11B NMR of the Morphological Evolution of Traditional Chinese Medicine Borax.

This article applies nuclear magnetic resonance technology to the study of boron-containing traditional Chinese medicine, in order to explore the morphological evolution of boron elements in traditional Chinese medicine. Borax is a traditional Chinese medicine with anti-corrosion, anti-inflammatory, antibacterial, and anticonvulsant effects. It is made by boiling, removing stones, and drying borax minerals like borate salts. This article introduces an 11B nuclear magnetic resonance method for identifying and characterizing boron-containing compounds in TCM. We applied this technology to borax aqueous solutions in different chemical environments and found that with boron mixed in the form of SP2 hybridization in equilateral triangles and SP3 hybridization in equilateral tetrahedra, the pH changes in alkaline environments significantly affected the ratio of the two. At the same time, it was found that in addition to the raw material peak, boron signals of other boron-containing compounds were also detected in 20 commercially available boron-containing TCM preparations. These new boron-containing compounds may be true pharmaceutical active ingredients, and adding them directly to the formula can improve quality and safety. This article describes the detection of 11B NMR in boron-containing traditional Chinese medicine preparations. It is simple, non-destructive, and can provide chemical fingerprint studies for boron-containing traditional Chinese medicine.

Advances in the mechanisms of polysaccharides in alleviating depression and its complications.

BACKGROUND: Depression is one of the most serious mental illnesses worldwide that endangers the health of people. The pathogenesis of depression is complex and is associated with abnormal neurotransmitter levels, activation of the hypothalamic-pituitary-adrenal (HPA) axis, inflammation, and gut flora-related disorders. However, most of the current pharmacological therapies used to manage depression are inconsistent and are associated with side effects. Owing to their low toxicity and wide availability in nature, polysaccharides are gradually attracting attention and are being discovered to exert direct or indirect antidepressant effects. PURPOSE: In this review, we have summarized the classification, dosage, and experimental models to study polysaccharides with antidepressant effects obtained from different sources. We have also reviewed the protective effects and underlying mechanisms of these polysaccharides in depression by modulating inflammation, the HPA axis, and intestinal flora. METHODS: We searched the PubMed, Web of Science, and Google scholar databases and included studies that reported the use of polysaccharides in treating depression. RESULTS: The unique benefits of natural polysaccharides as antidepressants lie in their potential to modulate inflammation, regulate the HPA axis, and regulate intestinal flora, giving full play to their antidepressant effects via multiple pathways and targets. CONCLUSION: Natural polysaccharides may be a promising resource for use as adjuvant antidepressant therapy. Our study might therefore provide evidence for the development of polysaccharide resources as antidepressants.

Advances in Chemical Composition, Extraction Techniques, Analytical Methods, and Biological Activity of Astragali Radix.

Astragali Radix (AR) is one of the well-known traditional Chinese medicines with a long history of medical use and a wide range of clinical applications. AR contains a variety of chemical constituents which can be classified into the following categories: polysaccharides, saponins, flavonoids, amino acids, and trace elements. There are several techniques to extract these constituents, of which microwave-assisted, enzymatic, aqueous, ultrasonic and reflux extraction are the most used. Several methods such as spectroscopy, capillary electrophoresis and various chromatographic methods have been developed to identify and analyze AR. Meanwhile, this paper also summarizes the biological activities of AR, such as anti-inflammatory, antioxidant, antitumor and antiviral activities. It is expected to provide theoretical support for the better development and utilization of AR.

Hypoglycemic effect of astragaloside IV via modulating gut microbiota and regulating AMPK/SIRT1 and PI3K/AKT pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: Radix Astragali, the dried root of Astragalus mongholicus Bunge, has long been used in traditional Chinese Medicine to treat diabetes. Astragaloside IV (AS-IV), one of the most active ingredients in the root, has been shown to have anti-diabetes ability; however, its underlying mechanism is still unclear. MATERIALS AND METHODS: In this study, we evaluated the hypoglycemic effect and possible mechanisms of AS-IV in diabetic mice and insulin resistance-HepG2 cells. The components of the intestinal microflora in mice with type 2 diabetes mellitus (T2DM) were determined using high-throughput 16S rRNA gene sequencing. Moreover, the molecular mechanisms of specific members of insulin signaling pathways were analyzed. RESULTS: AS-IV significantly reversed the abnormalities in blood lipids, glucose, insulin resistance, as well as oxidative stress levels in T2DM mice. Histological finding showed that AS-IV could protect the cellular architecture of the liver and pancreas. AS-IV also regulated the abundance and diversity of intestinal flora of T2DM mice in a positive direction and increased butyric acid levels. The active role of AS-IV as an anti-diabetic compound by regulating the AMPK/SIRT1 and PI3K/AKT signaling pathways was revealed using a T2DM model and verified through the intervention of inhibitors using insulin-resistance HepG2 cells. CONCLUSION: Our results suggested that AS-IV may be used as an anti-diabetic drug candidate owing to its effects of regulating gut microbiota and AMPK/SIRT1 and PI3K/AKT signaling pathways.

Anti-aging function and molecular mechanism of Radix Astragali and Radix Astragali preparata via network pharmacology and PI3K/Akt signaling pathway.

BACKGROUND: Radix Astragali (RA) consists of the dried root of Astragalus membranaceus Bunge and is one of the most frequently used dietetic Chinese herbs to treat inflammation and neurodegenerative disease among other conditions. Radix Astragali preparata (RAP) is a medicinal form of RA. RA and RAP have been used as anti-aging agent, however, the mechanisms underlying their effects are still unclear. PURPOSE: Considering the wide application of RA and RAP in clinical practice, it is necessary to identify the better product between the two and elucidate the molecular mechanism responsible for their anti-aging effects. STUDY DESIGN: In this study, network pharmacology integrated with molecular biology techniques were employed to explore the possible mechanism of RA and RAP against aging. METHODS: Aging animal models were constructed by exposure to D-galactose (D-gal), and the anti-aging effect of RA and RAP were determined based on behavior tests and histomorphological observation. Network pharmacology was performed to construct the "compound-target-pathway" network. Gene and protein expression of possible targets were validated and analyzed using qRT-PCR and Western blotting. RESULTS: Treatment by RA and RAP could alleviate the symptoms of aging such as a decrease in body weight and organ indices, behavioral impairment, increased oxidative stress, weaken histopathological evaluation. The effect of RAP was more pronounced than that of RA in preventing aging process in a mouse model. The anti-aging effect of RA and RAP is associated with the balance of oxidative stress and activation of PI3K/Akt signaling pathway. CONCLUSION: Using an integrated strategy of network pharmacology and molecular biology we attempted to elucidate the mechanisms of action of RA and RAP.

Antimicrobial mechanism of strictinin isomers extracted from the root of Rosa roxburghii Tratt (Ci Li Gen).

ETHNOPHARMACOLOGICAL RELEVANCE: The root of Rosa roxburghii Tratt (Ci Li Gen) is a kind of Chinese ethnomedicine in Gui Zhou province, used for the treatment of abdominal pain, acute bacillary dysentery, gastroenteritis and other diseases in human and livestock. AIM OF THE STUDY: The aim of this study was to isolate and identify the effective antimicrobial components from the ethyl acetate extract of the Ci Li Gen and to investigate its antimicrobial mechanism afterwards. MATERIALS AND METHODS: The effective antimicrobial components in the ethyl acetate extract from the Ci Li Gen were isolated by high-performance liquid chromatography (HPLC) and identified by high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR). The antibacterial activity was evaluated by the minimum inhibition concentration (MIC) measured by microdilution technique. The antibacterial mechanism was investigated by the time-kill curve, sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) combined with NanoLC-ESI-MS/MS, intracellular esterase activity detected by Flow cytometry, and the ultrastructural changes of the Escherichia coli ATCC 25922 observed by scanning electron microscope (SEM). RESULTS: The effective antimicrobial component (peak 4) was identified as strictinin isomers by HRMS and NMR. The MIC of strictinin isomers against E. coli was 0.125 mg/mL. With respect to the negative control group, the results of SDS-PAGE and NanoLC-ESI-MS/MS showed that the up-regulated proteins of the strictinin isomers treated group were Metal-binding protein ZinT, 30S ribosomal protein S4 and 50S ribosomal protein L4, while the down-regulated protein was hydroperoxide reductase subunit C. Moreover, in the strictinin isomers treated group, the esterase activity in the E. coli cells was reduced and the bacteria E. coli became atrophied, pitted and contorted, and the surface of E. coli was rough and blurred. CONCLUSIONS: According to the above results, the antimicrobial mechanism of strictinin isomers against E. coli were oxidative stress and protein synthesis disorder, which inhibited the activity of the enzymes required for bacterial growth and metabolism. These findings reflected the pleiotropic effects of strictinin isomers, making it a promising antimicrobial agent for pharmaceutical research.

[Effect of ferulic acid on cholesterol efflux in macrophage foam cell formation and potential mechanism].

The formation of macrophage-derived foam cells is a typical feature of atherosclerosis (AS). Reverse cholesterol efflux (RCT) is one of important factors for the formation of macrophage foam cells. In this study, macrophage form cells were induced by oxidized low density lipoprotein (ox-LDL) and then treated with different concentrations of ferulic acid, so as to observe the effect of ferulic acid on the intracellular lipid metabolism in the ox-LDL-induced macrophage foam cell formation, the cholesterol efflux and the mRNA expression and protein levels of ATP binding cassette transporter A1 (ABCA1) and ATP binding cassette transporter G1 (ABCG1) that mediate cholesterol efflux, and discuss the potential mechanism of ferulic acid in resisting AS. According to the findings, compared with the control group, the ox-LDL-treated group showed significant increase in intracellular lipid content, especially for the cholesterol content; whereas the intracellular lipid accumulation markedly decreased, after the treatment with ferulic acid. The data also demonstrated that the mRNA and protein expressions of ABCA1 and ABCG1 significantly increased after macrophage foam cells were treated with different concentrations of ferulic acid. In summary, ferulic acid may show the anti-atherosclerosis effect by increasing the surface ABCA1 and ABCG1 expressions of macrophage form cells and promoting cholesterol efflux.

Protective effects of blueberries (Vaccinium corymbosum L.) extract against cadmium-induced hepatotoxicity in mice.

The oxidative status and morphological changes of mouse liver exposed to cadmium chloride (Cd(II)) and therapeutic potential of blueberry (Vaccinium corymbosum L.) extract against Cd(II)-induced hepatic injury were investigated. A variety of parameters were evaluated, including lipid peroxidation (LPO), protein carbonyl (PCO) level, DNA fragment, as well as antioxidative defense system (i.e., superoxide dismutase (SOD), catalase (CAT), reduced glutathione (GSH)). Elemental analysis and evaluation of morphological changes and NO levels were also performed. Exposure to Cd(II) led to increased LPO and PCO as well as DNA fragment and a reduction of SOD and CAT activities, however, the content of GSH elevated probably due to biological adaptive-response. In contrast, co-treatment of anthocyanin (Ay) inhibited the increased oxidative parameters as well as restored the activities of antioxidative defense system in a dose-dependent manner. Ay administration regained these morphological changes caused by intoxication of Cd(II) to nearly normal levels. Moreover, the accumulation of Cd(II) in liver may be one of the reasons for Cd(II) toxicity and Ay can chelate with Cd(II) to reduce Cd(II) burden. The influence of Cd(II) on the Zn and Ca levels can also be adjusted by the co-administration of Ay. Exposure to Cd(II) led to an increase of NO and Ay reduced NO contents probably by directly scavenging. Potential mechanisms for the protective effect of Ay have been proposed, including its anti-oxidative and anti-inflammatory effect along with the metal-chelating capacity. These results suggest that blueberry extract may be valuable as a therapeutic agent in combating Cd(II)-induced tissue injury.

Protective effect of caffeic acid phenethyl ester against cadmium-induced renal damage in mice.

Cadmium (Cd) is classified as an environmental pollutant and human carcinogen. Caffeic acid phenethyl ester (CAPE), a biological active component of honeybee propolis extracts, has been used as a folk medicine with no harmful effects on normal cells. Here we investigated the beneficial effect of CAPE on Cd-induced renal damage in mice. Since renal damage induced by Cd (II) is related to oxidative stress, lipid peroxidation (LPO), protein carbonyl (PCO), superoxide dismutase (SOD), catalase (CAT) and glutathione (GSH) were evaluated. Moreover, the concentrations of Cd and zinc (Zn) in the kidney were analyzed. The intoxication of Cd (II) leads to the enhanced production of LPO and PCO, and the decrease of SOD activity and GSH level, probably due to the serious oxidative stress. However, the activities of CAT in the Cd (II)-induced group showed an elevated tendency, probably relating to an adaptive-response to the oxidative damage. The co-administration of CAPE can attenuate the oxidative stress caused by the intoxication of Cd and restore the altered antioxidant defense system. Based on our data, it is proposed that CAPE may involve in the protection of renal damage induced by Cd (II) owing to its antioxidant capacity and anti-inflammatory effect.