Role of Rubia cordifolia Linn. in radiation protection

The radioprotective potential of alcoholic extract of root of R. cordifolia, was studied by survival, hemopoietic cell protection and micronucleus assay. The LD50 value for the alcoholic root extract was found to be 1200 mg/kg body weight at 72 hr post irradiation. A significant radiation protection (67%) as assessed by increased animal survival was observed when R. cordifolia (RC) extract was administered intraperitoneally, 90 min. before the radiation exposure. Besides, the extract also inhibited radiation induced lipid peroxidation measured by the inhibition of thiobarbituric acid reactive substance (TBARS). The RC extract at a selected dose of 460 mg/kg body weight was effective in protecting the radiation induced suppression of endogenous colony forming units in spleen. A significant inhibition of radiation (2 Gy) induced micronuclei formation was observed when RC extract was administered 90 min prior to irradiation. Thus, it appears that the alcoholic root extract of R. cordifolia provides significant protection against radiation induced lipid peroxidation, hemopoietic injury and genotoxicity. The mechanism of action of RC extract appears to be through its anti-oxidant, metal chelation and anti-inflammatory property.     

Antihyperglycemic, antistress and nootropic activity of roots of Rubia cordifolia Linn

Effect of alcoholic extract of roots of Rubia cordifolia was studied on elevated blood glucose level in alloxan treated animals. The extract reduced the blood sugar level raised by alloxan. Effect of alcoholic extract was also investigated on cold restraint induced stress and on scopolamine-induced memory impairment. Alcoholic extract enhanced brain gamma-amino-n-butyric acid (GABA) levels and decreased brain dopamine and plasma corticosterone levels. Acidity and ulcers caused due to cold restraint stress were inhibited by alcoholic extract. Animals treated with alcoholic extract spent more time in open arm in elevated plus maze model. It also antagonized scopolamine induced learning and memory impairment. Baclofen induced catatonia was potentiated by alcoholic extract.     

Two pentacyclic triterpenes from Rubia cordifolia

Rubicoumaric acid and rubifolic acid isolated from Rubia cordifolia have been shown to be 30-hydroxy-3β-p-hydroxycoumaryloxy-urs-12-ene-28-oic acid and 3β,30-dihydroxy-urs-12-ene-28-oic acid(30-hydroxyursolic acid) respectively on the basis of ¹H NMR, ¹³C NMR and mass spectral and chemical evidence.     

茜草内生菌的分离鉴定及其抗菌活性物质研究

对中药植物茜草(Rubia cordifoliaL)的内生菌进行了分离和抗菌活性筛选,获得一株具有广谱抗菌活性的内生细菌。该细菌对常见的3种人类病原菌和4种植物病原菌具有拮抗作用。传统分类学和基于16S rRNA基因的分子分类学证据表明,该内生细菌为一株新的枯草芽孢杆菌,命名为Bacillus subtilisRC4。B.subtilisRC4在综合马铃薯培养基(pH值5.0)中于28℃振荡培养60h,产生的代谢物对白色念珠菌的抗菌活性最强。抗菌活性物质在100℃受热20min,活性维持80%以上,且在pH值2.0~11.0范围内稳定。经硅胶柱层析和高效液相色谱分离,得到主要抗菌活性化合物,质谱分析表明其分子量约为288Da。     

茜草叶绿体全基因组序列及其系统发育分析

以茜草科(Rubiaceae)植物茜草(Rubia cordifolia L.)为研究对象,采用Illumination高通量测序技术对其叶绿体全基因组进行测序,并运用MAGA11等生信学工具进行全基因组解析及系统发育分析。结果表明,(1)茜草叶绿体基因组呈典型的四分环状结构,总GC含量37.2%,长153 959 bp,其中包含大单拷贝(LSC)区83 844 bp、小单拷贝(SSC)区17 083 bp和2个反向重复(IR)区26 516 bp;共注释得到124个基因,包括79个蛋白质编码基因、37个tRNA和8个rRNA。(2)序列共鉴定到169个SSR位点,以A、T组成为主,包括129个单核苷酸、18个双核苷酸、11个三核苷酸、9个四核苷酸和2个五核苷酸,六核苷酸SSR未检测到;边界分析显示,茜草叶绿体基因组LSC区差异性最大,变异程度最高,而IRa区则差异性最小,最为保守。(3)最大似然法(ML)构建系统发育树显示,样品茜草与同属植物Rubia horrida以100%支持率聚为一类,茜草亚科、仙丹花亚科与金鸡纳亚科聚为姐妹类群,证明茜草科植物在进化过程中保守发育。     

茜草根、茎、叶多糖含量分析

采用苯酚一硫酸法[1]测定茜草根、茎、叶多糖含量为根、0.23%;茎、0.15%;叶、1.67%.并对根茎叶多糖含量进行分析比较,其结果表明:茜草叶的多糖含量最高,其次为根,茎最少,结果显示叶中的多糖含量是根中的7～8倍.     

中低压制备色谱制备茜草蒽醌成分的研究

建立新的中低压制备色谱技术,分离纯化茜草蒽醌单体.先采用高压液相色谱技术分析所分离产物的纯度,再用核兹共振谱、红外、质谱分析确证单体的化学结构.结果表明:用中低压色谱分离茜草的乙醇提取物而得到的4个单体,其纯度分别为99.87％、99.56％、99.42％、98.21％,结构鉴定为从石油醚萃取物中分离得到的单体为大叶茜...     

O-Seco-RA-XXIV,a possible precursor of an antitumor peptide RA-XXIV,from Rubia cordifolia L.

O-Seco-RA-XXIV, a new cyclic peptide, cyclo-(d-alanyl-l-glutaminyl-N,O-dimethyl-l-tyrosyl-l-alanyl-N-methyl-l-tyrosyl-N-methyl-l-tyrosyl), was isolated from the roots of Rubia cordifolia L. along with RA-XXIV. Its structure and relative stereochemistry were determined by interpretation of the spectroscopic data and X-ray crystallography, and its absolute stereochemistry by the Marfey's amino acid analysis of its acid hydrolysate. Isolation of the two peptides from the same plant source may indicate that O-seco-RA-XXIV is a possible precursor of RA-XXIV and that the formation of the diphenyl ether linkage in the cycloisodityrosine moiety is to be formed after the formation of the cyclohexapeptide chain in this series of peptides.     

A novel bicyclic hexapeptide, RA-XVIII, from Rubia cordifolia: structure, semi-synthesis, and cytotoxicity

A new bicyclic peptide of RA-series, RA-XVIII (3), was isolated from the roots of Rubia cordifolia L. Its structure was established to be a hydroxylated derivative of RA-VII by the semi-synthesis of 3 from deoxybouvardin, and its cytotoxicity against P-388 cells was 0.012 microg/mL.     

Comparison of the antioxidant action of the alcoholic extract of Rubia cordifolia with rubiadin.

The inhibition of FeSO4 induced lipid peroxidation in rat liver by alcoholic extract of Rubia cordifolia and by one of its constituent rubiadin (1, 3-dihydroxy-2-methyl anthraquinone) (pure form) has been compared. Both have been found to inhibit lipid peroxidation in a dose dependent manner. Whereas the former shows both oxidising and reducing properties with Fe2+ and Fe3+, the latter shows oxidising property only by converting Fe2+ to Fe3+. The former inhibits the oxidation of reduced glutathione while the latter does not.     

Effect of Rubia cordifolia, Fagonia cretica linn, and Tinospora cordifolia on free radical generation and lipid peroxidation during oxygen-glucose deprivation in rat hippocampal slices

The major damaging factor during and after the ischemic/hypoxic insult is the generation of free radicals, which leads to apoptosis, necrosis, and ultimately cell death. Rubia cordifolia (RC), Fagonia cretica linn (FC), and Tinospora cordifolia (TC) have been reported to contain a wide variety of antioxidants and have been in use in the eastern system of medicine for various disorders. Hippocampal slices were subjected to oxygen-glucose deprivation (OGD) and divided into three groups, control, OGD, and OGD+drug treated. Cytosolic reduced glutathione (GSH), nitric oxide [NO, measured as nitrite (NO2)]. EPR was used to establish the antioxidant effect of RC, FC, and TC with respect to superoxide anion (O*2-), hydroxyl radicals (*OH), nitric oxide (NO) radical, and peroxynitrite anion (ONOO-) generated from pyrogallol, menadione, DETA-NO, and Sin-1, respectively. RT-PCR was performed for the three herbs to assess their effect on the expression of gamma-glutamylcysteine ligase (GCLC), iNOS, and GAPDH gene expression. All the three herbs were effective in elevating the GSH levels and expression of the GCLC. The herbs also exhibited strong free radical scavenging properties against reactive oxygen and nitrogen species as revealed by electron paramagnetic resonance spectroscopy, diminishing the expression of iNOS gene. RC, FC, and TC therefore attenuate oxidative stress mediated cell injury during OGD and exert the above effects at both the cytosolic as well as at gene expression levels and may be effective therapeutic tool against ischemic brain damage.     

Suppression of reactive oxygen species and enhanced stress tolerance in Rubia cordifolia cells expressing the rolC oncogene

It is known that expression of the Agrobacterium rhizogenes rolC gene in transformed plant cells causes defense-like reactions, such as increased phytoalexin production and expression of pathogenesis-related proteins. In the present study, we examined whether this phenomenon is associated with increased production of reactive oxygen species (ROS). Single-cell assays based on confocal microscopy and fluorogenic dyes (2,7-dichlorofluorescein diacetate and dihydrorhodamine 123) showed reduced steady-state levels of ROS in rolC-expressing Rubia cordifolia cells as compared with normal cells. Paraquat, a ROS inducer, caused significant ROS elevation in normal cells but had little effect on rolC-transformed cells. Likewise, ROS elevation triggered by a light stress was suppressed in transformed cells. Our results indicate that the rolC gene acts as a ROS suppressor in unstressed cells and its expression prevents stress-induced ROS elevations. We detected a two- to threefold increase in tolerance of rolC-transformed cells to salt, heat, and cold treatments. Simultaneously, rolC-transformed cells maintained permanently active defensive status, as found by measuring isochorismate synthase gene expression and anthraquinone production. Thus, the oncogene provoked multiple effects in which ROS production and phytoalexin production were clearly dissociated.     

Network pharmacology-based research on the active component and mechanism of the antihepatoma effect of Rubia cordifolia L.

Rubia cordifolia L. is widely used in Asia and its antihepatoma effect has been proved by in vitro and in vivo experiments. However, there are few studies on its specific mechanism. In the present study, the network pharmacology method was used to construct the component/target/pathway molecular regulatory network for the antihepatoma effect of Rubia cordifolia L. to explore the effective components of Rubia cordifolia L. and its potential mechanism. The chemical components of Rubia cordifolia L. were identified through literature and databases, and the components were evaluated and screened by drug likeness and pharmacokinetic characteristics (ADMET). The targets of active components were predicted according to the reverse pharmacophore matching model. The hepatic carcinoma-related genes were found in databases, and antihepatoma-related gene targets were selected through comparison. The functions of target genes and related pathways were analyzed and screened using the Database for Annotation, Visualization and Integrated Discovery, and the component/target/pathways network of antihepatoma effect of Rubia cordifolia L. was constructed using Cytoscape software. Finally, 16 active compounds were screened from Rubia cordifolia L., and 39 gene targets, including AKT1, mitogen-activated protein kinase 1, and epidermal growth factor receptor, were involved. Rubia cordifolia L. also affected the hepatitis B, phosphoinositide-3-kinase-protein kinase B, and mitogen-activated protein kinase signaling pathways. Many direct-acting tumor-related signaling pathways and indirect-acting hepatitis pathways inhibit the generation of liver cancer. The present study provided a scientific basis for further elucidating the mechanism of Rubia cordifolia L. against liver cancer.     

Induction of anthraquinone biosynthesis in Rubia cordifolia cells by heterologous expression of a calcium-dependent protein kinase gene

Calcium-dependent protein kinases (CDPKs) play an important role in plant cell responses to stress and pathogenic attack. In this study, we investigated the effect of heterologous expression of the Arabidopsis CDPK gene, AtCPK1, on anthraquinone production in transgenic Rubia cordifolia cells. AtCPK1 variants (a constitutively active, Ca(2+) -independent form and a non-active form used as a negative control) were transferred to callus cells by agrobacterial transformation. Overexpression of the constitutively active, Ca(2+) -independent form in R. cordifolia cells caused a 10-fold increase in anthraquinone content compared with non-transformed control cells, while the non-active form of AtCPK1 had no effect on anthraquinone production. Real-time PCR measurements showed that the activation of anthraquinone biosynthesis in transgenic calli correlated with the activation of isochorismate synthase gene expression. The activator effect of AtCPK1 was stable during prolonged periods of transgenic cell cultivation (more than 3 years) and the transgenic cultures exhibited high growth. Our results provide the first evidence that a CDPK gene can be used for the engineering of secondary metabolism in plant cells.     

Pistagremic acid a new leishmanicidal triterpene isolated from Pistacia integerrima Stewart

The present study was designed to investigate the whole plant of Pistacia integerrima Stewart in order to examine the pharmacological basis of the use of the plant in folk medicine for the treatment of infectious diseases and disorder. Phytochemical and pharmacological studies led to the isolation of a new triterpene pistagremic acid (3-methyl-7-(4,4,10,13,14-pentamethyl-3-2,3,4,5,6,7,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-oct-3-enoic). Pistagremic acid showed significant leishmanicidal activity (IC(50): 6.71 ± 0.09 μM) against Leishmania major (DESTO) promastigotes in comparison to standard compound amphotericin B (IC(50): 0.21 ± 0.06 μM).     

Anticonvulsant potential of holy basil, Ocimum sanctum Linn., and its cultures

Callus cultures from stem of O. sanctum were induced on slightly modified Murashige and Skoog's (MS) medium and supplemented with 2,4-dichlorophenoxyacetic acid (2,4-D, 1-2 ppm) and kinetin (kn, 1 ppm). Different extractives of stem, leaf and stem callus of O. sanctum were tested for anticonvulsant activity against standard drug phenytoin using maximal electroshock (MES) model. Ethanol and chloroform extractives of stem, leaf and stem calli were effective in preventing tonic convulsions induced by transcorneal electroshock.     

Structure of acacigenin-B,a novel triterpene ester isolated from Acacia concinna

The structure of acacigenin-B, a novel ester genin from the pods of Acacia concinna was established from its PMR and ¹³ C NMR spectra. It was identified as the 21-hydroxy ester of acacic acid; the esterifying acid was a hitherto unknown monoterpene acid of tetrahydrofuranoid structure. This appears to be the first report of a higher terpenoid forming an ester with a monoterpene acid     

茜草对II型单纯疱疹病毒的体外生长抑制作用

茜草为常用中药。本研究发现,茜草的甲醇提取物在体外细胞培养上对HSV-2有明显的抑制作用。在Vero细胞上,病毒抑制数可达3个对数。病毒增殖抑制实验表明,该制剂确实抑制了HSV-2感染性病毒颗丝的产生。在不同的细胞系上进行比较,发现该制剂的抗病毒作用具有明显的细胞系依赖性。本文认为,茜草的甲醇提取物具有抑制HSV-2的作用,但其有效成分为何种,尚待进一步研究。     

The interaction of Rubia cordifolia with iron redox status: a mechanistic aspect in free radical reactions.

The present publication investigates the antioxidant property and mechanistic aspect of alcoholic extract of R. cordifolia. The extract of R. cordifolia has shown significant inhibitory effect on FeSO4 induced lipid peroxidation. Study with iron redox status showed that R. cordifolia extract reduced or oxidixed; Fe3+ or Fe2+ respectively, in a dose dependent manner. Results with superoxide anion (O2-.) and hydroxyl radical (OH.), showed no radical scavenging activity. The alcoholic extract significantly maintains the reduced glutathione content both in time and dose dependent manner. It also reduced the rate of depletion of reduced glutathione (GSH) level in presence of ferrous sulphate (FeSO4) and cumene hydroperoxide (CHP). On the basis of these observations, it can be concluded that the antioxidant property of R. cordifolia is due to a direct interaction with iron.