Study of chemical composition and antimicrobial activity of leaves and roots of Scrophularia ningpoensis.
Li Jing,Huang Xiaoyan,Du Xianjie,Sun Wenji,Zhang Yongmin
Natural product research
Two saponins: scrokoelziside A (1), scrokoelziside B (2), one iridoid glycoside, eurostoside (3), and two flavonoids: nepitrin (4) and homoplantaginin (5), were isolated from the leaves of Scrophularia ningpoensis for the first time. Moreover, eight known compounds: cane sugar (6), harpagide (7), aucubin (8), 6-O-methylcatalpol (9), harpagoside (10), angoroside C (11), beta-sitosterol (12) and beta-sitosterol glucoside (13) were isolated from the roots of S. ningpoensis. Furthermore, the antimicrobial activity of the extracts of the leaves of S. ningpoensis and the 10 compounds (1, 2, 3, 4, 5, 7, 8, 9, 10, 11) was studied in vitro against eight reference strains of bacteria by using the disc-diffusion method and micro-well dilution assay. The extracts of leaves and scrokoelziside A are effective against beta-haemolytic streptococci but had no effect against other strains. The extract of roots and other compounds showed no activity against all bacterial strains at the test concentration.
10.1080/14786410802696247
Dynamic analysis of secondary metabolites in various parts of Scrophularia ningpoensis by liquid chromatography tandem mass spectrometry.
Xie Guoyong,Jiang Yuxuan,Huang Mengmeng,Zhu Yan,Wu Gang,Qin Minjian
Journal of pharmaceutical and biomedical analysis
The roots of Scrophularia ningpoensis are used as traditional medicines for thousands of years in China, nevertheless the stems and leaves were discarded as non-medicinal parts. Modern research have indicated the chemical constituents in the stems and leaves are similar to the identified in the roots, and the therapeutic effects of stems and leaves are superior to roots for some disease. In the study, the chemical constituents in roots, stems and leaves of S. ningpoensis were analyzed qualitatively by HPLC-Q-TOF-MS/MS. 40 compounds including 17 iridoid glycosides, 15 phenylpropanoids and 8 flavonoids were identified. Meantime, the dynamic accumulations of six index constituents in various parts were measured by HPLC-DAD. The results indicated the S. ningpoensis stems contained high content of aucubin (30.09 mg/g) and harpagide (28.4 mg/g) in August, and the leaves contained high content of harpagoside (12.02 mg/g) in July. The study provides the basis for the full development and utilization of the resource of stems and leaves from S. ningpoensis.
10.1016/j.jpba.2020.113307
Neuroprotective phenylpropanoid esters of rhamnose isolated from roots of Scrophularia buergeriana.
Kim S R,Kim Y C
Phytochemistry
Four phenylpropanoid esters of rhamnose, buergerisides A1, B1, B2 and C1 were isolated from roots of Scrophularia huergeriana MIQ. (Scrophulariaceae), and were characterized as 2-O-acetyl-3,4-di-O-(E)-p-methoxycinnamoyl-alpha-L-rhamnopyranosid e, 2-O-acetyl-3-O-(E)-p-methoxycinnamoyl-alpha-L-rhamnopyranoside, 2-O-acetvl-3-O-(Z)-p-methoxycinnamoyl-alpha-L-rhamnopyranosi de and 4-O-(E)-p-methoxycinnamoyl-alpha-L-rhamnopyranoside, respectively. In addition, six known phenylpropanoids were authenticated as: (E)-cinnamic acid, (E)-p-methoxycinnamic acid, (E)-p-methoxycinnamic acid methyl ester, (E)-p-coumaric acid, (E)-caffeic acid, (E)-ferulic acid and a phenylalcohol, 2-(3-hydroxy-4-methoxyphenyl)ethanol. These ten phenylpropanoids all attenuated glutamate-induced neurotoxicity when added to primary cultures of rat cortical cells in a dose-dependent manner. These results demonstrate that phenylpropanoids isolated from S. buergeriana may exert significant protective effects against glutamate-induced neurodegeneration in primary cultures of cortical neurons.
Synergistic nourishing 'Yin' effect of iridoid and phenylpropanoid glycosides from Radix Scrophulariae in vivo and in vitro.
Gong Pu-Yang,He Yu-Wei,Qi Jin,Chai Cheng-Zhi,Yu Bo-Yang
Journal of ethnopharmacology
ETHNOPHARMACOLOGICAL RELEVANCE:Radix Scrophulariae (RS), is a renowned traditional Chinese medicine used as nourishing 'Yin'. The iridoid glycosides (IG) and phenylpropanoid glycosides (PG) are main chemical constituents in RS. However, there had been no pharmacological experiment studies of synergy between IG and PG. Due to the constituents interactions, exploring their synergy profile is of great important for explaining the essence of nourishing 'Yin' efficacy of RS. AIM OF STUDY:The present study was undertaken to evaluate synergistic nourishing 'Yin' effect of IG and PG from RS in vivo and in vitro through their immunoregulation and antioxidant activities. MATERIALS AND METHODS:In this study, IG and PG fractions in RS were isolated and identified by High Performance Liquid Chromatography coupled with tandem quadrupole time-of-flight Mass Spectrometry (HPLC-Q-TOF-MS). The synergistic nourishing 'Yin' effect of two fractions were investigated in vivo and in vitro with thyroxine-induced 'Yin' deficiency (YD) mice model and primary splenic lymphocyte, respectively. The exterior syndrome signs and serologic and cellular biomarkers changes were detected. Then, the synergistic coefficient (SC) of IG and PG on every pharmacodynamics index were calculated by Webb method. RESULTS:Compared with model and mono-therapy group (IG or PG group), IG combined with PG group significantly ameliorated YD by exerting immunoregulation and antioxidant effects. Based on the SC, IG and PG possessed a synergistic effect on heart rate, average speed, upright times, spleen index, LPO, SOD, IL-6, Na-K-ATP enzyme in vivo, and cAMP/cGMP, IFN-γ/IL-10, and MDA in vitro with SC > 1. CONCLUSIONS:The nourishing 'Yin' benefits were clearly produced when IG and PG were used in combination, which provided the scientific evidence of multiple-components and multiple-approach synergistic effect of Chinese traditional herbal medicine to control and management of diseases.
10.1016/j.jep.2019.112209
Influence of processing procedure on the quality of Radix Scrophulariae: a quantitative evaluation of the main compounds obtained by accelerated solvent extraction and high-performance liquid chromatography.
Cao Gang,Wu Xin,Li Qinglin,Cai Hao,Cai Baochang,Zhu Xuemei
Journal of separation science
An improved high-performance liquid chromatography with diode array detection combined with accelerated solvent extraction method was used to simultaneously determine six compounds in crude and processed Radix Scrophulariae samples. Accelerated solvent extraction parameters such as extraction solvent, temperature, number of cycles, and analysis procedure were systematically optimized. The results indicated that compared with crude Radix Scrophulariae samples, the processed samples had lower contents of harpagide and harpagoside but higher contents of catalpol, acteoside, angoroside C, and cinnamic acid. The established method was sufficiently rapid and reliable for the global quality evaluation of crude and processed herbal medicines.
10.1002/jssc.201401141
Iridoid glycosides from Radix Scrophulariae attenuates focal cerebral ischemia‑reperfusion injury via inhibiting endoplasmic reticulum stress‑mediated neuronal apoptosis in rats.
Chen Yanyue,Zhang Lei,Gong Xueyuan,Gong Hengpei,Cheng Rubin,Qiu Fengmei,Zhong Xiaoming,Huang Zhen
Molecular medicine reports
Iridoid glycosides of Radix Scrophulariae (IGRS) are a group of the major bioactive components from Radix Scrophulariae with extensive pharmacological activities. The present study investigated the effects of IGRS on cerebral ischemia‑reperfusion injury (CIRI) and explored its potential mechanisms of action. A CIRI model in rats was established by occlusion of the right middle cerebral artery for 90 min, followed by 24 h of reperfusion. Prior to surgery, 30, 60 or 120 mg/kg IGRS was administered to the rats once a day for 7 days. Then, the neurological scores, brain edema and volume of the cerebral infarction were measured. The apoptosis index was determined by terminal deoxynucleotidyl transferase mediated dUTP nick end labeling. The effects of IGRS on the histopathology of the cortex in brain tissues and the endoplasmic reticulum ultrastructure in the hippocampus were analyzed. Finally, the expression of endoplasmic reticulum stress (ERS)‑regulating mediators, endoplasmic reticulum chaperone BiP (GRP78), DNA damage‑inducible transcript 3 protein (CHOP) and caspase‑12, were detected by reverse transcription quantitative polymerase chain reaction (RT‑qPCR) and western blot analysis. The volume of cerebral infarction and brain water content in the IGRS‑treated groups treated at doses of 60 and 120 mg/kg were decreased significantly compared with the Model group. The neurological scores were also significantly decreased in the IGRS‑treated groups. IGRS treatment effectively decreased neuronal apoptosis resulting from CIRI‑induced neuron injury. In addition, the histopathological damage and the endoplasmic reticulum ultrastructure injury were partially improved in CIRI rats following IGRS treatment. RT‑qPCR and western blot analysis data indicated that IGRS significantly decreased the expression levels of GRP78, CHOP and caspase‑12 at both mRNA and protein levels. The results of the present study demonstrated that IGRS exerted a protective effect against CIRI in brain tissue via the inhibition of apoptosis and ERS.
10.3892/mmr.2019.10833
[Identification of chemical constituents in Scrophulariae Radix by HPLC-IT-TOF-MS].
Wang Jing-Zhe,Xu Feng,Liu Zhen,Ma Li-Man,Shang Ming-Ying,Liu Guang-Xue,Cai Shao-Qing
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica
This experiment was performed to establish a qualitative analysis on chemical constituents of Scrophulariae Radix by HPLC-ESI-IT-TOF-MS．The analysis was conducted on a C₁₈ column (Kromasil 100-5, 4.6 mm×250 mm, 5 μm) with 0.1% formic acid-acetonitrile as the mobile phase for gradient elution; ESI ion source was used for mass spectra, and data were collected innegative and positive modes. The results showed that 64 compounds from Scrophulariae Radix had been identified by analyzing negative ion mass data including element composition and by comparing with data from literature. Two new compounds (4-hydroxy-6-O-methylcatalpol and acetylangoroside C) and seventeen known compounds were detected from Scrophulariae Radix for the first time. Seventeen known compounds included twelve iridoid glycosides, three phenylpropanoid glycosides and two other kind compounds. This study will provide chemical basis for elucidation of the effective substance in the Scrophulariae Radix.
10.4268/cjcmm20160717
Simultaneous Determination of Iridoid Glycosides, Phenylpropanoid Glycosides, Organic Acids, Nucleosides and Amino Acids in Scrophulariae Radix Processed by Different Processing Methods by HPLC-QTRAP-MS/MS.
Wang Shengnan,Wang Qin,Yin Xiaoqin,Chen Bohua,Liu Xunhong
Journal of chromatographic science
Scrophulariae Radix is one of the widely used traditional Chinese medicines. In this study, a high-performance liquid chromatography coupled with triple quadrupole-linear ion trap mass spectrometry method was established for the simultaneous determination of multiple bioactive constituents including four iridoid glycosides, two phenylpropanoid glycosides, six organic acids, 11 nucleosides and 16 amino acids in Scrophulariae Radix. The validated method was used to analyze nine Scrophulariae Radix samples processed by different processing methods. In addition, Grey relational analysis and DTOPSIS were used to evaluate the samples according to the content of 39 ayalytes. The results showed that the quality of Scrophulariae Radix processed by cutting into slices, sun drying and "sweating" methods were better. All the results proved that the developed method was available and could be used to evaluate the quality of Scrophulariae Radix.
10.1093/chromsci/bmab056
New Iridoids from Scrophularia ningpoensis.
Ma Qing-Juan,Han Li,Mu Yu,Guan Pei-Pei,Lei Hui,Wang Zhan-You,Huang Xue-Shi
Chemical & pharmaceutical bulletin
Five new compounds including five iridoids (1-5) and six known compounds were isolated from the rhizomes of Scrophularia ningpoensis. Their structures were determined by extensive NMR and IR, MS spectroscopic data analyses. The anti-inflammatory, antibacterial, antifungal, and cytotoxic activities of the isolated compounds were evaluated. Compound 11 exhibited significant inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophage cells.
10.1248/cpb.c17-00163
Molecular Insights into the Macrophage Immunomodulatory Effects of Scrophulariae Radix Polysaccharides.
Chemistry & biodiversity
Scrophulariae Radix (SR) has been widely used in Chinese herbal compound prescriptions, health care products and functional foods. The present study aimed to investigate the immunomodulatory activity of polysaccharides from SR (SRPs) in macrophages and explore the potential mechanisms. The results showed that four SRPs fractions (SRPs40, SRPs60, SRPs80 and SRPs100) had similar absorption peaks and monosaccharide compositions, but the intensities of absorption peaks and monosaccharide contents were distinguished. All SRPs fractions significantly enhanced the pinocytic activity, promoted the production of NO and TNF-α, increased the mRNA expressions of inflammatory factors (IL-1β, IL-6, TNF-α and PTGS2) and TLR2, and elevated the phosphorylation levels of p38, ERK, JNK, p65 and IκB. Moreover, the production of NO and TNF-α stimulated by SRPs was dramatically suppressed by anti-TLR2 antibody. These results indicated that SRPs activated macrophages through MAPK and NF-κB signaling pathways via recognition of TLR2.
10.1002/cbdv.202301180
Radix Scrophulariae extracts (harpagoside) suppresses hypoxia-induced microglial activation and neurotoxicity.
Sheu Shiow-Yunn,Hong Yi-Wen,Sun Jui-Sheng,Liu Man-Hai,Chen Ching-Yun,Ke Cherng-Jyh
BMC complementary and alternative medicine
BACKGROUND:Hypoxia could lead to microglia activation and inflammatory mediators' overproduction. These inflammatory molecules could amplify the neuroinflammatory process and exacerbate neuronal injury. The aim of this study is to find out whether harpagoside could reduce hypoxia-induced microglia activation. METHODS:In this study, primary microglia cells harvested from neonatal ICR mice were activated by exposure to hypoxia (1 % O2 for 3 h). Harpagoside had been shown to be no cytotoxicity on microglia cells by MTT assay. The scavenger effect of harpagoside on hypoxia-enhanced microglial cells proliferation, associated inflammatory genes expression (COX-II, IL-1β and IL-6 genes) and NO synthesis were also examined. RESULTS:Hypoxia enhances active proliferation of microglial cells, while harpagoside can scavenge this effect. We find that harpagoside could scavenge hypoxia-enhanced inflammatory genes expression (COX-2, IL-1β and IL-6 genes) and NO synthesis of microglial cells. Under 3 h' hypoxic stimulation, the nuclear contents of p65 and hypoxia inducible factor-1α (HIF-1α) significantly increase, while the cytosol IκB-α content decreases; these effects can be reversed by 1 h's pre-incubation of 10(-8) M harpagoside. Harpagoside could decrease IκB-α protein phosphorylation and inhibit p65 protein translocation from the cytosol to the nucleus, thus suppress NF-κB activation and reduce the HIF-1α generation. CONCLUSION:These results suggested that the anti-inflammatory mechanism of harpagoside might be associated with the NF-κB signaling pathway. Harpagoside protect against hypoxia-induced toxicity on microglial cells through HIF-α pathway.
10.1186/s12906-015-0842-x
Comparison of Chemical Constituents in Scrophulariae Radix Processed by Different Methods based on UFLC-MS Combined with Multivariate Statistical Analysis.
Wang Shengnan,Hua Yujiao,Zou Lisi,Liu Xunhong,Yan Ying,Zhao Hui,Luo Yiyuan,Liu Juanxiu
Journal of chromatographic science
Scrophulariae Radix is one of the most popular traditional Chinese medicines (TCMs). Primary processing of Scrophulariae Radix is an important link which closely related to the quality of products in this TCM. The aim of this study is to explore the influence of different processing methods on chemical constituents in Scrophulariae Radix. The difference of chemical constituents in Scrophulariae Radix processed by different methods was analyzed by using ultra fast liquid chromatography-triple quadrupole-time of flight mass spectrometry coupled with principal component analysis and orthogonal partial least squares discriminant analysis. Furthermore, the contents of 12 index differential constituents in Scrophulariae Radix processed by different methods were simultaneously determined by using ultra fast liquid chromatography coupled with triple quadrupole-linear ion trap mass spectrometry. Gray relational analysis was performed to evaluate the different processed samples according to the contents of 12 constituents. All of the results demonstrated that the quality of Scrophulariae Radix processed by "sweating" method was better. This study will provide the basic information for revealing the change law of chemical constituents in Scrophulariae Radix processed by different methods and facilitating selection of the suitable processing method of this TCM.
10.1093/chromsci/bmx090