Lignans are the main active components of Schisandrae Chinensis Fructus for liver disease treatment:a review

As a traditional Chinese herbal medicine,Schisandrae Chinensis Fructus(SC)has been used in medicine and food industry due to its health care and therapeutic effects.Over the past 20 years,the use of SC and its active ingredient lignans in the prevention and treatment of liver diseases has been increasing,and their hepatoprotective effects has increased the interest of the public and academia.Therefore,in the present work,we first determined the effectiveness of SC in the treatment of liver diseases such as metabolic associated fatty liver disease,alcoholic liver disease,cholestatic liver disease and acute liver injury.Subsequently,the pharmacological effects and molecular mechanisms of lignans,the active components of SC,for liver disease treatment were comprehensively summarized for the first time.The results showed that the lignans in SC could achieve hepatoprotective effects by regulating lipid metabolism,anti-fibrosis,anti-inflammation,anti-oxidation,anti-tumor and regulating bile acid metabolism.The mechanism mainly involved adenosine 5’-monophosphate-activated protein kinase,endoplasmic reticulum stress,sterol regulatory element binding protein 1c,autophagy,transforming growth factor-β,mitogen-activated protein kinase,microRNA,nuclear factor kappa-B,nuclear factor erythroid-2-related factor 2,heat shock proteins and pregnane X receptor signaling pathways.These results can lay a scientific foundation for the development of hepatoprotective drugs or functional foods from SC/lignans.

Effects of Different Decolorants on Retention Rate of Total Triterpenes in Fruit and Rattan Stems of Schisandra chinensis(Turcz.) Baill

This study was to investigate the decoloration effects of activated clay, activated carbon, diatomite, Ca group bentonite, kaolin, activated aluminum oxide, magnesium oxide and attapulgite. Ultraviolet-visible spectroscopywas adopted to de- tect the absorbanees of the extracts of Schisandra chinensis fruit and rattan stems, the contents of total triterpenoids in S. chinensis fruit and rattan stems were deter- mined, and the decoloration rate and the retention rate of total triterpenoids of S. chi- nensis fruit and rattan stems were calculated. The results indicated that, attapulgite exhibited the best decoloration effect on the extract of S. chinensis fruit, with a de- coloration rate up to 60.47%, activated carbon exhibited a better decoloration effect on the extract of S. chinensis rattan stems, with a decoloration rate up to 69.24%, and they had relatively higher retention rates of total triterpenoids. In the eight de- colorants, attapulgite showed the best decoloration effect on the extract of S. chi- nensis fruit, and activated carbon exhibited the best decoloration effect on the ex- tract of S. chinensisrattan stems.

胚乳和外源赤霉素对五味子[Schisandra chinensis (Turcz.) Baill]种子发芽的影响

以组织培养和土壤播种的未经层积处理的五味子种子为材料，检测胚乳和外源赤霉素（GA3）对发芽影响的结果表明，在不加生长调节物质的MS培养基上，去掉外种皮带全胚乳的种子发芽率只有2．7％，而带1／2和1／3胚乳的种子发芽率则分别为46％和70．6％；培养基中添加GA，，可提高去掉外种皮带全胚乳和带1／2胚乳种子的发芽率，而对带1／3胚乳的种子则无效果。土壤播种时，用10—1000mg·L—GA3对去掉外种皮种子进行1~10d前处理，其中100mg·L—GA3前处理10d的发芽率最高，达到38．7％。

不同产地五味子果皮和种子中微量元素含量的研究

[目的]测定不同产地五味子果皮和种子中微量元素含量,从微量元素角度评价中药材质量。[方法]采用电感耦合等离子体质谱仪对各元素含量进行测定。[结果]五味子中含多种微量元素,且重金属含量符合药典规定。[结论]同一产地果皮和种子中微量元素含量不同,不同产地相同元素含量差异较大。

Effect of Schisandra chinensis polysaccharide on intracerebral acetylcholinesterase and monoamine neurotransmitters in a D-galactose-induced aging brain mouse model

BACKGROUND： The most prominent characteristic of brain aging is decreased learning and memory ability. The functions of learning and memory are closely related to intracerebral acetylcholinesterase （ACHE） and monoamine neurotransmitter activity. Previous studies have shown that Schisandra chinensis polysaccharide has an anti-aging effect. OBJECTIVE： To explore the effects of Schisandra chinensis polysaccharide on AChE activity and monoamine neurotransmitter content, as well as learning and memory ability in a D-galactose-induced aging mouse brain model compared with the positive control drug Kangnaoling. DESIGN, TIME AND SETTING： Completely randomized, controlled experiment based on neurobiochemistry was performed at the Pharmacological Laboratory, Henan University of Traditional Chinese Medicine from September to December 2003. MATERIALS： Schisandra chinensis was purchased from Henan Provincial Medicinal Company. Schisandra chinensis polysaccharide was obtained by water extraction and alcohol precipitation. Kangnaoling pellets were provided by Liaoning Tianlong Pharmaceutical （batch No. 20030804; state drug permit No. H21023095）. A total of 50 six-week-old Kunming mice were randomly divided into five groups： blank control, model, Kangnaoling, high and low dosage Schisandra chinensis polysaccharide groups, with 10 mice per group. METHODS： Mice in the blank control group were subcutaneously injected with 0.5 mL/20 g normal saline into the nape of the neck each day, while the remaining mice were subcutaneously injected with 5% D-galactose saline solution （0.5 mL/20 g） in the nape for 40 days to induce a brain aging model. On day 11, mice in the high and low dosage Schisandra chinensis polysaccharide groups were intragastrically infused with 20 mg/mL and 10 mg/mL Schisandra chinensis polysaccharide solution （0.2 mL/10 g）, respectively. Mice from the Kangnaoling group were intragastrically infused with 35 mg/mL Kangnaoling suspension （0.2 mL/10 g）, and the mice in the model group were intragastrically infused with the same volume of normal saline （0.2 mL/10 g） once per day for 30 consecutive days. MAIN OUTCOME MEASURES： Two hours after the final administration, pathohistological changes in the cerebral cortex and hippocampus were observed using hematoxylin ＆ eosin staining. AChE activity was detected using chromatometry. Monoamine neurotransmitter content was measured using fluorimetry. Learning and memory was measured using the step down test and darkness avoidance test. RESULTS： Both Schisandra chinensis polysaccharide and Kangnaoling improved pathological injury to the cerebral cortex and hippocampus in a mouse model of brain aging. Compared with the blank control group, AChE activity and content of norepinephrine （NA）, dopamine （DA）, and 5-hydroxytryptamine （5-HT） were significantly decreased in the model group （P 〈 0.01 ）. In contrast, AChE activity and NA, DA, and 5-HT levels significantly increased in the Kangnaoling and high dosage Schisandra chinensis polysaccharide groups （P 〈 0.01）, while NA levels significantly increased in the low dosage Schisandra chinensis polysaccharide group （P 〈 0.01）. Drug treatment improved learning and memory abilities （P 〈 0.01 or P 〈 0.05）. CONCLUSION： Schisandra chinensis polysaccharide significantly increased levels of central neurotransmitters and improved learning and memory in a mouse model of brain aging. The effects of Schisandra chinensis polysaccharide were equal to that of Kangnaoling pellets.

Nortriterpenoids from the fruit stalk of Schisandra chinensis (Turcz.) Baill.

Objective:The fruit stalk of Schisandra chinensis(Turcz.)Baill.(S.chinensis)has been found to contain bioactive components similar to the fruit of S.chinensis.Here,we report a recent discovery about new nortriterpenoids with a novel skeleton and anti-gastric cancer activity,which were isolated from the fruit stalk of S.chinensis.Methods:The chemical components of ethyl acetate extract from 70%ethanol extract from S.chinensis fruit stalk were separated,purified,and identified by liquid chromatography methods(silica gel,ODS,HPLC)and extensive spectroscopic analyses(NMR,IR,UV,MS,CD).Results:Two new nortriterpenoids,schilancitrilactone M and 25-hydroxyl schindilactone D(1 and 2),along with ten known nortriterpenoids(3-12)were isolated from the fruit stalk of S.chinensis.The isolated compounds were tested for their cytotoxic activities against MGC-803 cells,and the results showed that compounds 6-8 possessed significant activities with IC50 of 9.01,11.77,and 2.74μmol/L,respectively.Conclusion:Twelve nortriterpenoids including two new compounds were isolated from the fruit stalk of S.chinensis for the first time.Among them,compounds 6-8 showed significant anti-gastric cancer activities.We postulated that the fruit stalk of S.chinensis could be used as an anti-gastric cancer drug.

Study on HPLC method to determine contents of Schisandrin A and Schisandrin B in Schisandra chinensis extraction

The determination method of Schisandrin A and Schisandrin B in Schisandra chinensis was improved with the high performance liquid chromagraphy （HPLC）. The sample was extracted exceedingly in the critical limit of CO2. The retention time of Schisandrin A and Schisandrin B was reduced, with methano/water （75 ： 25） as mobile phase. The wavelength for detection was 254 nm. The R^2 of standard curve was 0.9998 and the relative standard deviation was 2.31% and 3.17% with the recovery of 96.45% and 97.37%, respectively. The result shows that the rate of veracity of this method is higher and it proves that the determination method of Sehisandrin A and Schisandrin B in Schisandra chinensis is a feasible method.

Pharmacological effects of Schisandra Chinensis Fructus polysaccharide on intestinal protection

Schisandra Chinensis Fructus(SCF)is the fruit of Schisandra chinensis(Turcz.)Baill.,a perennial vine.It was first recorded in Shen Nong′s herbal classic and has a long application history.Studies have shown that SCF has anti-inflammatory,protective liver,antioxidant,antibacterial and other pharmacological effects.Ancient prescriptions are commonly used in the treatment of chronic diarrhea and other intestinal diseases and diabetes.Modern clinical pharmacology features of SCF polysaccharide(SCFP)in diabetes,liver diseases,enteritis and other aspects have achieved excellent results.Gut is an important digestive organ of human body,but intestinal diseases are varied,including Crohn′s disease,ulcerative colitis,intestinal flora imbalance,etc..It is a chronic and non-specific inflammatory disease.The disease is persisted for a long time and the incidence rate is expected to rise.Most of the symptoms are recurrent diarrhea,bloody stool and abdominal pain.It is considered by the World Health Organization as a refractory disease.At present,there is little possibility of complete cure,which is closely related to complex environmental factors,eating habits and heredity.In recent years,clinical studies have found that SCFP has a variety of pharmacological effects on intestinal protection.①Reduce inflammatory factors:intestinal mucositis is a common adverse reaction in patients with chemotherapy.The development of mucositis is related to pro-inflammatory factors such as tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),IL^(-1)β,Interferon-γ(IFN-γ).SCFP can significantly reduce IL-6 TNF-α,IL^(-1)β,and IL-8,as well as the accumulation of T cells in the process of resisting apoptosis,reduce the inflammatory reaction and protect the damage to villi and crypts,improve the symptoms of small intestinal mucositis caused by weight loss and diarrhea.②Promote immunoglobulin A secretion:intestinal mucosal immunity is the first line of defense of the body′s immune system.Its main antibody is secretory immunoglobulin A,which can destroy and phagocytize microorganisms,bacteria and viruses.SCFP can improve intestinal immunity by increasing the number and activity of T lymphocytes,promoting the secretion of secretory immunoglobulin A,and affecting the activity of a variety of cytokines.③Regulation of intestinal flora:the flora in the intestine has the functions of auxiliary nutrient absorption,biological antagonism and immune regulation,and can form a natural barrier for the host's intestine.When the human intestinal flora is disordered,probiotics will be greatly reduced,harmful bacteria will proliferate and destroy the intestinal environment.Under these conditions,the intake of SCFP significantly increased the number of beneficial bacteria such as bifidobacteria and lactobacillus,and significantly decreased the number of conditional pathogens such as enterococcus and escherichia coli,indicating that SCFP can indeed regulate the intestinal disorder caused by lincomycin hydrochloride to a certain extent. This may be because beneficial bacteria in the intestine metabolize polysaccharides produce short chain fatty acids such as lactic acid and acetic acid, which reduces the pH value in the intestine and inhibits the growth of enterococcus and Escherichia coli. In conclusion, SCFP can treat and protect intestinal diseases to a certain extent, which provides a favorable basis for the treatment of intestinal diseases.

Metabolism alternation of schisandra chinensis in carbon tetrachloride-intoxicated rats and patients with advanced hepatocellular carcinoma

OBJECTIVE To study the pharmacokinetics change of schisandra chinensis under the pathological condition of liver dysfunction for safe and rational use of herbal medicines.METHODS The metabolism of four effective lignans from schisandra chinensis(SC),schisandrin,schisantherin A,deoxyshisandrin and γ-schisandrin was studied using microsomes from patients with advanced hepato.cellular carcinoma.In situ intestinal and hepatic perfusions were conducted to clarify the contributions from impairments of gut and liver on the pharmacokinetics of the four schisandra lignans in CCl4-intoxi.cated rats.The metabolism in rat and human liver microsomes and transport in Caco-2 monolayer cell model were studied to reveal the key factors for the in vivo disposition of the four lignans.RESULTS When SC alcoholic extract was orally administrated to CCl4-intoxicated rat for a short term(4 d),the pharmacokinetics of four active SC lignans was significantly changed while its hepatoprotective effect was not obviously observed.The plasma concentrations of the four schisandra lignans were dramatical.ly elevated compared with the control.The Cmax,AUC and MRT were all increased or prolonged signif.icantly while parameter CLz/F was obviously reduced in rat pretreated with CCl4.In hepatic perfusion study and liver microsomes incubation,it was found that the hepatic metabolism of the four lignans was markedly decreased mainly due to the activity reduction of multiple CYP450 isoenzymes involved the metabolism,which,eventually,might lead to the alternation of their pharmacokinetic profiles in CCl4-intoxicated rats or patients with advanced hepatocellular carcinoma.CONCLUSION The pharmacoki.netic studies of SC components in pathological situation of liver dysfunction are expected to provide useful data for rational and safe application of SC preparations in clinic or further pharmacological and toxicological research.

Analysis of Essential Oil from Stems of Schisandra Chinensis(Turc z.) Baill

The essential oil of Schisandra Chinensis(Turc z.) Baill was extracted and analyzed. The essential oil was obtained in a 1.8%(mL/100 g material) yield. Forty eight compounds were isolated and characterized from the oil. The results show that the content(20.42%) of β -pinene of naturally essential oil is the highest among the components of the oil,which has laid a foundation for the futher development and application of the stems of Schisandra Chinensis(Turc z.) Baill .

How Schisandrae Fructus Benefits the Body: Mechanisms in Traditional Chinese Medicine and Modern Medicine

Schisandrae chinensis Fructus (SF) is a commonly used herb in Traditional Chinese Medicine (TCM). According to TCM theory, SF can invigorate Qi in the liver and other visceral organs through the meridian system. Furthermore, the liver’s pivotal role in regulating the functions of various visceral organs helps explain how SF can promote holistic health benefits. The main active ingredient of SF, schisandrin B (Sch B), has been found to improve mitochondrial ATP production and enhance glutathione redox status in multiple organs. This could account for the overall protective effects of Sch B on organs. Due to its stronger impact on liver function, the positive influence of Sch B on different organs may be facilitated by signal molecules originating from the liver.

Schisandra chinensis (Turcz.) Baill

Schisandra chinensis (Turcz.) Baill. is a deciduous woody vine, and belongs to the Schisandraceae family. This species is a horticultural plant with edible fruit. It is used medicinally and for making rope. It is distributed in Hebei, Heilongjiang, Jilin, Liaoning, Nei Mongol, Shanxi

五味子及其制剂中木脂素类成分含量测定的研究进展

综述了五味子及其制剂中主要活性成分木脂素含量测定方法的最新进展,包括分光光度法,TLCS,HPLC,GC MS和CEC法,评述了每一种分析方法的特点和适用范围,为五味子药材和制剂质量评价提供参考。

北五味子果实超临界CO_2萃取工艺的研究

通过正交设计的试验方法,探讨了超临界CO2 法萃取五味子果实中木脂素的工艺条件,确定了最佳工艺条件为萃取压力30Mpa,萃取温度50℃,萃取时间120min。

反相高效液相色谱法测定五味子中木脂素的含量

目的 建立反相高效液相色谱法对五味子中的保留木脂素成分同时进行含量测定。方法 反相高效液相色谱法,色谱柱为Inertsil ODS-3 column(250 mm×4.6 mm i.d.,5μm),采用梯度洗脱的方式,流动相:A 甲醇,B 水。梯度洗脱:0-16 min VA : VB=70:30,16-40 min VA:VB=100:0。结果 五味子中四种木脂素与周围未知成分达到基线分离,四种木脂素线形关系良好,相关系数r>0.999。结论 此法简单、灵敏、快速,为分析五味子及其相关制剂中主要单体木脂素提供了一种可行质量控制方法。

高效液相色谱法测定五味子乙素含量

采用高效液相色谱法,测定了五味子果实中五味子乙素的含量,检测波长为254nm,标准曲线线性关系R2为0.9907,相对标准偏差为0.48%,平均加样回收率为99.14%。结果表明,此方法准确度较高,为五味子生药及成品药中五味子乙素含量测定提供了一种切实可行的方法。

北五味子中2种木脂素的NMR数据解析

从北五味子(Schisandra chinensis (Turcz.))的果实中分离并鉴定了 3 个木脂素类化合物二氢愈疮木脂素(Ⅰ), Gomisin J (Ⅱ)和Gomisin D (Ⅲ), 利用高分辨 NMR技术及二维谱 (1H 1H COSY、HSQC、HMBC和NOESY) , 对Gomisin J(Ⅱ)和Gomisin D (Ⅲ)的1H和13C NMR数据进行了全归属和较详细的解析. 同时, 采用计算机分子模拟实验对结构较为复杂的Gomisin D的立体构型进行了研究.

Protective effects of extracts of Schisandra chinensis stems against acetaminophen-induced hepatotoxicity via regulation of MAPK and caspase-3 signaling pathways

The present study was designed to evaluate protective activity of an ethanol extract of the stems of Schisandra chinensis(SCE) and explore its possible molecular mechanisms on acetaminophen(APAP) induced hepatotoxicity in a mouse model. The results of HPLC analysis showed that the main components of SCE included schisandrol A, schisandrol B, deoxyschisandrin, schisan--drin B, and schisandrin C and their contents were 5.83, 7.11, 2.13, 4.86, 0.42 mg·g^(-1), respectively. SCE extract was given for 7 con--secutive days before a single hepatotoxic dose of APAP(250 mg·kg^(-1)) was injected to mice. Our results showed that SCE pretreatment ameliorated liver dysfunction and oxidative stress, which was evidenced by significant decreases in aspartate transaminase(AST), alanine aminotransferase(ALT), malondialdehyde(MDA) contents and elevations in reduced glutathione(GSH) and superoxide dismutase(SOD) levels. These findings were associated with the result that the SCE pretreatment significantly decreased expression levels of 4-hydroxynonenal(4-HNE) and 3-nitrotyrosine(3-NT). SCE also significantly decreased the expression levels of Bax, mitogen-activated protein kinase(MAPK), and cleaved caspase-3 by APAP exposure. Furthermore, supplementation with SCE suppressed the expression levels of inducible nitric oxide synthase(iNOS) and cyclooxygenase-2(COX-2), suggesting alleviation of inflammatory response. In summary, these findings from the present study clearly demonstrated that SCE exerted significant alleviation in APAP-induced oxidative stress, inflammation and apoptosis mainly via regulating MAPK and caspase-3 signaling pathways.

肝得宁片中五味子、女贞子提取工艺研究

目的 :为肝得宁片优化五味子、女贞子提取工艺条件。方法 :以五味子甲素转移率和得膏率为主要指标 ,结合工业化生产的可行性 ,对超临界CO2 萃取法、醇提法、水煮法等提取方法进行了比较研究 ,并采用正交设计法优选醇提工艺条件。结果 :3种提取方法以醇提法为佳 ,醇提工艺正交设计优化结果为 :乙醇浓度 90 % ,回流次数2次 ,时间为 1h ,溶媒用量为 6倍。结论 :本工艺稳定可行 ,可为提取五味子。

多成分含量测定结合抗氧化活性的化学计量学分析筛选五味子标准汤剂质量标志物的研究

目的探究五味子标准汤剂抗氧化活性的质量标志物。方法采用基于一测多评法(QAMS)的超高效液相色谱法(UPLC)结合化学计量学评价15批五味子标准汤剂的质量;采用DPPH法和ABTS法测定15批样品的抗氧化活性,并借助灰色关联度(GRA)和偏最小二乘回归法(PLSR)分析8种成分含量与抗氧化活性的关联。采用分子对接技术探讨候选质量标志物与抗氧化核心靶点的结合性,同时对单体的体外抗氧化活性进行实验验证。结果QAMS法与外标法(ESM)的含量结果差异不显著(P>0.05),并推测原儿茶酸、五味子醇乙、五味子酯乙、五味子乙素为五味子标准汤剂的质量差异成分。根据GRA和PLSR结果,上述4个质量差异成分可作为抗氧化能力的备选标志物。分子对接结果显示4个候选质量标志物与抗氧化相关靶点具有良好的亲和力。研究认为五味子标准汤剂的抗氧化作用可能是多种成分综合作用的结果,其中,单体成分验证结果显示原儿茶酸具有明显的抗氧化活性并呈现剂量依赖关系,最符合作为质量标志物的特征,因而可能作为五味子标准汤剂抗氧化的质量标志物。结论基于UPLC含量测定法和体外抗氧化实验,预测了五味子标准汤剂中的潜在抗氧化活性物质,也为五味子其它相关制剂的质量评价提供合理依据。