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At present, 141 compounds have been isolated from Picrorhiza scrophulariiflora and P. kurroa of the Scrophulariaceae plants, including 46 iridoid glycosides, 29 tetracyclic triterpenoids, 25 phenylpropanoids, and 11 phenylethanoid glycosides. Pharmacological studies have demonstrated that they have liver-, heart-, brain-, kidney-, and nerve cells-protecting effects as well as anti-tumor, anti-inflammatory, anti-bacterial, anti-asthma, anti-diabetic, immunomodulatory, and blood lipid-lowering activities. This article reviews the chemical components and pharmacological activities of P. scrophulariiflora and P. kurroa, aiming to provide a basis for the in-depth research, development, and utilization of the two plants.
Subject(s)
Iridoid Glycosides , Picrorhiza , Triterpenes/pharmacologyABSTRACT
Objective: To investigate the therapeutic effect of total iridoid glycosides of Picrorhiza scrophulariiflora (TIGP) on non-alcoholic steatohepatitis (NASH). Methods: SD rats were fed with high-fat and high-sugar diet for 8 weeks to establish NASH. TIGP were given orally at doses of 20, 40 and 80 mg/kg/d for 4 weeks. Triglycerides assay (TG), total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), aspartate aminotransferase (AST), alanine aminotransferase (ALT), fasting plasma glucose (FPG), fasting insulin (FINS), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), chemokine-1 (MCP-1), leptin (LEP) in serum were tested. TG, TC, superoxide dismutase (SOD), malondialdehyde (MDA), and free fatty acid (FFA) in liver tissue were determined by colorimetric methods. Steatosis of hepatocytes and inflammation was performed by pathological examination. Results: The results showed that TIGP significantly decreased TC, TG and FFA in liver tissue, increased SOD activity, decreased MDA content, decreased serum levels of TG, TC, HDL-C/LDL-C, ALT, AST, GLU, HOMA-IR, TNF-α and LEP, and in addition, improved steatosis of liver cells compared to NASH. Conclusion: TIGP had anti-fatty liver effect against NASH rats induced by high-fat and high-sugar diet. Its mechanism was related to the regulation of lipid metabolism and reduction of insulin resistance, through inhibition of oxidative stress and inflammation.
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Now days, one of the major lacunae in the Ayurvedic system of medicine is adulteration of medicinal plant species i.e. raw drug. Drug sellers for their financial gains adulterate the raw drugs with cheap, similar looking drugs or other substances. So, it has become necessary for the Ayurvedic physicians and pharmaceuticals to identify the raw drug before its clinical use. There is a need to set the standards for proper identification of the raw drug. So, this study was designed to establish various pharmacognostical standards which can help in ensuring identification of Katuka, a well known herb in Ayurvedic medicine. Botanically, the drug Katuka is Picrorhiza kurroa Royal ex. Benth belonging to the family Scrophulariaceae. Katuka is a valuable bitter tonic and is mainly used in Ayurveda for its hepatoprotective action. Its rhizome is used for medicinal purpose. So, macroscopical and microscopical characters of intact and powdered rhizome were studied. Macroscopic study of rhizome and its powder indicated the organoleptic characters like size, shape, colour, odour, taste and texture. Microscopic study of T.S. of rhizome showed the presence of cork, cortex, vascular cambium, xylem, phloem, pith and pith ray. Microscopic study of powder of rhizome showed the presence of starch grain, cork cells, xylem vessels, and pith cell with pitted wall thickenings, tracheid and lignified fiber. Pharmacognostical characters of rhizome of Katuka revealed from this study will help in standardization of this raw drug and preventing adulteration in the herbal raw drug market.
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Objective To establish the UPLC fingerprint for effective quality control and scientific evaluation of Picrorhiza scrophulariiflora. Methods The analysis was performed on Waters ACQUITY UPLC BEH C18 column (100 mm × 2.1 mm, 1.7 μm), using acetonitrile-0.5% glacial acetic acid aqueous solution as mobile phase for gradient elution, with the flow rate at 0.3 mL/min, the column temperature at 32 ℃, and the detection wavelength at 295 nm. Total of 25 batches of P. scrophulariiflora and its adulterants were analyzed. Similarity evaluation combined with hierarchical clustering analysis (HCA) and principal components analysis (PCA) were used to evaluate the quality of herbs from different batches. Ultra-performance liquid chromatography- quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF/MS) was used for qualitative analysis in the positive and negative ion modes. Results There were significant differences in fingerprint chromatogram among P. scrophulariiflora and its adulterants. There were 16 common peaks in UPLC fingerprint of 22 batches of P. scrophulariiflora, and 12 peaks among which were carried out for chemical components identification with the similarity at 0.939-0.998. Twenty-two samples could be classified into three clusters. The PCA result was consistent with that of HCA. The four symbolic compounds in samples were verified by PLS-DA analysis, which identified that No.1, 12, 9 peaks were picroside I, picroside III, and scrophenoside C. Conclusion The establishment of UPLC fingerprint and the recognition of chemical pattern of P. scrophulariiflora can provide a more comprehensive reference for the quality control of herbs.
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BACKGROUND/AIMS: Hepatic steatosis is caused by an imbalance between free fatty acids (FFAs) uptake, utilization, storage, and disposal. Understanding the molecular mechanisms involved in FFAs accumulation and its modulation could drive the development of potential therapies for Nonalcoholic fatty liver disease. The aim of the current study was to explore the effects of picroside II, a phytoactive found in Picrorhiza kurroa, on fatty acid accumulation vis-à-vis silibinin, a known hepatoprotective phytoactive from Silybum marianum. METHODS: HepG2 cells were loaded with FFAs (oleic acid:palmitic acid/2:1) for 20 hours to mimic hepatic steatosis. The FFAs concentration achieving maximum fat accumulation and minimal cytotoxicity (500 μM) was standardized. HepG2 cells were exposed to the standardized FFAs concentration with and without picroside II pretreatment. RESULTS: Picroside II pretreatment inhibited FFAs-induced lipid accumulation by attenuating the expression of fatty acid transport protein 5, sterol regulatory element binding protein 1 and stearoyl CoA desaturase. Preatreatment with picroside II was also found to decrease the expression of forkhead box protein O1 and phosphoenolpyruvate carboxykinase. CONCLUSIONS: These findings suggest that picroside II effectively attenuated fatty acid accumulation by decreasing FFAs uptake and lipogenesis. Picroside II also decreased the expression of gluconeogenic genes.
Subject(s)
Fatty Acid Transport Proteins , Fatty Acids, Nonesterified , Hep G2 Cells , Lipogenesis , Silybum marianum , Non-alcoholic Fatty Liver Disease , Phosphoenolpyruvate , Picrorhiza , Stearoyl-CoA Desaturase , Sterol Regulatory Element Binding Protein 1ABSTRACT
Objective: To study the constituents in the roots of Picrorhiza scrophulariiflora. Methods: The constituents of P. scrophulariiflora were separated and purified with chromatographic methods. The structures were elucidated by spectroscopic methods and chemical analyses. Results: Ten compounds were isolated from the roots of P. scrophulariiflora and identified as β-sitosterol (1), palmitic acid (2), octacosyl trans-ferulate (3), 3β-hydroxystigmast-5-en-7-one (4), 6β-hydroxystigmast-4-en-3-one (5), caffeic acid methyl ester (6), protocatechuic acid methyl ester (7), vanillic acid (8), caffeic acid (9), and piceoside (10). Conclusion: Compounds 2-7 and 9 are obtained from the plants of Picrorhiza Royle for the first time.
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Objective:To establish the identification method for Aucklandia Lappa and Picrorhiza kurrooa Royle ex Benth and the content determination of hydroxysaffor yellow A in Liangxue Shiwei San. Methods:The identification was carried out by TLC. The con-tent of hydroxysaffor yellow A was determined by HPLC. The column was Kormasil C18 (250 mm × 4. 6 mm, 5 μm) and the flow rate was 1. 0 ml·min-1. The mobile phase was methanol-0. 5% acetic acid (30∶70). The detection wavelength was 403 nm and the col-umn temperature was 25℃,and the sample size was 10 μl. Results:The TLC spots were clear with high resolution without interference from the negative sample. A good linearity of hydroxysaffor yellow A was within the range of 1.212-48.480μg·ml-1(r=0.999 8). The average recovery was 98. 13%(RSD=1. 6%,n=6). Conclusion:The established TLC and HPLC methods are simple and accu-rate with good reproducibility, which can be used in the quality control of Liangxue Shiwei San.
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Objective: To study the chemical constituents in the roots of Picrorhiza scrophulariiflora. Methods: The chemical constituents in the roots of P. scrophulariiflora were separated and purified with chromatographic methods. The structures were elucidated by spectroscopic methods and chemical analyses. Results: A new secoiridoid glycoside, picrogentioside II (1) was successfully isolated from the roots of P. scrophulariiflora. Conclusion: Compound 1 is a new secoiridoid glycoside. © 2013 Tianjin Press of Chinese Herbal Medicines.
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Objective: To study the characteristics of 2-C-methyl-D-erythritol 4-phosphate cytidylytransferase (MCT) gene and to predict the structure and function site of MCT. Methods: Based on MCT gene of Picrorhiza kurrooa, NCBI website and bio-informatics software were used to predict and analyze the base distribution, amino acid composition, hydrophilicity or hydrophobicity, and secondary and three-level structures of hyper-conservative region. The results were compared with MCT gene sequences in other eight species and the related evolution analysis was followed. Results: The mRNA sequence of MCT gene in P. kurrooa was 1216 bp (GenBank: JQ991625.1), coding the protein containing 399 amino acids, and the relative molecular mass of protein was 44448.5 with 10.0% Ser in volume; In polypeptide, hydrophobic amino acid was 59.5% in volume, and the average hydropathicity was 0.050; The homology was found as high as 99% compared with MCT gene in Salvia miltiorrhiza. Conclusion: The MCT gene in P. kurrooa was quite stable and the coded protein was hydrophobic, which was quite conservative in evolution; The sequence information in conservative region gained in the test provides the basis for clone ofnovel gene in other species.
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Objective: To study the constituents in the roots of Picrorhiza scrophulariiflora. Methods: The constituents of P. scrophulariiflora were separated and purified with chromatographic methods. The structures were elucidated by spectroscopic methods and chemical analyses. Results: Four compounds isolated from the 90% ethanol extract in the roots of P. scrophulariiflora were identified as picrogentioside D (1), sweroside (2), gentiopicroside (3), and mannitol (4). Conclusion: Compounds 1-4 are obtained from the roots of P. scrophulariiflora for the first time and compound 1 is a new secoiridoid glycoside, named picrogentioside D.
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As a major organ of intermediary metabolism, the liver is exposed to a variety of metabolic insults due to diseases and xenobiotics viz., insulin resistance (IR) drugs, toxins, microbial products, etc. One of the consequences of these metabolic insults including obesity and type 2 diabetes mellitus is the development of non-alcoholic fatty liver disease (NAFLD). The recent alarming increase in the prevalence of NAFLD compels the need to develop an appropriate animal model of the disease so as to evolve effective interventions. In this study, we have developed, in the rat, a new model of NAFLD showing several key features akin to the disease in humans. Male Wistar rats were challenged with 30% high fat diet (HFD) – butter, for 2 weeks to induce NAFLD. A hydroalcoholic extract of Picrorhiza kurroa was administered to study the possible reversal of fatty changes in the liver. The extract was given in two doses viz., 200mg/kg and 400 mg/kg b.i.d., p.o. for a period of 4 weeks. There were three control groups (n = 6/group) – vehicle with a regular diet, vehicle with HFD, and HFD with silymarin – a known hepatoprotective. Histopathology showed that the P. kurroa extract brought about a reversal of the fatty infiltration of the liver (mg/g) and a lowering of the quantity of hepatic lipids (mg/g) compared to that in the HFD control group (38.33 ± 5.35 for 200mg/ kg; 29.44 ± 8.49 for 400mg/kg of P. kurroa vs.130.07 ± 6.36mg/g of liver tissue in the HFD control group; P<0.001). Compared to the standard dose of the known hepatoprotective silymarin, P. kurroa reduced the lipid content (mg/g) of the liver more significantly at the dose of 400mg/kg (57.71 ± 12.45mg/kg vs. 29.44 ± 8.49 for the silymarin group vs. 400mg/kg of P. kurroa, P<0.001). In view of the increasing prevalence of metabolic syndrome and NAFLD, P. kurroa should be investigated by the reverse pharmacology path as a potential drug for the treatment of NAFLD, and essential safety studies and preformulation research for concentration of the putative actives should be carried out.
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Picrorhiza kurroa Royle ex Benth., is widely used in the Indian systems of medicine for the treatment of various liver ailments. Since, the role of oxidative stress in the pathogenesis of liver injury has become generally recognized, in present study the free radical scavenging effect of P. kurroa was assessed by on-line HPLC-DPPH and colorimetric DPPH methods. The comparative study on antioxidant activity of P. kurroa extracts by both methods revealed that colorimetric method showed very less free radical scavenging effect while HPLC-DPPH method showed high activity. Further, the kutkoside, an important ingredient of a potent hepatoprotective formulation “kutkin/ picroliv” was investigated for its chemical composition by ultra-performance liquid chromatography coupled with diode array detection/electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-DAD/ESI-QTOF-MS). Kutkoside was considered to be a single compound and reported as picroside-II or kutkoside, however, present investigation illustrated that kutkoside is a mixture of iridoid glycosides namely, picroside II, picroside IV and 6-ferulloylcatalpol.
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Ohjective To observe the inhibition effect of total glucosides of Picrorhiza on hepatitis B virus covalently closed circular DNA (HBV cccDNA) in HepG 2.2.15 cell line. Methods HepG 2.2.15 cells were incubated with culture medium containing 50 mg/L of picrosides or 5 mg/L of adefovir dipivoxil for 2 or 5 days. HBV DNA in the supernatant, intracellular cccDNA, relaxed circular DNA (rcDNA) and pregenomic RNA (pgRNA) were quantified by specific real-time polymerase chain reaction (RT-PCR) and inhibition rates were calculated. The means were compared by t test. Results After treated with picrosides for 2 and 5 days, the inhibition rates of HBV DNA in thesupernatant were 49. 74% (t=4.723, P<0.05) and 79.48% (t = 7.512, P<0.05), respectively. The inhibition rates of intracellular cccDNA were 43.55% (t = 5.216, P<0.05) and 56.43% (t=7.262, P<0.05), respectively, while those of intracellular rcDNA were 43.39% (t=4.137, P<0.05) and 63.86% (t=7.861, P<0.05), respectively, and those of intracellular pgRNA were 54.72% (t=4.532, P<0.05) and 56.08% (t=4.833, P<0.05), respectively. Comparatively, after treatment with adefovir dipivoxil for 2 and 5 days, the inhibition rates of HBV DNA in the supernatant were 25.56% (t=2.874, P<0.05) and 92.44% (t =10.276, P<0.05), respectively. Those of cccDNA were 18.54% (t=2.736, P<0.05) and 47.19% (t=6.852, P<0.05), respectively. Those of rcDNA were 21. 20% (t=3.206, P<0.05) and 71.47% (t=8.332, P<0.05), respectively, pgRNA were 11.14% (t=1.761, P>0.05) and 37.61%(t=3.632, P<0.05) respectively in HepG2.2.15 cells. Conclusions Pierosides may inhibit the replication cycle of HBV, including the formation of cccDNA in HepG 2.2.15 cells. The mechanism of pierosides on cccDNA may differ from adefovir dipivoxil's due to its earlier inhibition time phase.
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Objective To investigate the protective effect of extract of Picrhoriza scrophulariflora on renal ischemia/reperfusion injury(I/R). Methods Male SD rats were randomly divided into sham-operated group (n=5), I/R group(n=8), I/R+ extracts of Picrhoriza scrophulariflora groups (each group had 8 rats). Acute renal ischemia/reperfusion injury in rats was reproduced by removing the right kidney and clamping the left renal artery with a non-traumatic vascular clamp for 60min followed by reperfusion for 72h. Serum creatinine, urine creatinine and renal pathological changes, were compared between I/R and I/R+ extracts of Picrhoriza scrophulariflora groups, malondialdehyde (MDA) and glutathione peroxidase (GSHPx). Results CCr levels were significant decreased after renal I/R injury. Kidneys of animal with I/R injury displayed significant pathological changes. 72h after ischemia, Ccr and serum GSHPx of animals of the I/R+ extracts of Picrhoriza scrophulariflora group were significantly higher than those of I/R group(P