Prediction and analysis of Q-markers of Elephantopus scaber based on its UPLC fingerprint, content determination of components, and in vitro a nti-tumor activity / 中国中药杂志

This study aimed to provide scientific evidence for predicting quality markers(Q-markers) of Elephantopus scaber by establishing UPLC fingerprint of E. scaber from different geographical origins and determining the content of 13 major components, as well as conducting in vitro anti-cancer activity investigation of the main components. The chromatographic column used was Waters CORTECS UPLC C_(18)(2.1 mm×150 mm, 1.6 μm), and the mobile phase consisted of acetonitrile and 0.1% formic acid solution(gradient elution). The column temperature was set at 30 ℃, and the flow rate was 0.2 mL·min~(-1). The injection volume was 1 μL, and the detection wavelength was 240 nm. The UPLC fingerprint of E. scaber was fitted using the Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine(2012 edition) to determine common peaks, evaluate similarity, identify and determine the content of major components. The CCK-8 assay was used to explore the inhibitory effect of the main components on the proliferation of lung cancer cells. The results showed that in the established UPLC fingerprint of E. scaber, 35 common peaks were identified. Thirteen major components, including neochlorogenic acid(peak 1), chlorogenic acid(peak 2), cryptochlorogenic acid(peak 3), caffeic acid(peak 4), schaftoside(peak 6), galuteolin(peak 9), isochlorogenic acid B(peak 10), isochlorogenic acid A(peak 12), isochlorogenic acid C(peak 18), deoxyelephantopin(peak 28), isodeoxyelephantopin(peak 29), isoscabertopin(peak 31), and scabertopin(peak 32) were identified and quantified, and a quantitative analysis method was established. The results of the in vitro anti-cancer activity study showed that deoxyelephantopin, isodeoxyelephantopin, isoscabertopin, and scabertopin in E. scaber exhibited inhibition rates of lung cancer cell proliferation exceeding 80% at a concentration of 10 μmol·L~(-1), higher than the positive drug paclitaxel. These results indicate that the fingerprint of E. scaber is highly characteristic, and the quantitative analysis method is accurate and stable, providing references for the research on quality standards of E. scaber. Four sesquiterpene lactones in E. scaber show significant anti-cancer activity and can serve as Q-markers for E. scaber.

The Effects of Deoxyelephantopin on the Akt/mTOR/P70S6K Signaling Pathway in MCF-7 Breast Carcinoma Cells In Vitro

Objective To determine the effects of deoxyelephantopin on mTOR and its related target molecules (Akt/mTOR/P70S6K) in the ER-positive breast cancer cell line. Materials and Methods Primary in silico simulations were determined, and the effects of deoxyelephantopin on the phosphorylation of the Akt/mTOR/P70S6K molecules were evaluated using AlphaScreen-based assays and western blot analysis, respectively. Results Based on the estimated FEB and Ki values, deoxyelephantopin appeared to have a stronger affinity toward P70S6K as compared with Akt and mTOR. Both deoxyelephantopin and control inhibitors were observed to form hydrogen bonds with the same key residue, Leu175 of the P70S6K molecule. Deoxyelephantopin downregulated the p P70S6K protein expression significantly from 18 µM (p < 0.05) and onward. Based on the AlphaScreen assay, deoxyelephantopin produced a concentration-dependent inhibition on the phosphorylation of P70S6K with an IC50 value of 7.13 µM. Conclusion Deoxyelephantopin induced cell death in MCF-7 cells possibly via DNA fragmentation, inhibition of the phosphorylation of P70SK6, and downregulation of the relative p-p70S6K protein expression levels.

The Effect of Ethanol Extract of Elephantopus scaber Linn in Decreasing Blood Uric Acid Levels of Hyperuricemic Male Rats

Background: Gout causes attacks of pain and swelling in one or more joints and control of serum uric acid level has been used as one of the therapeutic methods for gout. Inhibition method of xanthine oxidase (XO) activity which can oxidize hypoxanthine to uric acid has been commonly used to decrease serum uric acid level. On the other hand, Elephantopus scaber Linn leaf has been used for the treatment of rheumatoid arthritis as folk medicine by some people in Indonesia. Aims: This study was to determine the hypouricemic effect of ethanol extract of Elephantopus scaber leaf by in vivo study in caffeine (PO)-induced hyperuricemic male rats. Methodology: The E. scaber leaf was obtained from Research Institute for Spices and Medicinal Plants, Bagor, Indonesia. Preparation of E. scaber leaf extract was done by cold maceration extraction technique using ethanol 70%. Male rats (Sprague-Dawley) were induced by using caffeine with dose 27 mg/200 g b.w until the levels in the blood of male rats become hyperuricemic. Equipment (Easy Touch) was used by detecting the level of uric acid in a rat blood. Equipment (Easy Touch) was used by detecting the level of uric acid in a rat blood. Rats were divided into 6 groups, as a positive control was used allopurinol 36 mg/200 g b.w, test preparation were used 3 doses, i.e, 175 mg/200 g b.w, 350 mg/200 g b.w and 700 mg/200 b.w which suspended in Na-CMC 0.5%. Results: The results from a decrease in blood uric acid levels in rats, on the 15th days showed that a dose of 350 mg / 200 g b.w gave decrease in the highest percentage ie 43%. Statistical analysis on the 15th day showed that all of the test preparation groups of E. scaber had effects decrease uric acid in blood serum of rats and significantly different from negative controls (p ≤ 0.05). The dose of 350 mg/200 g b.w of E. scaber had the same effect with a dose of 36 mg/200 g b.w allopurinol in reducing uric acid in experimental rats. Conclusions: E. scaber is a plant that is quite potential to be used in the treatment of gout.

Effect of Ethanol from Extract of Tapak Liman Leaves (Elephantopus scaber Linn.) on Hematopoiesis of Anemia Mice

This study assessed the impact of the electrochemically activated aqueous solutions (ECA AS) on the growth and formationof the biofilm of lactic acid bacteria (LAB). The effectiveness of biocides produced by the unipolar electrochemicalactivation of aqueous solutions of sodium chloride was studied. It was found that sequential treatment of the biofilm withcatholyte and anolyte (fractions ECA AS) lead to the most pronounced decrease in the growth rate and density of bacteria.The results obtained demonstrate antibacterial efficacy and the possibility of using ECA AS for the prevention anddisinfection of aquatic systems, for example, at the enterprises of the agro-industry and the food industry

Isolation and Identification of Antioxidant Activity Constituents from Elephantopus scaber / 中国实验方剂学杂志

Objective:To study the chemical constituents of 95% ethanol extract of the whole plant of Elephantopus scaber and investigate its antioxidant activity. Method:The chemical constituents were isolated and purified by silica gel column chromatography,Sephadex LH-20 column chromatography,ODS column chromatography,semi-preparative high performance liquid chromatography (HPLC) and recrystallization methods,while their structures were identified on the basis of nuclear magnetic resonance (NMR), mass spectrometry and comparison of their spectral data with those reported in the literature. Result:Fourteen compounds were isolated and their structures were identified as:(E)-3-(3,4-dihydroxybenzylidene)-5-(3,4-dihydroxyphenyl)-2(3H)-furanone (1),esculetin (2),dihydrosyringenin (3),(+)-isololiolide (4),caffic acid (5),luteolin-7-O-β-D-glucuronide (6),luteolin-7-O-β-D-glucuronide methyl ester (7),chlorogenic acid methyl ester (8),blumenol A (9),(6R,9R)-3-oxo-α-ionol-β-D-glucopyranoside (10),byzantionoside B (11),3,5-O-dicaffeoyl quinic acid methyl ester (12),3,4-O-dicaffeoyl quinic acid methyl ester (13) and 4,5-O-dicaffeoyl quinic acid methyl ester (14). Conclusion:Compounds 1-4 and 8-10 were isolated from the genus Elephantopus for the first time. Compound 11 was isolated from E. scaber for the first time. The DPPH radical and ABTS+ radical scavenging experiments on twelve of these compounds showed that compounds 1,2,5,6,12 and 13 had significant antioxidant activity.

Simultaneous determination of four sesquiterpene lactones in the whole herb of Elephantopus scaber Linn / 国际药学研究杂志

Objective: To establish an ultra-performance liquid chromatography(UPLC)method for the simul-taneous determination of four sesquiterpene lactones, deoxyelephantopin, isodeoxyelephantopin, isoscabertopin and sca- bertopin in Elephantopus scaber Linn.. Methods: The UPLC conditions were as follows: the separation was performed using an Acquity UPLC BEH C18(2.1 mm × 100 mm, 1.7 μm)column, the temperature of the column was maintained at 40℃, and the detection wavelength was 220 nm. The mobile phase was the water and acetonitrile solution in a binary gra- dient elution at the flow rate of 0.3 ml/min. Results: The four components, deoxyelephantopin, isodeoxyelephantopin, isoscabertopin and scabertopin were separated well under the UPLC conditions and showed a good linearity within the ranges of 0.383-76.500(R2=0.9999), 0.775-155.0(R2=0.9999), 0.507-101.5(R2=0.9999), and 0.850-(R2=0.9997), respectively. Their average recovery(n=6)was 102.31%, 103.87%, 102.66% and 105.68%, RSD was 1.20%, 2.00%, 1.24% and 1.73%, respectively. The four components were validated by the simultaneous termination in eleven batches of E. scaber samples from different areas in the present study. Conclusion: lished UPLC method could be used for the determination of four sesquiterpene lactones, deoxyelephantopin, elephantopin, isoscabertopin and scabertopin in E. scaber. The present results provide a reference for further velopment and quality evaluation of E. scaber.

Dose-response effects of Elephantopus scaber methanolic extract on N-nitrosodiethylamine-induced hepatotoxicity in rats / 中国天然药物

AIM@#A decoction of Elephantopus scaber (Asteraceae) root is used to treat liver disorders in Indian and Chinese traditional medicine. The study was designed to examine the dose response effects of E. scaber methanolic extract on rats exposed to N-nitrosodiethylamine (NDEA) induced hepatotoxicity (0.02% NDEA in water five days per week, per oral) in preventive and curative models.@*METHODS@#In preventive groups, NDEA was administered for six weeks. Daily doses of E. scaber methanolic extract (200 and 100 mg·kg-1) started one week before the onset of NDEA intoxication and continued for six weeks. In curative animals, NDEA was administered for six weeks followed by treatment with the methanolic n-hexane extract of E. scaber (200 and 100 mg·kg-1) for ten days.@*RESULTS@#E. scaber extract treatment significantly (P ≤ 0.05) reduced the levels of AST, ALT, and MDA in both experimental groups. The extract also enhanced the antioxidant enzyme and protein levels in rats intoxicated with NDEA. Treatment with the extract dose dependently protected the liver from NDEA-induced hepatotoxicity with normal hepatocytes and uniform sinusoids, but in some areas showed degenerating hepatic cells in both treatment groups.@*CONCLUSION@#E. scaber methanolic extract dose dependently prevented and reversed the hepatotoxicity induced by NDEA in both experimental models.

Evaluation of acute administration of natural products with potential diuretic effects, in humans

In order to evaluate the potential diuretic effect of two natural products, Elephantopus scaber and Alpinia speciosa, a trial administration was carried out in ten healthy volunteers and the effects compared to the those of a placebo. The substances were given on different days, with a seven day interval between doses. The amount of substance administered to the subjects was five times the usual dose i.e. 7.5 g/100 ml and 0.8 g/100 ml respectively. The following parameters parameteres were measured: urinary and plasma sodium, potassium, uric acid, calcium, phosphate, urea, creatinine. The subjects were also examined clinically and total urinary volume was assessed. The only significant finding (p < 0.05) was a slight diuresis with Alpinia speciosa, which also lowered the diastolic (p < 0.05) and systolic (p < 0.01) blood pressures. No effect on electrolytes or renal function parameters was observed, and this probably excludes any renal tubular or glomerular effect from these substances. .