Traditional Chinese medicine Scrophulariae Radix, which is also called Yuan Shen, black Shen, is the dried root of Scrophularia ningpoensis of the Scrophulariaceae family. Research has indicated that the chemical constituents of Scrophulariae Radix mainly include terpenoids, phenylpropanoids, organic acids, volatile oils, steroids, sugars, flavonoids, alkaloids and phenols, among which iridoids and phenylpropanoids were the main active constituents. It has been reported that extracts of Scrophulariae Radix or its active substances have anti-inflammatory, antioxidant, hepatoprotective, anti-tumor, anti-fatigue, uric acid-lowering, anti-depression, myocardial cell-protective and other pharmacological activities, and can regulate cardiovascular system, central nervous system and immune system. This paper reviewed the present research achievements of Scrophulariae Radix in chemical constituents, pharmacological activities, processing methods, toxicity and other aspects, and the clinical application of Scrophulariae Radix in ancient and modern times was illustrated. This paper aimed to provide reference for further research of Scrophulariae Radix and facilitated its clinical application.
Medicine, Chinese Traditional ; Drugs, Chinese Herbal/chemistry* ; Chromatography, High Pressure Liquid ; Plant Roots/chemistry* ; Scrophularia/chemistry*

The present study investigated the chemical constituents of Scrophulariae Radix and their antitumor activities in vitro. The compounds in the ethyl acetate extract were separated and purified by conventional column chromatographies(such as silica gel, Sephadex LH-20, and ODS column) and semi-preparative high-performance liquid chromatography(HPLC), and their structures were identified by various spectral techniques such as nuclear magnetic resonance(NMR) and mass spectrometry(MS). Twenty-three compounds were isolated and identified as benzyl-β-D-(3',6'-di-O-acetyl) glucoside(1), 5-O-p-methoxybenzoyl kojic acid(2), 5-O-methoxybenzoyl kojic acid(3), 7-O-methylbenzoyl kojic acid(4), 5-O-benzoyl kojic acid(5), methyl ferulate ethyl ether(6), trans-ferulic acid(7), trans-isoferulic acid(8), trans-caffeic acid(9), trans-caffeic acid methyl ester(10), caffeic acid ethyl ester(11), trans-cinnamic acid(12), trans-p-methoxycinnamic acid(13), trans-p-hydroxycinnamic acid(14), trans-p-hydroxycinnamic acid methyl ester(15), 2-(3,4-dihydroxyphenethyl) alcohol(16),(p-hydroxyphenyl) propanoic acid(17), coniferaldehyde(18), sinapaldehyde(19), benzyl β-primeveroside(20), 5-(hydroxymethyl) furfural(21), furan-2-carboxylic acid(22), and decanedioic acid(23). Among them, compound 1 is a new benzyl glucoside, compounds 2-4 are new pyranone compounds, compound 5 is a new natural product of pyranone. The NMR data of compounds 5 and 6 are reported for the first time. Compounds 6 and 20 were isolated from the Scrophularia plant for the first time. Compounds 8, 11, 14, 16, 18, 19, 22, and 23 were isolated from this plant for the first time. The in vitro cytotoxic activities of these compounds against three tumor cell lines(HepG2, A549, and 4 T1) were evaluated. The results showed that compounds 10 and 15 showed cytotoxic activities against HepG2 cells with IC_(50) values of(19.46±0.48) μmol·L~(-1) and(46.10±1.21) μmol·L~(-1).
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal/chemistry* ; Mass Spectrometry ; Plant Roots/chemistry* ; Scrophularia/chemistry*

The quality constant evaluation method was applied in the grade evaluation of Scrophulariae Radix pieces. Nineteen batches of Scrophulariae Radix were measured for the appearance index. Harpagide and harpagoside were taken as index components for the content determination. The traditional grading standard and the modern quality control index were combined to calculate the quality constant and grade Scrophulariae Radix pieces. The results showed that the quality constants ranged between 156. 75 and 491. 65; according to the percentage mass constants,more than 80% were graded as first-class pieces,50%-80% were graded as second-class pieces,and the rest were graded as third-class pieces. The quality constants of first-class Scrophulariae Radix were >393. 32,that of second-class Scrophulariae Radix was between 245. 83 and 393. 32,and that of third-class Scrophulariae Radix was < 245. 83. The study shows that this method can objectively,reasonably and effectively classify Scrophulariae Radix pieces,and further promote and apply the evaluation method of slice model quality constant to prove the rationality,scientificity and practicability.
Drugs, Chinese Herbal ; standards ; Plant Roots ; chemistry ; Quality Control ; Scrophularia ; chemistry

The standard decoction of Chinese herbal decoction pieces is a standard reference substance to measure whether different dosage forms of Chinese medicine are basically consistent with those of clinical decoction,and provides new ideas and methods for effectively solving the problems of uneven quality in Chinese medicine dispensing granules. In this study,a systematic method for evaluating the quality of Scrophulariae Radix decoction was established from the perspective of " standard decoction",providing reference for the quality control of the Scrophulariae Radix dispensing granules. 15 batches of Scrophulariae Radix decoction pieces from different origins were collected,and 15 batches of standard decoctions were prepared according to the standardized process with water as solvent.Harpagide and harpagoside were used as quantitative detection indicators to determine the content,calculate the transfer rates and determine the extraction rate. The high performance liquid chromatography( HPLC) was used to establish a standard decoction fingerprint analysis method. The results showed that the transfer rates of harpagide and harpagoside in 15 batches of Scrophulariae Radix pieces standard decoction were( 70. 84±13. 39) % and( 48. 56±6. 40) % respectively; the extraction rate was( 57. 47±5. 89) %. Nine peaks were identified in the HPLC fingerprint,and the similarity was higher than 0. 97 between the fingerprints of 15 batches of standard decoction and the control fingerprint. In this study,the preparation process of standard decoction of Scrophulariae Radix pieces conformed to the traditional decoction preparation method. The sources of the samples were representative,and the established fingerprint method was stable and feasible,which can provide reference for the preparation and quality control of Scrophulariae Radix dispensing granules.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; standards ; Plant Roots ; chemistry ; Quality Control ; Scrophularia ; chemistry

The morphological indexes of the Scuophularia ningpoensis seedlings including the longth, diameter and weight were measured, clustering analysis was used to set up the standard quality grading of seedlings of S. Ningpoensis by SPSS. Field experiment was carried out to measure the indicators of plants growth and development, the yield and the quality. The results showed that the growth and yield of class I seedlings were better than those of class II and III. The content of main active ingredients was affected barely by seedlings classification. To ensure the quality, class II seedlings or above should be used for plantation. The established quality classification standard of S. ningpoensis seedlings was scientific and feasible, and provides the basis for the standardized cultivation of S. ningpoensis.
Drugs, Chinese Herbal ; analysis ; standards ; Quality Control ; Scrophularia ; chemistry ; classification ; growth & development ; Seedlings ; chemistry ; growth & development

Modern drying technology was used to explore suitable drying process to provide scientific basis for improving drying processing methods of Scrophulariae Radix. Controlled temperature and humidity drying, vacuum drying apparatus, microwave vacuum drying apparatus, short infrared drying device were used to gain samples for analyzing. The character appearance, concentration of main components and power consumption indicators were chosen for preliminary judging. Six major components, including iridoids and phenylpropanoids were analyzed by UPLC-MS/MS method. The contents of polysaccharides were determined by UV-visible spectrophotometry. The character appearance with controlled temperature and humidity drying and short infrared drying meet the pharmacopoeia standard (Ch. p, edition 2015), while samples with vacuum and microwave vacuum drying apparatus didn't. Compared to fresh sample, concentrations of harpagide, harpagoside, aucubin and catalpol were lower in the dried samples. Angoroside-C showed no significant change before and after drying. Concentration of acteoside increased after drying. Samples with controlled temperature (70 degrees C) and humidity (15% - 10%) drying had high content and short drying time. The better drying process of Scrophulariae Radix was controlled temperature and humidity drying. The method will provide the reference for the drying technology standard of roots medicine.
Desiccation ; methods ; Drugs, Chinese Herbal ; chemistry ; Plant Roots ; chemistry ; Quality Control ; Scrophularia ; chemistry

Phytochemical investigation of the roots of Scrophularia buergeriana Miq. (Scrophulariaceae), resulted in the isolation of a new iridoid derivative named as buergerinin (1). Its structure was elucidated as rel-(1R, 5R, 6R)-(2-oxa-bicyclo[3.3.0]oct-7-en-6, 7-diyl)dimethoxypropane based mainly on MS and 1D and 2D NMR spectroscopic analyses.
Iridoids ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Plant Roots ; chemistry ; Scrophularia ; chemistry

AIM: To analyze the major constituents in Radix Scrophulariae (Scrophularia ningpoensis). METHOD: Radix Scrophulariae was analyzed by HPLC coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (ESI-Q-TOF MS/MS). Compounds were separated by HPLC using a C18 column and gradient elution of acetonitrile and 0.1 % (V/V) acetic acid-water. Negative ion mode was employed. RESULTS: A total of thirty-six compounds, including fourteen iridoid glycosides, nineteen phenylpropanoid glycosides, and three organic acids, were identified from Radix Scrophulariae based on the accurate mass measurement of precursor and product ions. Twenty-one of the constituents were identified by comparing their retention times (tR) and ESI-MS/MS data with those of reference standards and/or previous publications, while another fifteen compounds were tentatively identified or deduced according to their Q-TOF MS/MS data which afforded sufficient structural information. CONCLUSION It is believed that this study is useful for the identification of constituents in Radix Scrophulariae, as well as related plants and complex prescriptions.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Molecular Structure ; Plant Roots ; chemistry ; Scrophularia ; chemistry ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

A new oleanane-type triterpenoid glycoside, 3beta-O-(f-D-xylopyranosyl-(1-->2)-[beta-D-glucopyranosyl (1-->4)-beta-D-glucopyranosyl-(1 -->3)]-beta-D-fucopyranosyl-11, 13(18) diene-olean-23alpha, 28 diol (1), along with three known phenylethyl glycosides (2-4), was isolated from the root of traditional Chinese medicine Scrophularia ningpoensis. Among them, compounds 2 and 3 were obtained from Scrophularia genus for the first time. The structure of compound 1 was elucidated on the basis of spectroscopic method including 1D, 2D NMR and HR-ESI-MS.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Glycosides ; chemistry ; isolation & purification ; Molecular Structure ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Scrophularia ; chemistry ; Triterpenes ; chemistry ; isolation & purification

OBJECTIVETo study the effects of the water extract of Rehmannia glutionsa, Scrophularia ningpoensis, Asparagus cochinchinensis and Ophiopogon japonicas, which are the drug from Tianwang Buxin Wan from nourishing vin, on the content of cytohrome P450 (CYP450) in rat and the activities of CYP3A, CYP2E1 and CYP1A2 to investigate the role of CYP450 in the biotransformation of Tianwang Buxin Wan.

METHODThe rats were killed after administrated with extracts once daily for consecutive 7 days, the livers were removed rapidly and weighed, liver microsomes were prepared with ultra-centrifuge method, the contents of liver microsomal CYP450, cytochrome b5 (Cytb5) and the activities of CYP3A were examined by ultraviolet spectrophotometry, the activities of CYP2E1 and CYP1A2 were determined by high performance liquid chromatography (HPLC).

RESULTAll groups had no difference in the levels of liver indexe compared with normal sodium group. The water extract of R. glutionsa obviously decreased the contents of P450 (P < 0.01) and increased the activity of CYP3A (P < 0.01) and CYP1A2 (P <0.05). The water extract of S. ningpoensis decreased the contents of P450 (P < 0.05) and significantly increased CYP3A and CYP1A2 activities (P < 0.01). A. cochinchinensis increased content of Cytb5 (P < 0.05) in rat and increased the activity of CYP2E1 (P < 0.05) and CYP1A2 (P < 0.01). O. japonicas had no significant difference on the contents of CYP450 and Cytb5 while increased the activities of CYP3A (P < 0.05), CYP2E1 (P < 0.05) and CYP1A2 (P < 0.01).

CONCLUSIONR. glutionsa and S. ningpoensis could decrease the content of CYP450 enzyme in rat liver and induct the activities of CYP3A and CYP1A2. A. cochinchinensis could induct the activities of CYP2E1 and CYP1A2. O. japonicus could induction the activities of CYP3A, CYP2E1 and CYP1A2 in Tianwang Buxin Wan. By inhibiting CYP450 activity to decrease the metabolism of other drugs, the effect of other functional groups in the compatibility of Tianwang Buxin Wan can be enhanced, and a theoretical basis on studying the compatible mechanism can be provided.

Animals ; Asparagus Plant ; chemistry ; Cytochrome P-450 CYP1A2 ; metabolism ; Cytochrome P-450 CYP2E1 ; metabolism ; Cytochrome P-450 CYP3A ; metabolism ; Cytochrome P-450 Enzyme System ; metabolism ; Drugs, Chinese Herbal ; Enzyme Activation ; drug effects ; Humans ; Liver ; drug effects ; enzymology ; Male ; Microsomes, Liver ; drug effects ; enzymology ; Ophiopogon ; chemistry ; Rats ; Rats, Sprague-Dawley ; Rehmannia ; chemistry ; Scrophularia ; chemistry