minority tea, ethnomedicines and food supplements in southwestern areas of China, Docynia indica (Wall.) Decne (DID) mainly consists of phlorizin (PHZ), which is the main active component. In this study, the holistic activities and the interactions of components of PHZ, non-phlorizin (NP) in the DID extract (DIDE) were evaluated. A rapid and effective high-speed counter-current chromatography (HSCCC) was performed to knock out PHZ from DIDE and the purity of PHZ was 96.01% determined by HPLC, with a recovery rate of 96.76%. After 13 weeks of treatment course in a high-fat diet (HFD)-induced obese mice model, the results revealed that the DIDE and PHZ significantly decreased weight gain, blood lipid levels, hyperplasia of adipocytes and alleviated inflammation (p < 0.05). Both DIDE and PHZ improves insulin resistance (p < 0.001). Meanwhile, the intestinal barrier function was improved compared to HFD group, through the determination of serum lipopolysaccharides (LPS), glucagon-likepeptide-2 (GLP-2) and hematoxylin-eosin staining of jejunum. Interestingly, after NP treatment, the metabolic syndrome of the HFD-induced obesity appeared to have a similar improvement. All the experiments showed that there is a synergistic weakening phenomenon when PHZ and NP interact with each other in the mixed state. In conclusion, for the PHZ and NP showing a good effect on anti-obesity, anti-inflammation, and intestinal barrier function, DIDE could be a good source of functional food to prevent obesity.

Phlorizin ameliorates obesity-associated endotoxemia and insulin resistance in high-fat diet-fed mice by targeting the gut microbiota and intestinal barrier integrity

“…Thus, both the gut microbiota and the physical barrier of the gastrointestinal tract are considered as therapeutic targets for MDs. [26][27][28][29][30][31] The role of PHZ as a competitive inhibitor of SGLT2 might potentially help alleviate hyperglycemia and thus improve MDs-associated conditions; however, providing the extremely low bioavailability of PHZ, it is hard to completely explain the therapeutic efficacy. Based on the facts that a large portion of PHZ would enter the gut after ingestion and that the gut microbiota could play a major role in protecting the gut barrier integrity and inhibiting LPS leakage into the systemic circulation, this study hypothesized that the gut microbiota was an alternative target for PHZ to alleviate MDs-associated conditions.…”

The complete chloroplast genome sequence of Docynia indica (Wall.) Decne

“…2003 ; Zhang et al. 2018 b). The fruits contain high levels of biologically active components including anti-oxidants, tannins and flavonoids, which were used as natural remedy to treat digestive problems and infectious diseases (Tiep et al.…”

“…Decne., also called Duo-Yi in China, is an evergreen wild fruit tree species belonging to the Rosaceae family, which wildly distributed from East Asia to China (Rymbai et al 2016). Its leaves are rich in polyphenols and flavonoids, extracts from the leaves have several pharmacological actions such as anti-obesity (Nguyen et al 2011), antifungal (Zhang et al 2018a), antioxidant (Sharma et al 2015), which were widely used as a medicine for the healing of empyrosis, fracture and fever by the local ethnic minorities in China (Lin et al 2003;Zhang et al 2018b). The fruits contain high levels of biologically active components including anti-oxidants, tannins and flavonoids, which were used as natural remedy to treat digestive problems and infectious diseases (Tiep et al 2018).…”

Preparation of Herbal Formulation for Inflammatory Bowel Disease Based on In Vitro Screening and In Vivo Evaluation in a Mouse Model of Experimental Colitis

“…Medicinal plants generally contain multiple bioactive compounds that are responsible for the beneficial effects on human diseases through synergistic actions [14]. Synergistic anti-inflammatory effects of the compound combination of the herbal formula GuGe FengTong, prepared from three herbs, Spatholobus suberectus (Leguminosae), Dioscorea nipponica (Dioscoreaceae), and Zingiber officinale (Zingiberaceae), were recently reported [15].…”