桑树细胞培养物的化学成分研究

目的:研究桑树细胞培养物的化学成分.方法:采用多种色谱技术,对桑树悬浮细胞培养物的化学成分进行分离纯化,通过理化性质及波谱数据确定化合物结构.结果:共分离鉴定了8个化合物,分别为异补骨脂查尔酮(1),染料木素(2),norartocarpetin (3),阿尔本A(4),光桑酮E(5),桑呋喃F(6),chalcomoracin (7),桑酮J(8).结论:化合物1～8均为黄酮类化合物,其中化合物3～6为首次从桑树细胞培养物中分离得到的化合物.     

The root barks of Morus alba and the flavonoid constituents inhibit airway inflammation

Ethnopharmacological relevance

The root barks of Morus alba have been used in traditional medicine as an anti-inflammatory drug, especially for treating lung inflammatory disorders.

Aim of study

To find new alternative agents against airway inflammation and to establish the scientific rationale of the herbal medicine in clinical use, the root barks of Morus alba and its flavonoid constituents were examined for the first time for their pharmacological activity against lung inflammation.

Materials and methods

For in vivo evaluation, an animal model of lipopolysaccharide-induced airway inflammation in mice was used. An inhibitory action against the production of proinflammatory molecules in lung epithelial cells and lung macrophages was examined.

Results

Against lipopolysaccharide-induced airway inflammation, the ethanol extract of the root barks of Morus alba clearly inhibited bronchitis-like symptoms, as determined by TNF-α production, inflammatory cells infiltration and histological observation at 200–400 mg/kg/day by oral administration. In addition, Morus alba and their major flavonoid constituents including kuwanone E, kuwanone G and norartocarpanone significantly inhibited IL-6 production in lung epithelial cells (A549) and NO production in lung macrophages (MH-S).

Conclusions

Taken together, it is concluded that Morus alba and the major prenylated flavonoid constituents have a potential for new agents to control lung inflammation including bronchitis.     

Antimicrobial activity of the methanolic extract and compounds from Morus mesozygia stem bark

Aim of the study

This study was aimed at investigating the antimicrobial activity of the methanolic extract (MMB) and compounds isolated from the stem bark of Morus mesozygia, namely 3β-acetoxyurs-12-en-11-one (1), moracin Q (2), moracin T (3), artocarpesin (4), cycloartocarpesin (5), moracin R (6), moracin U (8), moracin C (9), and moracin M (10).

Materials and Methods

The liquid microdilution assay was used in the determination of the minimal inhibitory concentration (MIC) and the minimal microbicidal concentration (MMC), against nine bacterial and two fungal species.

Results

The results of the MIC determination showed that the compounds 3, 4, 8 and 9 were able to prevent the growth of all tested microbial species. All other samples showed selective activities. Their inhibitory effects were noted on 90.9% studied organisms for the crude extract, 81.8% for compound 6, 72.7% for compound 10, 63.6% for compound 1, 54.5% for compound 5, and 45.5% for compound 2. The lowest MIC value of 39 μg/ml was obtained with the crude extract against Escherichia coli. The corresponding value for compounds (5 μg/ml) was registered with compound 9 on Shigella dysenteriae and compound 3 on E. coli, S. dysenteriae, Pseudomonas aeruginosa, Salmonella typhi and Bacillus cereus. The lowest MIC value (39 μg/ml) observed with the crude extract (on E. coli) was only eightfold greater than that of gentamycin used as reference antibiotic (RA) while the corresponding value (5 μg/ml) recorded with compounds 3 and 9 was equal to that of RA on the corresponding microorganisms.

Conclusions

The obtained results highlighted the interesting antimicrobial potency of M. mesozygia as well as that of the studied compounds, and provided scientific basis for the traditional use of this species.     

RP-HPLC测定桑椹中芦丁的含量

目的:优化桑椹中芦丁的提取条件并建立芦丁的HPLC测定方法。方法:采用单因素考察法优化桑椹中芦丁的提取条件,采用HPLC法测定芦丁的含量,色谱柱为Agilent Zobax C18(4.6 mm×250 mm,5μm),以乙腈-0.1%磷酸(19∶81)为流动相,流速1.0 mL.min-1,检测波长360 nm,柱温30℃。结果:芦丁最佳提取条件为料液比1∶25,50%乙醇回流60 min,芦丁在0.1～2.0μg有良好线性关系(r=0.999 9)。平均回收率为102.4%,RSD 1.8%(n=6)。结论:该方法简便、准确、可靠,可作为桑椹中芦丁含量测定的方法。     

Melanin-concentrating hormone-1 receptor antagonism and anti-obesity effects of ethanolic extract from Morus alba leaves in diet-induced obese mice

Ethnopharmacological relevance

In Korea, Morus alba leaves have been traditionally administered as natural therapeutic agent for the alleviating dropsy and diabetes.

Aim of the study

The present study was performed to evaluate melanin-concentrating hormone receptor subtype 1 (MCH1) antagonism of the ethanol extract of Morus alba leaves (EMA) and its anti-obesity effect in diet-induced obese (DIO) mice.

Materials and methods

The binding affinity of EMA for the MCH1 receptor with europium-labeled MCH (Eu-MCH), the function of recombinant MCH1 receptors expressed in CHO cells, and the anti-obesity effects in DIO mice were evaluated.

Results

MCH1 receptor binding studies showed, EMA exhibited a potent inhibitory activity with IC₅₀ value of 2.3 ± 1.0 μg/ml. EMA (10–100 μg/ml) also inhibited the intracellular calcium mobilization with the recombinant MCH1 receptors expressed in CHO cells. In an anti-obesity study with DIO mice, long-term oral administrations of EMA for 32 consecutive days produced a dose-dependent decrease in body weight and hepatic lipid accumulation.

Conclusions

These results suggest that chronic treatment with EMA exerts an anti-obesity effect in DIO mice, and its direct MCH1 receptor antagonism may contribute to decrease body weight.     

The production of nitric oxide and prostaglandin E2 in peritoneal macrophages is inhibited by Andrographis paniculata, Angelica sinensis and Morus alba ethyl acetate fractions

Aim of the study

Traditional Chinese medicine herbs (TCMHs) are used in medicines as well as in daily dietary supplements in Asia. In this study, we employed pNF-κB-Luc or pIFN-γ-Luc and BALB/c mice peritoneal macrophages or splenocytes to investigate both the immune and inflammatory effects of six selected plant species.

Materials and Methods

Specifically, we used ethyl acetate fractions of Astragalus membranaceus (Fisch.) Bunge var. mongholicus (Bunge) Hsiao (Fabaceae) (AM), Andrographis paniculata (Burm. f.) Nees (Acanthaceae) (AP), Angelica sinensis (Oliv.) Diels (Apiaceae) (AS), Eucommia ulmodes Oliv. (Eucommiaceae) leaves (EU leaves), Isatis indigotica Fort. (Brassicaceae) (II) and Morus alba L. (Moraceae) (MA).

Results

We found that ethyl acetate fractions of AP, AS and MA significantly decreased NF-κB luciferase activity and also the secretion of NO and PGE₂ in LPS/IFN-γ stimulated mouse peritoneal macrophages (p < 0.05). In contrast, they did not affect IFN-γ luciferase activity or IFN-γ production in concanavalin A (Con A)-activated mouse splenocytes. Our results indicated that the anti-inflammatory properties of these plant extracts might be resulted from the inhibition of pro-inflammatory mediators (e.g., NO and PGE₂), at least in part via suppression of a signaling pathway such as NF-κB.

Conclusions

Collectively, we have found that three potent bioactive TCMH species exerted significant NF-κB inhibitory activity and acted in a cell type dependent fashion.     

Morus alba leaf extract stimulates 5′-AMP-activated protein kinase in isolated rat skeletal muscle

Aim of the study

Morus alba (mulberry) leaf is a natural therapeutic agent that has been shown to have an antidiabetic effect. We explored the possibility that 5′-AMP-activated protein kinase (AMPK) is involved in metabolic enhancement by the Morus alba leaf.

Materials and methods

Isolated rat epitrochlearis muscle was incubated in a buffer containing Morus alba leaf hot water extract (MLE) and the AMPK activation and related events were examined.

Results

In response to MLE treatment, the Thr¹⁷² phosphorylation of the catalytic α subunit of AMPK, an essential step for full kinase activation increased in a dose- and time-dependent manner. Ser⁷⁹ phosphorylation of acetyl CoA carboxylase, an intracellular substrate of AMPK, increased similarly. Analysis of isoform-specific AMPK activity revealed that MLE activated both the α1 and α2 isoforms of the catalytic subunit. This increase in enzyme activity was associated with an increased rate of 3-O-methyl-d-glucose transport in the absence of insulin and with phosphorylation of AS160, a signaling intermediary leading to glucose transporter 4 translocation. The intracellular energy status, estimated from the ATP and phosphocreatine concentrations, was not affected by MLE.

Conclusion

MLE stimulates skeletal muscle AMPK activity acutely without changing the intracellular energy status.     

滇桑叶中的异戊烯基酚类化合物

利用各种色谱技术和波谱手段,从滇桑叶乙醇提取物中分离鉴定了11个异戊烯基酚类化合物,分别为滇桑素G(1),桑查耳酮B(2),柘树咕吨酮M(3),柘树咕吨酮D(4),桑根呋喃B(5),桑辛素D(6),桑辛素C(7),桑辛素Ⅰ(8),去甲基桑辛素Ⅰ(9),桑查耳酮A(10),异补骨脂查耳酮(11).化合物1为新化合物,2～11均为首次从该植物中分离得到.     

广东桑根皮的化学成分研究

目的:研究桑科植物广东桑Morus atropurpurea根皮的化学成分。方法:运用各种色谱方法进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构。结果:从广东桑根皮的70%乙醇提取物分离并鉴定了15个化合物,分别为sanggenol O(1),kuwanon S(2),moracin C(3),mulberrofuran A(4),mulberrofuran B(5),mulberrofuran C(6),mulberrofuran G(7),mulberroside A(8),mulberroside C(9),1-deoxynojirimycin(10),2-O-α-D-galactopyranosyl-1-deoxynojirimycin(11),fagomine(12),白桦酸(13),熊果酸(14)和β-谷甾醇(15)。结论:化合物1~6和8~13为首次从该植物中分离得到。     

白芥子炒制前后HPLC指纹图谱的比较分析

目的:研究建立白芥子不同饮片的指纹图谱测定方法,指认主要色谱峰,分析白芥子炒制前后化学成分的变化情况。方法:采用HPLC,Agilent TC-C18(2)柱,乙腈-0.1%磷酸溶液梯度洗脱,检测波长254 nm,流速1.0 mL.min-1,柱温35℃,以指纹图谱软件计算相似度,并进行图谱比较和指认。结果:各饮片10批次样品平均相似度大于0.96,确定了白芥子生品、炒制品的HPLC标准指纹图谱,并指认了5个主要色谱峰。结论:白芥子炒制前后的HPLC指纹图谱有明显差异,通过2种提取溶剂的比较分析结合色谱峰指认,为揭示白芥子的炒制原理提供了可靠线索。     

桑白皮中1个新的异戊二烯基取代黄酮(英文)

目的:研究桑白皮Morus alba的化学成分。方法:应用硅胶、Sephadex LH-20和Rp-C18柱色谱进行分离纯化,根据化合物的理化常数和波谱数据鉴定其结构。结果:从桑白皮根皮中分离得到10个化合物,分别鉴定为桑根醇P(1),环桑辛素(2),桑辛素(3),桑呋喃G(4),桑根醇A(5),桑根醇L(6),桑根醇N(7),环桑素(8),cyclocommunol(9)和熊果酸(10)。结论:化合物1为新化合物,化合物5,6,7和9为首次从该植物中分离得到。     

长穗桑茎皮中的酚类成分及其抗炎和细胞毒活性

目的:研究长穗桑茎皮中具有抗炎和细胞毒活性的化学成分。方法:采用各种柱色谱对长穗桑茎皮95%乙醇提取物的醋酸乙酯部位进行分离纯化,通过NMR,MS等波谱分析手段鉴定化合物结构。结果:从醋酸乙酯部位中分离得到9个酚类化合物,其中6个黄酮类化合物,3个二苯乙烯类化合物。分别鉴定为槲皮素(1),5,7,3,′4′-四羟基-3-甲氧基黄酮(2),norartocarpanone(3),二氢山柰酚(4),euchrenone a7(5),morachalcone A(6),白藜芦醇(7),高白藜芦醇(8),4′-异戊烯基高白藜芦醇(9)。化合物1~8分别进行了抗炎和细胞毒活性筛选。结论:化合物1~9均为首次从该植物中分离得到。其中化合物6和8浓度在1.0×10-5mol.L-1时对血小板活化因子刺激的多形核白细胞β-葡萄糖苷酸酶释放的抑制率分别为76.8%,94.2%;化合物2和8分别对人卵巢癌细胞(A2780)和人胃癌细胞(BGC-823)有选择性细胞毒活性,IC50分别为0.66,1.31μmol.L-1。     

Anti-obesity effect of Morus bombycis root extract: Anti-lipase activity and lipolytic effect

Aim of the study

This study evaluated anti-obesity effect of the ethanolic extract of Morus bombycis root on lipase activity and lipolysis in adipocytes and adipose tissues.

Materials and methods

Lipase (triacylgycerol acylhydrolase, EC 3.1.1.3) activity was determined by measuring the hydrolysis of p-nitrophenyl butyrate to p-nitrophenol at 405 nm. Lipolytic effects were assayed in fully differentiated 3T3-L1 adipocytes and adipose tissues. In vitro, phosphodiesterase (PDE) activity was also measured.

Results

Morus bombycis root extract exhibited strong anti-lipase activity, with an IC₅₀ value of 2.07 μg/mL. In differentiated adipocytes and adipose tissues, the extract increased lipolytic effects such as decreased intracellular triglyceride and the release of glycerol. Further, the extract inhibited PDE activity in a dose-dependent manner.

Conclusion

The present study suggests that Morus bombycis root extract might be of therapeutic interest with respect to the treatment of obesity.     

桑叶药材HPLC指纹图谱研究

目的: 建立桑叶药材的指纹图谱,为桑叶药材的质量控制提供依据。 方法: 采用HPLC法,Agilent Eclipse XDB-C₁₈(4.6 mm×250 mm,5 μm)色谱柱,以乙腈-1.0%醋酸水为流动相,梯度洗脱,流速为1.0 mL·min^-1,检测波长290 nm,柱温30 ℃,进样10 μL。 结果: 建立了13批桑叶药材的指纹图谱。桑叶合格药材有16个共有峰,多数峰可以达到较好分离,具有较高的相似度。 结论: 建立的高效液相指纹图谱有较好的精密度、重复性和稳定性,可作为桑叶质量评价参考。     

桑白皮中总黄酮含量测定方法研究

目的: 建立一种桑白皮中总黄酮的含量测定方法。 方法: 以桑根酮C为对照品,采用盐酸-镁粉显色体系,于481 nm下测定桑白皮总黄酮含量。 结果: 桑根酮C在146.8～734.0 mg·L^-1与吸光度呈良好线性关系(n=5,r=0.999 8),平均回收率为96.74%,RSD 2.60%(n=6)。 结论: 该含量测定方法准确、简便、经济,是一种较理想的测定桑白皮中总黄酮含量的方法。     

石松生物碱化学成分的研究

目的:研究石松Lycopodium japonicum生物碱化学成分。方法:采用硅胶柱色谱,RP-C18反相柱色谱,SephadexLH-20柱色谱,Waters半制备液相色谱等方法分离纯化,根据理化性质和波谱数据鉴定化合物的结构。结果:从石松中分离并鉴定了9个生物碱化学成分,分别为lycodoline(1),lucidioline(2),α-obscurine(3),lycopodine(4),lycoposerramine-L(5),lyco-poserramine-M(6),11α-O-acetyl-lycopodine(7),des-N-methyl-α-obscurine(8),clavolonine(9),其中化合物4～9为首次报道从石松中分离得到。     

荷梗中的细胞毒活性生物碱

研究植物莲Nelumbo nucifera Gaertn干燥茎的生物碱类成分及其细胞毒活性,为进一步开发利用荷梗提供依据。采用离子交换树脂、硅胶和Sephadex LH-20柱色谱等方法分离纯化,并运用波谱方法对所分离的化合物进行结构鉴定。采用MTT法对所分离得到的化合物进行HL-60癌细胞毒活性实验。从荷梗总生物碱提取物中分离鉴定了15个生物碱类化合物,分别为阿西米洛宾（1）、异乌药碱（2）、N-乙酰基去甲杏黄罂粟碱（3）、厚壳桂素（4）、velucryptine（5）、pycnarrhine（6）、鹅掌楸碱（7）、荷叶碱（8）、降荷叶碱（9）、杏黄罂粟碱（10）、N-甲基阿西米洛宾（11）、乌药碱（12）、N-去甲杏黄罂粟碱（13）、N-甲基乌药碱（14）、观音莲明（15）。化合物 1~7,12~15 为首次从荷梗中分离得到。化合物 2~6 为首次从莲科植物中分离得到。在样品溶液浓度为1×10^-5 mol·L^-1的条件下,化合物 7~10,13,14 对HL-60癌细胞体外生长的抑制率分别是51.36%,59.09%,52.51%,53.93%,51.43%和64.31%,表明上述化合物对人早幼粒细胞白血病HL-60细胞具有较明显的体外细胞毒活性。     

中药茺蔚子中一个新C-28降三萜

目的:研究益母草Leonurus japonicus果实茺蔚子中的化学成分。方法:茺蔚子乙酸乙酯部位经硅胶,RP-18,Sephadex LH-20和HPLC等色谱技术分离纯化,根据理化常数和波谱数据鉴定化合物的结构。结果:分离鉴定了2个具有特殊骨架的28位去甲基齐墩果烷型螺环三萜。结论:化合物1为新化合物,命名为茺蔚子三萜A(leonujaponin A),化合物2为已知化合物,鉴定为phlomistetraol B,均为首次从益母草属植物中分离得到。     

Antimicrobial activity of the methanolic extracts and compounds from Treculia obovoidea (Moraceae)

The crude extract from Treculia obovoidea was subjected to purification by repeated chromatography. Eight compounds were isolated from Treculia obovoidea and identified as Psoralen (1), Bergapten (2), 7-methoxycoumarin (3), 7-hydroxycoumarin (4), 4,2′,4′-trihydroxychalcone (5), 4,2′,4′-trihydroxy-3-prenylchalcone (6), 3-hydroxy-4-methoxybenzoic acid (7) and O-[3-(2,2-dimethyl-3-oxo-2H-furan-5-yl) butyl] bergaptol (8). These compounds together with the extract were tested for their antimicrobial activity against Gram-positive bacteria (six species), Gram-negative bacteria (12 species) and three Candida species using micro-dilution methods for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC). The MIC values obtained with the crude extracts varied from 78.12 to 156.25 μg/ml against 17 (80.95%) of the 21 tested microorganisms. All the isolated compounds showed selective activity. The antimicrobial activity of this plant as well as that of compounds 6 and 8 is being reported for the first time. The obtained results provide promising baseline information for the potential use of these crude extract as well as some of the isolated compounds in the treatment of bacterial and fungal infections.     

辣椒黄酮苷A的化学结构

该文对辣椒Capsicum annuum果实进行化学成分研究,采用多种色谱技术(硅胶,Sephadex LH-20,MCI GEL CHP-20P,HPLC等) 分离纯化,根据波谱学数据(UV,IR,MS,1D-和2D-NMR) 进行结构鉴定.从辣椒果实中分离得到5个化合物,结构分别鉴定为辣椒黄酮苷A(1),尿苷(2),腺苷(3),7-羟基-6-甲氧基桂皮酸乙酯(4) 和7-羟基桂皮酸乙酯(5).其中,化合物1为新化合物,其化学结构为木犀草素-7-O-[2″-O-(5'-O-芥子酰基)-β-D-芹糖]-β-D-葡萄糖苷,命名为辣椒黄酮苷A.化合物2~5为首次从该植物中分离得到.