Four new lanostane triterpenoids featuring extendedπ-conjugated systems from the stems of Kadsura coccinea

Four new 14(13→12)-abeolanostane triterpenoids featuring extendedπ-conjugated systems,kadcoccitanes E-H(1-4),were obtained from the stems of Kadsura coccinea through using a HPLC−UV-guided approach.Their structural and configurational determination was accomplished through extensive spectroscopic analysis coupled with quantum chemical calculations.Kadcoccitanes E-H were tested for their cytotoxic activities against five human tumor cell lines(HL-60,A-549,SMMC-7721,MDA-MB-231,SW-480)but none of them exhibited activities at the concentration 40μM.

Dibenzocyclooctadiene Lignans with Platelet-Activating Factor (PAF) Antagonist Activity from Kadsura heteroclita

Seven known dibenzocyclooctadiene lignans,tigloylgomisin P(1), angeloylgomisin P(2),gomisin A(3),Schizandrin(4),angeloylgomisin H(5),gomisin B(6) and R(+)-gomisin M_1(7)were isolated from Kadsura heteroclita.The conformation of tiglolylgomisin P(1)was established by 2D NMR techniques.Using[~3H]platelet activating factor(PAF)binding to human platelet membrane assay,(1),(2)and(7)showed PAF receptor antagonistic activities.

Study on Effect of Drought Stress with PEG-6000 on Physiological and Biochemical Indicators in Kadsura coccinea

[Objective] The aim was to research drought resistance and adaptation mechanisms of Kaclsura coccinea under different drought stresses. [Method] The seedlings of Kadsura coccinea growing one year were taken as materials in order to investigate and analyze leaf SPAD value, relative water content （RWC）, malonaldehyde （MAD）, cell membrane permeability （RP）, proline （PRO） and superoxide dismutase activity （SOD）. [Result] As drought stress improved, leaf SPAD value and RWC were both diminishing and RWC fell remarkably; MAD, Pro, RP and SOD activity were increasing; MAD and RP grew significantly. [Conclusion] Kadsura coccinea is much sensitive to drought stress and will be affected if water loss is too much high.

A new triterpenoid from Kadsura coccinea

A new triterpenoid,possessing a lanost-9（11）-3-one skeleton,was isolated from the roots of Kadsura coccinea,based on the spectral analysis,its structure was elucidated as 3-hydroxy-12-acetoxycoccinic acid.

Four 14(13→12)‑Abeolanostane Triterpenoids with 6/6/5/6‑Fused Ring System from the Roots of Kadsura coccinea

Four new rearranged 6/6/5/6-fused lanostane-type triterpenoids,kadcoccitanes A-D(1-4),were isolated from the roots of Kadsura coccinea,and their structures were mainly elucidated by comprehensive analysis of their spectroscopic data.Additionally,the structure of 1 was ambiguously verifed by single-crystal X-ray difraction,while the structure of 2,which features a novel 8,16-epoxy motif,was validated by quantum chemical calculation of NMR parameters and ECD spectrum.Moreover,1 and 4 were found to exhibited anticoagulant activity,while 3 and 4 were found to possess anti-platelet aggregation activity.

Preparative isolation of Heteroclitin D from Kadsurae Caulis using normal-phase flash chromatography

Heteroclitin D （H.D） was successfully isolated from Kadsurae Caulis by using flash chromatography and recrystalllzed by methanol, 10.2 mg of H.D was obtained from 4.86 g of crude extract, and the purity determined by HPLC was 99.4%. The structure was identified by UV, IR, MS, and NMR analysis. The fast, simple and efficient method can be applied to the preparation of reference substance of H. D.

Analysis of Growth and Quality of Sun-cured Tobacco Kadsura Coccinea In Guangchang County

[Objective] The aim was to study the growth and quality characteristics of sun-cured tobacco Kadsura Coccinea in Guangchang County and give full play to its advantages. [Method] The research took tobacco varieties including Tiechi in Yiqian, Mushao in Yangxi Tiechi in Chishui, and Liuye in Toupo as test materials to explore development process, quality characteristics and economic traits of different varieties. [Result] The variety of Tiechi in Yiqian had medium growht, moderate growth periods, and the best economic benefits. Total content of aroma matter was the highest in the varieties of Tiechi in Yiqian. Also it had more content of products of browning reaction and products degraded by cembranoids. Besides, volume and quality of aroma were higher, as well as the score of sensory quality. [Conclusion]Comprehensive comparisons suggested that the variety of Tiechi in Yiqian was superior to others at tobacco-growing, economic benefits and quality.

Experimental Study on Anti-adjuvant Arthritis in Rats of Kadsura coccinea

[Objectives] To investigate the therapeutic effect of Kadsura coccinea on adjuvant arthritis( AA) rats and its mechanism from cytokine levels. [Methods] The complete Freund's adjuvant( CFA)-induced AA model of rats was used. The therapeutic effect of K. coccinea on AA rats was evaluated by the articular swelling,arthritis score,immune organ index and hematoxylin-eosin( HE) staining. The content of inflammatory factors TNF-α,IL-6,and IL-1β in the serum of AA rats was detected by enzyme-linked immunosorbent assay( ELISA) respectively. [Results]Compared with the model group,the total extract of K. coccinea( KCTE) could significantly inhibit the primary and secondary articular swelling of AA rats,lower the arthritis score and immune organ index,and improve the pathological state of ankles of AA rats. In the groups with a high and middle dosage of KCTE( KCTE-H and KCTE-M),KCTE could significantly reduce the content of TNF-α and IL-6 in the serum of rats,exhibiting a certain dose-effect relationship. [Conclusions]KCTE had significant therapeutic effect on the AA of rats,and the mechanism might be associated with the modulation of immune function and the decrease in the secretion of inflammatory cytokines TNF-α and IL-6.

A Review of Triterpenoids and Their Pharmacological Activities from Genus Kadsura

Plants in genus Kadsura,belong to the Schisandraceae family including genus Schisandra and genus Kadsura,revealed folk efficacy and medicinal application in the treatment of rheumatoid arthritis and gastroenteric disorders for a long history.Previous study indicated that plants from genus Kadsura mainly contain lignans,triterpenoids and essential oils,and showed the active compounds were lignans and triterpenoids.Among all compounds from Schisandraceae family,the triterpenoids between the genus Schisandra and genus Kadsura had obvious differences.In this paper,we reviewed214triterpenoids and their pharmacological activities reported from genus Kadsura in the past30years(from1987to2017),aiming to provide reference for further study.

Comparative Identification between Kadsura coccinea and Kadsura heteroclite

[Objectives]The purpose was to provide scientific basis for the identification and application of Kadsura coccinea and its chief adulterant Kadsura heteroclite.[Methods]The botanical characteristics,traits and microscopic morphology of the two plants were compared.[Results]K.coccinea was clearly distinguished from K.heteroclite in botanical characteristics,traits and microscopic morphology.[Conclusions]This study is of great significance to the identification and development of K.coccinea.

Differential metabolome landscape of Kadsura coccinea fruit tissues and potential valorization of the peel and seed tissues

Kadsura coccinea(Lem.)is a woody wine plant with a peculiar fruit enriched in important health-promoting compounds.The non-editable part of the fruit,i.e.,the seed and peel,represents more than 60%of the fruit and is considered a biowaste.This significantly restricts the development of the K.coccinea fruit industry.Clarifying the metabolic components of the different fruit parts can help to improve the utilization rate and valorization of K.coccinea.Herein,we evaluated K.coccinea fruit peel,pulp,and seed using widely-targeted metabolomics and quantified a set of 736 bioactive compounds from 11 major metabolite classes.The most prominent metabolite classes included lipids,amino acids,flavonoids,and lignans.Furthermore,our results emphasized a significant accumulation of flavonoids in pulp tissues,while alkaloids and lignans were abundant in peel and seed tissues,respectively.A total of 183 metabolites were differentially accumulated among the three tissues.Procyanidin C2,rutinoside,2-hydroxyoleanolic acid,5-hydroxymethyluracil,nootkatol,isoquercitrin,isohyperoside,quercetin-7-O-glucoside,hyperin,and rutin showed elevated accumulation in the peel.In the seed,kadsuralignan G,kadcoccilactone A,kadsuralignan H,lysoPE 20:5,iso-schisandrin ethyl alcohol,and kadangustin were significantly enriched.Our results highlight the diverse metabolome composition of K.coccinea fruit parts,which can be further exploited for its valorization in various industries.

BICYCLOOCTANOID NEOLIGNANS FROM PIPER KADSURA

Three new bicyclooctanoid neolignans, kadsurenin A, kadsurenin B and kadsurenin C were isolated from Piper kadsura (Choisy) Ohwi. Based on the spectroscopic analysis (UV, JR, MS, NMR, and X-ray), their structures were established as 7R, 8R, 3'S, 4'R, 5'R-△^(s')-3,4-methyienedioxy-5'-methoxy-4'-acetyloxy-2',3',4',5'-tetrahydro-2'-oxo-7.3',8.5'-neolignan; 7R, 8R, 3'S, 4'R, 5'R-△^(s')-3, 4-methylenedioxy-5'-methoxy-4'-hydroxy-2',3',4',5'-tetrahydro-2'-oxo-7. 3', 8. 5'-neolignan and 7R, 8R. 3'S, 4'R, 5'R-△^(s')-3, 4, 5'-trimethoxy-4'-hydroxy- 2', 3', 4', 5'-tetrahydro-2'-oxo-7. 3', 8. 5'-neolignan respectively.

NEOLIGNANS FROM PIPER KADSURA

Two new neolignans, Kadsuranin G and Kadsuranin H, were isolated from Piper Kadsura (Choisy) Ohwi. Baaed on the spectroscopic analysis (UV, IR, MS, NNR, and X-ray) and chemical reactions, their structures were established as 7R,BR,1'S,2'R,3'5-△^(8')-3,4,5'-trimethoxy-2'-hydroxy-1',2',3',4'-tetrahydro-4'-oxo-7,3',8,1'-neolignan and 7R,8R,1'S,2'R,3'S-△^(8')-3,4,5'-trimethoxy-2'-acetyloxy-1',2',3',4'-tetrahydro-4'-oxo-7,3',8,1'-neolignan.

Diurnal Variation of Photosynthetic Physiological Characteristics of Kadsura coccinea(Lem.)A.C.Smith

[Objectives]This study was conducted to investigate the diurnal variations of photosynthetic and physiological characteristics in 3-year-old Kadsura coccinea(Lem.)A.C.Smith plants.[Methods]A Li-6400 portable photosynthetic system was used to study the diurnal variations of the photosynthetic physiological characteristics of K.coccinea.[Results]The diurnal variation of the net photosynthetic rate(Pn)of K.coccinea leaves showed a"double peak"curve,and there was a lunch break at noon.The maximum value of Pn[4.51 mmol/(m^(2)·s)]appeared at 10:00,and the daily average Pn was 3.98 mol/(m^(2)·s);and the stepwise regression analysis showed that photosynthetically active radiation(PAR)and stomatal conductance(Gs)were the main factors affecting Pn.The partial correlation analysis and path analysis showed that the order of effects on Pn was Gs>PAR.[Conclusions]This study provides a reference for further research on the development and utilization of K.coccinea.

Technical Regulations for Standardized Planting of Rare and Multi-purpose Wild Fruit Kadsura coccinea

The cultivation technology were standardized for improving the yield and quality,and the commodity value and the competitiveness of fruit market,and solving the bottleneck problem—fruit quality and yield that affect the industrial development of rare and multi-purpose wild fruit Kadsura coccinea(Lem.)A.C.Smith.Through the investigation of K.coccinea production area and planting area,collection and analysis of fruit samples,it was found that in most planting area,the varieties of K.coccinea were mixed,with great differences in fruit quality and yield,which makes it impossible to realize large-scale planting.In view of these problems,a series of studies have been carried out and the technical regulations for standardized planting of rare and multi-purpose wild fruit K.coccinea were formulated.

NEOLIGNANS FROM PIPER KADSURA(Ⅱ)

Two new bicyclo[3,2,1]octanoid neolignans,named as kadsurenin I and kadsurenin J were isolated from Piper kadsura(Choiey)Ohwi.Based on the spectros- copic analysis(UV,IR,MS and NMR)and chemical derivatization,their structures were established as 7R,8R,1'R,2'S,3'R-Δ~s'-3,4,5'-trimethoxy-2'-hydroxy-1',2',3',4'- tetrahydro-4'-oxo-7.3',8.1'-neolignan and 7R,8R,1'R,2'S,3'R-Δ~s'-3,4,5'-trimethoxy -2'-acetoxy-1',2',3',4'-tetrabydro-4'-oxo-7.3',8.1'-neolignan respectively.

Based on Network Pharmacology to Explore the Action Mechanism of Caulis Sinomenii-Caulis Piperis Kadsurae Herb Pair in the Treatment of Rheumatoid Arthritis

Objective:By using the method of network pharmacology to explore the mechanism of action of Caulis Sinomenii-Caulis Piperis Kadsurae herb pair in the treatment of rheumatoid arthritis.Methods:Search and screen the active ingredients and targets of Qingfengteng(Caulis Sinomenii)and Haifengteng(Caulis Piperis Kadsurae)through the TCMSP database,and predict and supplement the target points of the active ingredients through the Swiss Target Prediction platform;collect rheumatoid arthritis disease targets through GeneCards,OMIM database,and DRUGBANK database,construct a Venn diagram,and obtain the key target of Caulis Sinomenii-Caulis Piperis Kadsurae herb pairs in the treatment of rheumatoid arthritis;use Cytoscape 3.7.1 to establish the effect of Caysaceae sylvestris and Rhizoma sibirica in the treatment of rheumatoid arthritis"Drug-active ingredient-target"network diagram,submit key targets to STRING11.0 database to construct a protein interaction network model to obtain core targets;perform the GO and KEGG enrichment analysis of key targets on the Metascape platform,and draw the network diagram of"active pharmaceutical ingredients-targets-pathways".Results:After screening,discover a total of 27 active ingredients of Caulis Sinomenii-Caulis Piperis Kadsurae herb pairs,which can act on 229 targets,1269 related targets for rheumatoid arthritis diseases.And obtain a total of 95 common targets for drug active ingredients and diseases,including PTGS2,EGFR,MMP9,CASP3,JUN,etc.The common targets are mainly enriched in signaling pathways such as Pathways in cancer,Th17 cell differentiation and Endocrine resistance etc.Conclusion:This study preliminarily explored the potential mechanism of Caulis Sinomenii-Caulis Piperis Kadsurae herb pairs in the treatment of rheumatoid arthritis.The Caulis Sinomenii-Caulis Piperis Kadsurae herb pair may regulate cancer-related pathways,Th17 cell differentiation,endocrine resistance and other pathways to treat rheumatoid arthritis by regulating targets such as PTGS2,EGFR,and MMP9,providing clues and ideas for follow-up experimental research.

瑶药小钻的特征图谱及其安五脂素含量和抗炎活性研究

目的 建立瑶药小钻特征图谱及其主要成分安五脂素含量测定方法,并评价安五脂素抗炎活性。方法 采用高效液相色谱法,以乙腈-0.5%磷酸溶液为流动相进行梯度洗脱,采用《中药色谱指纹图谱相似度评价系统(2012版)》建立小钻药材的特征图谱和进行相似度评价,并测定小钻中安五脂素含量。以脂多糖诱导的RAW264.7巨噬细胞为炎症细胞模型,考察安五脂素对细胞上清液中肿瘤坏死因子α(TNF-α)、白细胞介素1β(IL-1β)、IL-6水平的影响。结果 10批小钻样品的特征图谱相似度为0.901~0.994;标定了9个共有峰,指认了3个成分,分别为长南五味子素E、南五味子内酯A、安五脂素;安五脂素的含量为(0.72±0.05)~(1.21±0.03)mg/g(n=3)。0.125~0.5μg/mL的安五脂素可显著降低炎症模型细胞上清液中TNF-α、IL-1β、IL-6水平(P<0.05或P<0.01)。结论 建立了小钻药材HPLC特征图谱及其安五脂素含量测定方法;安五脂素可能是小钻药材发挥抗炎作用的有效成分。

New Collection of Crude Drugs in Chinese Pharmacopoeia 2010 Ⅲ. Kadsurae Caulis

The dried cane of Kadsura interior (Kadsurae Caulis) is recorded in Chinese Pharmacopoeia 2010 as Dian Jixueteng for the treatment of rheumatism, irregular menstruation, and deficiency of Qi and blood. In this paper, morphological characteristics, chemical constituents, and pharmacological activities in the cane of K. interior were summarized. Moreover, some suggestions about application and quality control of Kadsurae Caulis were proposed in order to provide a theoretical basis for further scientific use.

滇鸡血藤红色素的提取工艺优化及其抑制COX-2活性研究

目的:研究滇鸡血藤红色素的最佳提取条件,考察其基本性质与环氧化酶-2(COX-2)抑制活性,为滇鸡血藤的临床用药及相关制剂开发提供参考。方法:以吸光度为指标,采用单因素试验和正交试验对滇鸡血藤红色素提取工艺中的液料比、浸提时间、乙醇体积分数进行优化,确定滇鸡血藤红色素的最佳提取工艺,对提取得到的红色素光、热、pH稳定性进行考察,进一步采用COX-2抑制剂筛选试剂盒考察滇鸡血藤红色素对COX-2的抑制作用。结果:在50%乙醇、液料比为110、浸提12 h的条件下提取的滇鸡血藤红色素吸光度最大;其在室温避光、pH 1~9条件下有较好的稳定性;滇鸡血藤红色素对COX-2有较好的抑制作用,半数抑制浓度(IC50)为2.04 ng·mL^(-1)(生药质量浓度)。结论:明确了滇鸡血藤红色素的最佳提取条件和稳定性条件,可为滇鸡血藤资源的综合开发利用与临床用药研究提供参考。