Increasing minor ginsenosides contents and enhancing neuroprotective effects of total ginsenosides fermented by Lactiplantibacillus plantarum.

Minor ginsenosides have been proven to have higher pharmacological activity than the major ginsenosides. The transformation of major ginsenosides to minor ginsenosides by lactic acid bacteria was considered to be a promising method. Therefore, this study focuses on utilizing glycosidase-producing Lactiplantibacillus plantarum GLP40 to transform total ginsenosides (TG) and increase the content of minor ginsenosides, as well as investigate the neuroprotective effects of fermented total ginsenosides (FTG). After 21d fermentation, the transformation products were purified using D101 macroporous resin column chromatography, and identified by HPLC and LC-MS analyses. The neuroprotective effect of FTG was evaluated using MPTP-induced neural injury mice model. Lact. plantarum GLP40 fermentation increased the contents of minor ginsenosides in TG, such as Rg3, Rh2, CK, and Rk3. FTG showed stronger alleviation of 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine Hydrochloride (MPTP) induced memory loss and dyskinesia in mice, and inhibited tyrosine hydroxylase (TH) depletion and ionized calcium binding adapter molecule 1 (Iba-1) production than TG. Further, FTG significantly increased serum IL-10 levels and inhibited the expression of pro-inflammatory cytokines compared to TG. Moreover, FTG treatment activated the anti-apoptotic PI3K/AKT/mTOR signaling pathway and inhibited the expression of the inflammatory NF-κB/COX-2/iNOS pathway. In conclusion, Lact. plantarum GLP40 fermentation enhances the neuroprotective effects of total ginsenosides by increasing minor ginsenosides. FTG protected MPTP induced neural injury in mice by regulating inflammation and cell apoptosis signaling pathways.

Weizmannia coagulans JA845 improves atherosclerosis induced by vitamin D3 and high-fat diet in rats through modulating lipid metabolism, oxidative stress, and endothelial vascular injury.

AIMS: Probiotics have been proved to be strongly linked to the occurrence and progression of atherosclerosis. This study aimed to investigate the improved effects and mechanisms underlying a potential probiotic, Weizmannia coagulans JA845, on atherosclerosis. METHODS AND RESULTS: Male Sprague-Dawley rats supported on a high-fat diet with vitamin D3 supplementation were subjected to W. coagulans JA845 treatment. W. coagulans JA845 obviously alleviated histological abnormalities of the abdominal aorta. After 6 weeks of W. coagulans JA845 administration, levels of TG, TC, LDL, ox-LDL, ROS, and MDA in the JA845 group decreased significantly, and those of HDL, GSH-Px, and SOD were markedly elevated. Treatment with W. coagulans JA845 also inhibited the secretion of ICAM-1 and VCAM-1 and regulated the plasma NO and eNOS content. In brief, administration of W. coagulans JA845 promoted the expression of the SIRT3/SOD2/FOXO3A pathway, inhibited the lipid metabolism pathway, SREBP-1c/FAS/DGAT2, and suppressed the JNK2/P38 MAPK/VEGF pathway implicated in endothelial injury. CONCLUSIONS: These results indicated W. coagulans JA845 improved atherosclerosis by regulating lipid metabolism, antioxidative stress, and protecting against endothelial injury.

Chondroitin sulfate stimulates the secretion of H2S by Desulfovibrio to improve insulin sensitivity in NAFLD mice.

Hydrogen sulfide (H2S) is a bioactive gas regulating insulin secretion and sensitivity, produced by sulfate-reducing bacteria in the gut. The present study investigated the effect of chondroitin sulfate (CS) treatment, which indirectly increased the H2S production on nonalcoholic fatty liver disease (NAFLD). A 7-week CS supplementation had beneficial effects on body weight gain, liver function, hepatic histology, and serum lipid levels. CS could ameliorate diet-induced insulin resistance and improve insulin sensitivity via the AKT pathway, and modulate gut microbiota composition, especially increased the abundance of Desulfovibrio and elevated levels of hydrogen sulfide (H2S). Collectively, these findings suggested that CS treatment was positively correlated with Desulfovibrio in the gut, and the metabolic H2S flowed into the liver via the gut-liver axis, thereby triggering the AKT signaling pathway and improving insulin resistance. Thus, CS-induced alterations in the gut microbiota seem a promising for ameliorating NAFLD.

Synthesis of Berberine and Canagliflozin Chimera and Investigation into New Antibacterial Activity and Mechanisms.

Berberine is an isoquinoline alkaloid isolated from Chinese herbal medicines such as Coptis chinensis. It has many pharmacological actions, such as antibacterial, hypoglycemic, anti-inflammatory, and so on. However, due to the low lipophilicity of berberine, it is difficult to penetrate the bacterial cell membrane and also difficult to be absorbed orally and usually needs a relatively high dose to achieve the ideal effect. The purpose of this study is to transform the structure of berberine in order to improve the bioavailability of berberine and reduce the dosage. Moreover, we introduce a pharmacophore named Canagliflozin, a hypoglycemic drug (which was also found to have potential anti-bacterial activity) into BBR to see whether this new compound has more existed activities. We at first connected berberine with Canagliflozin, to form a new compound (BC) and see whether BC has synergic effects. We use microbroth dilution method to determine the minimum inhibitory concentration of BC, determine the bacterial growth with the enzyme labeling instrument, observe the formation of bacterial biofilm with crystal violet staining method, observe the bacterial morphology with field emission scanning electron microscope, and determine the intracellular protein with SDS-PAGE. The above indicators reflect the damage of BC to bacteria. New compound BC was successfully obtained by chemical synthesis. The minimal inhibitory concentration of compound BC on three bacteria was significantly better than that of berberine and canagliflozin alone and the combination of berberine and canagliflozin. Moreover, compound BC has obvious destructive effect on bacterial morphology and biofilm, and the compound also has destructive effect on intracellular proteins. Therefore, new compound BC has broad-spectrum antibacterial activity and the inhibitory effect of BC might play a role by destroying the integrity of biofilm and the intracellular protein of bacteria. In conclusion, we create a new molecular entity of berberine and Canagliflozin chimera and open up a new prospect for berberine derivatives in the treatment of bacterial infection.

Regulation by walnut protein hydrolysate on the components and structural degradation of photoaged skin in SD rats.

Skin photoaging induced by consecutive exposure of skin to ultraviolet radiation is primarily responsible for skin aging and preparation of food-derived ingredients with anti-aging functions has been the hot topic worldwide. Dietary consumption of food supplements has been found to modulate skin functions and can be useful in the prevention of skin aging. To evaluate the effect of walnut protein hydrolysate (WPH) on photoaged skin, Sprague-Dawley rats (SD rats) were orally administered with WPH and then were regularly exposed to ultraviolet radiation (UV-R). After a consecutive UV-R for 18 weeks, the delaying efficiency of WPH against elasticity degradation was examined and the mechanical mechanism was explored subsequently. The contents of hydroxyproline (Hyp) and hyaluronic acid (HA) in the extracellular matrix (ECM) were measured by biochemical reactions and color rendering procedures; the levels of types I and III collagen (Col I and III) and the activity of matrix metalloproteinase-1 (MMP-1) were detected by enzyme-linked immunosorbent assay (ELISA); the protein levels of elastin and fibrillin-1 were examined by western blotting. Moreover, the histological change in the skin structure was illustrated by hematoxylin & eosin (HE) and Masson staining. The results revealed that WPH evidently enhanced the elasticity of photoaged skin and stimulated the biosynthesis of ECM components Col I, Hyp and HA in the dermal layer; meanwhile WPH inhibited the MMP-1 activity, alleviated epidermal hyperplasia, and repaired the damaged skin mechanical structure in a dose-dependent manner. In particular, in comparison with the UV-R group, the WPH group in which WPH was administered at a high-dose level showed significantly improved skin appearance, ECM components and structure (P < 0.05). Taken together, the elasticity improvement caused by WPH against the skin photoaging process can be attributed to the regulation of the metabolism of the components and repair of the damaged mechanical structure of the ECM. This research proved the potential of WPH as a functional ingredient for the development of anti-photoaging foods.

Influence of ultrasound-assisted extraction on the pyrolysis characteristics and kinetic parameters of eucalyptus.

In this study, the influence of ultrasound-assisted extraction on eucalyptus samples with special focus on pyrolysis characteristics and kinetic parameters was explored. Ultrasound and Soxhlet extraction were used to pretreat samples respectively, then samples were assayed by component analysis, TG-FTIR, and kinetic analysis. Ultrasound-assisted extraction did change the physiochemical characteristics of eucalyptus samples, particularly in regards to the quantity of extractives obtained. In TG and DTG curves, ultrasound-extracted samples reflected lower residual weight ratio (17.77%) and higher maximum weight loss rate (-22.92%/min), and were accompanied by a slight shift in the weight loss rate peak to lower temperature (366°C). The volatiles produced during pyrolysis and the discrepancies of product distribution between experimental and controlled groups were explored based on TG-FTIR spectra. According to kinetic analysis results, ultrasound-treated samples showed higher activation energy at the primary portion of thermal degradation with an average of 206.09kJ/mol.

Soulieoside O, a new cyclolanostane triterpenoid glycoside from Souliea vaginata.

A new cyclolanostane triterpenoid glycoside, soulieoside O (1), together with 25-O-acetylcimigenol-3-O-ß-d-xylopyranoside (2) and cimigenol-3-O-ß-d-xylopyranoside (3), was isolated from the rhizomes of Souliea vaginata. Their structures were characterized by spectroscopic analysis and chemical methods. The new compound showed moderate inhibitory activity against three human cancer cell lines with IC50 values of 9.3-22.5 µM.

A new cycloartane triterpenoid glycoside from Souliea vaginata.

One new cycloartane triterpenoid glycoside, soulieoside Q (1), together with four known compounds (2-5) were isolated from the ethanolic extract of the rhizomes of Souliea vaginata Maxim. The structure of the new compound was determined by extensive spectroscopic analysis including 1D and 2D NMR and HRESIMS, as well as chemical methods. Compound 1 was evaluated for its cytotoxic activities against HepG2 and A549 cancer cell lines.

Transdermal Permeation and Anti-Inflammation Activities of Novel Sinomenine Derivatives.

Sinomenine is extracted from Sinomenii caulis (a traditional Chinese medicine), and it is used as the active ingredient in rheumatic arthritis treatments. It has been used in clinical applications for decades. However, there are some disadvantages, including low activity in transdermal permeation and a high dosage being clinically required. To overcome these defects, sinomenine was used as a primer, and structural modification was performed. In our study, eight new compounds were screened out by transdermal permeation in vitro and anti-inflammatory response in vitro and in vivo. Compound 1a exhibited the most potent transdermal permeation and anti-inflammatory activity. Based on these results, further development of this compound may be warranted.