石香薷中两个新黄酮甙的研究

石香薷中两个新黄酮甙的研究郑尚珍，孙丽萍，沈序维王毅（西北师范大学化学系，兰州，７３００７０）（中国科学院兰州化学物理研究所）关键词石香薷，唇形科，黄酮甙唇形科植物石香薷（ＭＯｓｌａｃｈｉｎｅｎｓｉｓＭａｘｉｍ）作为中药，用来治疗暑湿感冒、头痛、腹痛...     

Two new noroleanane-type triterpenoid saponins from the stems of Stauntonia chinensis

Two new noroleanane-type triterpenoid saponins, 3β,20α,24-trihydroxy-29-norolean-12-en-28-oic acid 24-O-β-L-fucopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→3)]-β-D-glucopyranoside (1) and 3β,20α,24-trihydroxy-29-norolean-12-en-28-oic acid 24-O-β-D-glucopyranosyl-(1→2)-[α-L-arabinopyranosyl-(1→3)]-β-D-glucopyranoside (2) were isolated from the stems of Stauntonia chinensis DC., together with three known compounds, brachyantheraoside B₂ (3), eupteleasaponin Ⅷ (4) and fargoside B (5). Their structures were elucidated by spectroscopic and chemical methods. The cytotoxic activities of compounds 1 and 2 were evaluated against five human tumor cell lines (HCT-116, HepG2, BGC-823, NCI-H1650, and A2780). Compounds 1 and 2 showed moderate cytotoxic activities toward the tested cell lines with IC₅₀ values ranging from 12.71 to 32.04 μM.     

Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from Belamcanda chinensis

The aim of this study is to explore anti-inflammatory phytochemicals from B. chinensis based on the inhibition of pro-inflammatory enzyme, human neutrophil elastase (HNE) and anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage. Three stereoisomers of iridal-type triterpenoids (1–3) were isolated from the roots of B. chinensis and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC₅₀ values of 6.8–27.0 µM. The binding affinity experiment proved that iridal-type triterpenoids had only a single binding site to the HNE enzyme. Among them, isoiridogermanal (1) and iridobelamal A (2) displayed significant anti-inflammatory effects by suppressing the expressions of pro-inflammatory cytokines, such as iNOS, IL-1β, and TNF-α through the NF-κB pathway in LPS-stimulated RAW264.7 cells. This is the first report that iridal-type triterpenoids are considered responsible phytochemicals for anti-inflammatory effects of B. chinensis.     

Study on the Dynamic Difference between Single and Mixed Residues of Three Neonicotinoids in Brassica chinensis L.

Multiple insecticides’ residues after the mixed application of several neonicotinoids cause combined pollution and bring new challenges to food safety and pest control during agricultural production. In this study, three neonicotinoid insecticides, namely imidacloprid (IMI), acetamiprid (ACE), and thiamethoxam (TMX), were mixed and evenly sprayed on Brassica chinensis L. in the field. Then, the insecticides’ residues were dynamically monitored to determine the differences in their rates of dissipation and final residues after 10 days. The results showed that the dissipation kinetics of neonicotinoids still conformed to the first-order kinetic model for binary or ternary application of neonicotinoid mixtures, with all determination coefficients (R²) being above 0.9 and the dissipation half-life (DT₅₀) being 2.87–6.74 d. For treatment groups with five times the recommended dosages (IMI 300 g·hm⁻², ACE 900 g·hm⁻², and TMX 600 g·hm⁻²), mixed insecticides had a slower dissipation rate, and the DT₅₀ values of mixtures were longer than those of single insecticides. Moreover, the final insecticide residues with mixed application were higher than those of single compounds at 10 d after spraying. Thus, mixed applications of neonicotinoids may increase food safety risks as they increase the final insecticide residues in Brassica chinensis L., and care should therefore be taken when considering the combined use of such compounds.     

A Comparison Study on Polysaccharides Extracted from Atractylodes chinensis (DC.) Koidz. Using Different Methods: Structural Characterization and Anti-SGC-7901 Effect of Combination with Apatinib

For hundreds of years, Atractylodes chinensis (DC.) Koidz. (AK) has been widely used as a treatment for spleen and stomach diseases in China. The AK polysaccharides (AKPs) have been thought to be the important bioactive components. In this stud, the impacts of different extraction methods were analyzed. The differences between AKPs extracted by hot water extraction (HWE), AKPs extracted by ultrasonic extraction (UAE), and AKPs extracted by enzyme extraction (EAE) were compared in terms of yield, total carbohydrate content, molecular weight distribution, monosaccharide composition, and synergistic activity of the AKPs with apatinib were determined. The results indicated that the yield of the polysaccharide obtained from HWE was higher than that of UAE and EAE. However, activity assays indicated that UAE-AKPs and HWE-AKPs enhanced apoptosis of human gastric cancer cells (SGC-7901) treated with apatinib and UAE-AKPs showed the strongest synergistic activities. This is also in agreement with the fact that UAE-AKPs have a smaller molecular weight, β-configuration, and higher galactose content. These findings suggested that UAE is an efficient and environmentally friendly method for producing new polysaccharides from Atractylodes chinensis (DC.) Koidz. for the development of natural synergist and for the treatment of gastric cancer.     

Evaluation of the Antioxidant,Cytoprotective and Antityrosinase Effects of Schisandra chinensis Extracts and Their Applicability in Skin Care Product

Plant extracts have been widely used for skin care for many centuries, and nowadays, they are commonly applied for the development and enrichment of new cosmetic preparations. The present study aimed the assessment of the biological activity of aqueous Schisandra chinensis extracts as a potential ingredient of skin care products. The aspects studied involved the ability to neutralize free radicals, impact on viability and metabolism of keratinocytes, as well as tyrosinase inhibitory potential. Our study showed that aqueous S. chinensis extracts have a positive effect on keratinocyte growth and have high antioxidant potential and strong tyrosinase inhibitory activity. UPLC-MS analysis revealed that three groups of phenolic compounds were predominant in the analyzed extract, including lignans, phenolic acids and flavonoids and protocatechiuc and p-coumaryl quinic acids were predominant. Moreover, microwave-assisted extraction, followed by heat reflux extraction, was the most effective for extracting polyphenols. Furthermore, a prototypical natural body washes gel formulation containing the previously prepared extracts was developed. The irritation potential and viscosity were assessed for each of the formulations. The study demonstrated that the addition of these extracts to body wash gel formulations has a positive effect on their quality and may contribute to a decrease in skin irritation. In summary, S. chinensis aqueous extracts can be seen as an innovative ingredient useful in the cosmetic and pharmaceutical industry.     

Rapid separation of polysaccharides using a novel spiral coil column by high‐speed countercurrent chromatography

The separation of polysaccharides is time consuming. We developed and optimized a type‐J counter‐current chromatography system with a novel tri‐rotor spiral coil column for the rapid separation of polysaccharides. The optimal composition of an aqueous PEG1000/K₂HPO₄/KH₂PO₄ system was found to be 14:16:14 w/w/w where the lower phase was the mobile phase. Optimal performance was achieved at a column rotational speed, temperature, and flow rate of 1200 rpm, 45°C, and 3.0 mL/min, respectively. The mobile phase was pumped from the inner terminal in a ‘‘head‐to‐tail’’ elution mode. Polysaccharide LCP‐1 (10.7 mg) was successfully obtained in high purity in one step from 50.0 mg of a crude polysaccharide extracted from the lychee fruit (Litchi chinensis) within 100 min. LCP‐1 possess a number‐average molecular weight and weight‐average molecular weight of 1.05 × 10⁵ and 1.59 × 10⁵ kDa, respectively. The monosaccharide composition consists of the molar ratio of glucose, galactose, and arabinose of 1.3:3.5:1.     

Comparative pharmacokinetics and tissue distribution of schisandrin,deoxyschisandrin and schisandrin B in rats after combining acupuncture and herb medicine (schisandra chinensis)

Recently, combination therapy with acupuncture and medicine as a practical strategy to treat diseases has gained increasing attention. The present study aimed to investigate whether acupuncture stimulation at ST.36 had a potential impact on the pharmacokinetics and tissue distribution of lignans. An HPLC‐ESI/MS analytical method was established and successfully applied to a comparative study of drug concentration in plasma and tissues of three lignans. The parameters area under the plasma concentration–time curve from time zero to the final measurable point and from time zero to infinity, and peak concentration were significantly increased, with a prolonged mean residence time and a corresponding decrease in clearance in comparision with the Schisandra‐alone group. Additionally, tissue concentrations of three lignans were improved in the group with acupuncture, especially in liver. The results indicated that acupuncture has a synergistic effect on the pharmacokinetics and tissue distribution of the three lignans, which could postpone their elimination, resulting in a longer blood circulating time in rat plasma and prolonged residence time in target tissues, leading to higher tissue concentration. The findings provide some scientific evidence for the mechanism of the combined use of acupuncture and herbal medicine. Furthermore, we suggest that acupuncture and its combination with herbal medicine should be investigated further as a possible adjuvant therapy in clinical treatment for liver injury. Copyright © 2014 John Wiley & Sons, Ltd.     

A New Triterpenoid Oligoglycoside Escin IVe from the Seeds ofAesculus Chinensis

Inthecourseofourstudiesonnewbiologicallyactivesaponinsofnaturalmedicines,wehaveisolatedescinsla.fo.IVa.IVb,IVc,andIVdtyolnseedsof.4e'v"11/llSchinensisBee.(Hippocastanaceae),andsinglecrystalX-raydiffractionanalysiswasundertakenonescinla'.whichconfirmstheabsoluteconfigurationandsugarsequence.ThepresentpaperdescribesthestructuredeterminationofanewtriterpenoidsaponinnamedescinIVefromthesameplant.EscinIVe,whitepowder.Positive-modeTOF-MScm/zI111[M Na] ,coupledwitllNMRdata.correspondstoane…     

华根霉全细胞脂肪酶催化合成生物柴油

比较了5种不同商品化脂肪酶和自制的华根霉CCTCCM201021全细胞脂肪酶(RCL)催化油脂合成生物柴油的转化效果,结果表明,RCL能有效应用于无溶剂体系催化合成生物柴油.在无溶剂体系中对该酶催化生物柴油的转酯化反应工艺进行优化,考察了甲醇用量、体系含水量、酶的添加量和反应温度对生物柴油收率的影响,使生物柴油最终收率大于86.0%.在有机溶剂体系中选择不同有机溶剂作为助溶剂进行转酯化反应,发现logP值在4.0～4.5的有机溶剂具有较好的转化效果.其中以正庚烷为助溶剂的转酯化反应具有最高的生物柴油收率86.7%.在无溶剂体系中RCL催化转化油酸和模拟高酸价油脂合成脂肪酸甲酯的研究表明,该酶具有很好的催化合成生物柴油的潜力.