Journal of Holistic Integrative Pharmacy最新文献

Objective

To study the chemical constituents of the roots of Ephedra sinica Stapf.

Methods

The roots of E. sinica were extracted with 90% ethanol and isolated and purified by column chromatography on silica gel, Sephadex LH 20, and semipreparative RP-HPLC. All the compounds were identified based on spectral analysis (including MS, ¹H-NMR and ¹³C-NMR, and 2D NMR) and compared with the reported literature. Their cytotoxicities were evaluated against three human cancer cell lines.

Results

Two compounds were isolated from the roots of E. sinica and identified as (E)-eicosyl 3,4-dihydroxy-5-methoxycinnamate (1) and (E)-hexadecyl-ferulate (2).

Conclusion

Compound 1 was a new phenol named ephedrate A, and compound 2 was newly isolated from this plant. These two compounds showed no obvious cytotoxic activity, and their medicinal activities need to be studied further.

Objective

To obtain structurally novel and bioactive secondary metabolites from the marine fungus Xylariaceae sp. SCSIO41212.

Methods

Compounds were purified by comprehensive chromatography methods of silica gel column, Sephadex LH-20, Ostade-cylsilane (ODS) and semi-preparative HPLC, and their structures were elucidated by means of physical and chemical properties, magnefic resonance imaging, spectroscopic analysis, and comparison with the reported literatures.

Results

Chemical investigation of the fungus Xylariaceae sp. SCSIO41212 has led to the isolation of two new compounds, xylaolide B (1) and xylaolide C (2), together with nine known compounds (3–11). Their structures were determined on the basis of detailed analysis of the 1D and 2D NMR as well as MS data. Compounds 1–6 were evaluated for their antiviral, and cytotoxic activities, respectively. Compound 1 showed weak cytotoxicities against K562, MCF-7 and SGC7901 respectively.

Conclusion

This study enriches the diversity of secondary metabolites of marine-derived fungi and provides an important reference for novel promising drug leads research.

Objective

To explore the secondary metabolites of the higher fungus Stereum hirsutum.

Methods

The structures of these compounds were elucidated by extensive spectroscopic analyses and NMR calculations.

Results

Three new bisabolane sesquiterpenoids, sterene acids A–C (1–3), and one new phenolic derivative, sterephenol A (4), were isolated from the higher fungus S. hirsutum.

Conclusion

Compound 1 is the first example of bisabolane sesquiterpenoid bearing an allene group. It is also the first time to discover bisabolane sesquiterpenoids from the fungus S. hirsutum.

Developing an efficient biosensor with high sensitivity and selectivity is significant for the early diagnosis of cancers to improve the survival rate of cancer patients. Metal-organic framework (MOF)-based electrochemical aptamer biosensors have attracted wide attention in detecting tumor markers. MOF, as a porous crystal material, consists of metal ions and organic ligands with the unique advantages of large surface area, tunable pore scales, simple synthetic method, and good adsorption capabilities. Because of its weak specificity, MOF is often combined with aptamers to meet the selectivity of electrochemical sensors. Aptamer is a segment of oligonucleotide and is often used to capture tumor markers because of its good designability and excellent specificity. Considering the merits of MOF and aptamer, electrochemical aptamer biosensor has been widely applied to the detection of cancer tumor markers with low concentration under complex physiological environment. This review covers the remarkable developments in MOF-based electrochemical aptasensors for the detection of tumor markers, including monometallic MOFs, bimetallic organic frameworks and calcined MOFs. And their construction strategy of electrochemical sensor was analyzed for meeting the requirements of selectivity and sensitivity. Finally, we also discussed the future perspectives for development and application of electrochemical aptasensors.

Objective

The gut-brain axis has been implicated in the complex pathogenesis of Alzheimer's disease (AD), but the mechanism of action is unclear. This study was performed to clarify the link between the gut microbiota and AD.

Methods

Gut microbiota structure, long-term potentiation (LTP), inflammation levels, AD biomarkers, and metabolomics were monitored. Moreover, the regulatory action of bacterial metabolites on tau protein phosphorylation was evaluated.

Results

Early-life exposure to APP/PS1 mice showed that gut bacteria from donated mice altered the gut microbiota structure in newborn mice, LTP in hippocampal slices was significantly shortened, inflammatory marker levels increased, AD biomarkers were upregulated, and tau protein phosphorylation was significantly higher at multiple sites. Special bacteria, such as Akkermansia, Lactobacillus, and Klebsiella, increased in AD patient samples, which might induce and/or accelerate disease processes.

Conclusion

These results implied that the gut bacteria in AD could change the gut microbiota structure, induce metabolism disorders, induce inflammation and autophagy dysfunction (thus leading to accelerated tau protein phosphorylation), reduce LTP in AD cohoused mouse hippocampus, and increase neuroinflammation. Long-term clinical monitoring is needed to design dietary and nutritional interventions for AD based on the gut microbiota and mycobiota.

The effects of Xiao-Ban-Xia-Tang (XBXT) formula on cisplatin and 1-PBG induced emesis and gut microbiota were studied in this experiment. Cisplatin and 1-PBG induced pica rat models were established, the amount of kaolin intake was observed, and the effects of XBXT and ondansetron on the gut microbiota were studied by 16S rDNA gene analysis. The results showed that XBXT and ondansetron could ameliorate the acute and delayed pica induced by cisplatin and 1-PBG. XBXT decreased Firmicutes in the cisplatin treated rats. Ondansetron decreased the alpha diversity of the gut microbiota, and it decreased Firmicutes and increased Bacteroidetes in the cisplatin and 1-PBG treated rats. XBXT was as effective as ondansetron in the treatment of pica, while ondansetron was more likely to cause gut microbiota dysbiosis than XBXT. Our study provided new avenues for the roles and mechanisms of XBXT on the prevention and treatment of CINV.

Objective

This study focused on designing and subsequently screening novel phenanthroimidazole derivatives with activity as potential inhibitors of hepatocellular carcinoma.

Methods

We synthesized a series of phenanthroimidazole derivatives and their molecular structures were characterized by ESI-MS and ¹H NMR. The anti-tumor activity was evaluated using the MTT assay. The potential mechanism of anti-tumor activity based on DNA-damage-mediated apoptosis was analyzed by flow cytometry, immunofluorescence, and comet assay. Additionally, the anti-angiogenic activity was assessed by transgenic zebrafish. Furthermore, in vivo biodistribution of the compound was studied using a nude mice xenograft model.

Results

The screening results for anti-tumor activity revealed that the compounds, especially 2, exhibited promising restrain activity against the growth of HepG2 cells with an IC₅₀ value of 0.68 µM. Further studies showed that 2 can accumulate in the mitochondria of HepG2 cells, decreased the mitochondrial membrane potential, induce DNA damage and apoptosis of cells. Moreover, it was also discovered that 2 can inhibit the formation of neovascularization, which was confirmed by the decrease in ISV angiogenesis of zebrafish after being incubated with 2, as well as the decrease in the number and length of tubes formed in HUVECs cells. Besides, in vivo distribution and metabolism studies show that 2 is rapidly distributed in the whole body and accumulated in the tumor tissue of BALB/c mice.

Conclusion

Taken together, this type of phenanthroimidazole derivatives, especially 2, will be developed to be potent inhibitors against the growth of HepG2 cells through anti-angiogenesis and apoptosis based on mitochondrial-dependent pathways in the near future.

Objective

Black sesame pigment (BSP) was a natural pigment with a variety of bioactivities, including antioxidant, antimutagenic, and neuroprotective properties. However, the high molecular weight and heterogeneous structure of BSP necessitate further investigation. The study's goal is to develop a theoretical foundation for water-soluble BSP as a potential functional food supplement.

Methods

First, crude black sesame pigment (rBSP) was extracted from black sesame by sodium hydroxide-hydrochloric acid method, furtherly two water-soluble components (BSP-1, BSP-2) were prepared from rBSP by the separation methods of macroporous adsorption resin. In the dynamic test, 40% ethanol (v/v) was applied to five different macroporous resins (AB-8, D101, XAD-1600, D201, and HPD-600) for static adsorption/desorption of rBSP separation. The structure of the components was investigated using ultraviolet (UV) spectroscopy, Fourier-transform infrared spectroscopy (FT-IR), and ¹H and ¹³C nuclear magnetic resonance (NMR). Oxygen radical absorption capacity (ORAC) and cellular antioxidation activities (CAA) were used to assess the antioxidant activity of the components.

Results

A macroporous polymeric adsorbent method was developed to obtain water-soluble fractions of rBSP. For the static adsorption/desorption characteristics of rBSP, five types of macroporous resins (AB-8, D101, XAD-1600, D201, and HPD-600) were evaluated, and two fractions (BSP-1 and BSP-2) were isolated from rBSP by 40% ethanol (v/v) on D101 resin in the dynamic test. Furthermore, ultraviolet-visible spectroscopy, Fourier-transform infrared spectroscopy, ¹H and ¹³C NMR revealed that BSP-1 and BSP-2 were macromolecule conjugate structures, with BSP-2 having higher aromaticity than BSP-1. ORAC and CAA results showed that rBSP, BSP-1, and BSP-2 had comparable antioxidant activities. The BSP-2 exhibited the highest CAA value of 1121.92 ± 54.45 µmol QE/100 g, DW.

Conclusion

This study suggests that water-soluble BSP fractions could be used as functional food supplements that benefit human health.

Objective

To verify the antioxidant, whitening and anti-inflammatory effects of “Four white” extracts in cosmetic applications.

Methods

The extracts of the Chinese herbal medicines “Four white” (Silkworm Larva, Japanese Ampelopsis root, Largehead Atractylodes rhizome. White peony root) were prepared by an alcoholic extraction method. The safety and irritation of the extracts were assessed by the erythrocyte hemolysis test and MTT. The antioxidant ability of the extracts was determined by measuring their capabilities to scavenge hydroxyl and DPPH radicals, reduce iron ions and cellular antioxidant assays. The whitening capability was determined by the ability of tyrosinase inhibition. Its anti-inflammatory capacity was determined by measuring the inhibiting rates against hyaluronidase and lipopolysaccharide (LPS)-induced NO production in RAW264.7 cells.

Results

The results of the irritation test showed that the “Four white” extract has low irritation and high biosafety. It can scavenge different free radicals and has protective effect against oxidative damage. The tyrosinase inhibition test showed that the extracts had whitening ability. In terms of anti-inflammatory activity, it can inhibit hyaluronidase activity to a certain extent and reduce the production of NO by LPS-stimulated cells.

Conclusion

“Four white” extract has high biosafety and skin-care efficiency such as antioxidant, whitening and anti-inflammatory properties.