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Polygonum capitatum has unique curative effects on the urinary system. In fact, many Polygonum capitatum-based preparations are currently used in the clinic. In China, the combination of levofloxacin (LVFX) with a Chinese herbal preparation derived from Polygonum capitatum has been used for the clinical treatment of urinary system diseases, which can improve the curative effects and reduce the side effects of LVFX. However, the herb-drug interaction (HDI) between these drugs has not been reported and the effect of Polygonum capitatum on the in vivo process of LVFX is unclear. In this article, a sensitive ultraperformance liquid chromatography-tandem mass spectroscopy (UPLC-MS/MS) method was developed to evaluate the effects of the combined application of LVFX and the Polygonum capitatum extract on tissue distribution and excretion. Thereafter, the method was validated for selectivity, accuracy, precision, linearity, lower limit of quantification (LLOQ), dilution integrity, recovery, and matrix effect. Based on tissue distribution, LVFX could diffuse into all of the tested tissues, with significant differences in the content of each tissue between the coadministration group and single administration group. At 48 h after the combination was orally administered, the urinary cumulative excretion of LVFX decreased from 20.69% to 11.84% while its fecal cumulative excretion decreased from 26.08% to 13.28%. Our results suggest that a drug interaction exists between the two drugs in the process of distribution and excretion. This study provides important experimental evidence for further studies on the clinical efficacy and mechanism of the Polygonum capitatum extract and LVFX. [ABSTRACT FROM AUTHOR]

A rapid, reliable, and sensitive HPLC-electrospray ionization-tandem mass spectrometry (HPLC-MS/MS) method was established and validated for simultaneous determination of militarine and its three metabolites (gastrodin, α-isobutylmalic acid, and gymnoside I) in rat plasma. Plasma was acidified with formic acid, and protein was precipitated with methanol. MS/MS with ESI and multiple reaction monitoring at m/z 725.3→457.3, 457.1→127, 304.3→107.2, 189→129, and 417.1→267.1 was used for determination of militarine, gastrodin, α-isobutylmalic acid, gymnoside I, and puerarin (internal standard), respectively. Chromatographic separation was conducted using an ACE UltraCore SuperC18 (2.1 × 100 mm, 2.5 μm) column with gradient mobile phase (0.1% formic acid in water and acetonitrile). The lower limits of quantitation for militarine, gastrodin, α-isobutylmalic acid, and gymnoside I were 1.02, 2.96, 1.64, and 0.3 ng/mL, respectively. The relative standard deviations of intra- and interday measurements were less than 15%, and the method accuracy ranged from 87.4% to 112.5%. The extraction recovery was 83.52%-105.34%, and no matrix effect was observed. The three metabolites (gastrodin, α-isobutylmalic acid, and gymnoside I) were synchronously detected at 0.83 h, suggesting that militarine was rapidly transformed to gastrodin, α-isobutylmalic acid, and gymnoside I. Moreover, the area under the curve (AUC) and Cmax of militarine were significantly lower than those of gastrodin and α-isobutylmalic acid, showing that militarine was largely metabolized to gastrodin and α-isobutylmalic acid in vivo. The studies on pharmacokinetics of militarine and its three metabolites were of great use for facilitating the clinical application of militarine and were also highly meaningful for the potential development of militarine. [ABSTRACT FROM AUTHOR]

Two new phenolic glycosides, syringic acid-4-O-α-L-rhamnoside (1) and ( - )-hydnocarpin-7-O-β-D-glucoside (2), were isolated from the traditional Chinese medicinal herb Inula cappa. The structures of the new compounds were elucidated by means of spectroscopic methods such as 1D, 2D NMR, and HR-ESI-MS. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Kalimeris indica is a Miao׳s medicinal plant in Guizhou province of China employing to treat various inflammation-related diseases in clinical. The study aims to determine the active fractions of K. indica for its anti-inflammatory activity and to identify their chemical constituents. Material and methods The dried K. indica herb was extracted with 50% aqueous ethanol and then successively separated with macroporous resin and MCI column chromatography to give five fractions (A–E). The anti-inflammatory effects were determined by measuring the NO and TNF-α production in murine macrophage RAW 264.7 cells after exposure to LPS. The chemical constituents of the anti-inflammatory fractions were analyzed by the method of UHPLC-ESI-Q-TOF/MS or GC–MS. Results Five fractions (A–E) of different polarities were prepared from the 50% ethanol extract. Factions C and E showed significant inhibition of NO and TNF-α production. Six constituents, namely 3,4-dicaffeoylquinic acid ( 1 ), 3,5-dicaffeoylquinic acid ( 2 ), 1,5-dicaffeoylquinic acid ( 3 ), rutin ( 4 ), 1-malonyl-3,5-dicaffeoylquinic acid ( 5 ), and 4,5-dicaffeoylquinic acid ( 6 ) were identified from the active fraction C by UHPLC-ESI-Q-TOF/MS. Four compounds including 13-tetradecenal ( 7 ), ( Z , Z )-9,12-octadecadienoic acid ( 8 ), (3α)-12-oleanen-3-yl acetate ( 9 ), and (+)-3-oxo-urs-12-en-24-oic acid methyl ester ( 10 ) were identified from the active fraction E by GC–MS. Conclusion K. indica possessed pronounced anti-inflammatory effect. Dicaffeoylquinic acids and their dirivatives, rutin, as well as oleanolic and fatty acid derivatives are the major constituents and possibly the anti-inflammatory principles of the active fractions of K. indica . All the compounds were identified in K. indica for the first time. The work provided evidence for further development and utilization of K. indica and formed a basis for the establishment of quality control methods and standards for K. indica and its pharmaceutical preparations. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Polygonum capitatum is a well-known Miao medicinal plant that has been used for many years for its unique therapeutic effects on various urological disorders, including urinary calculus and urinary tract infections. To investigate the effect of Polygonum capitatum on cytochrome P450 (CYP) isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2E1, and CYP3A4) in vivo using a “cocktail” approach by administering five probe drugs to rats. This study assessed the potential of Polygonum capitatum to interact with co-administered drugs. Materials and methods An aqueous extract of dried whole Polygonum capitatum was prepared and administered orally to rats at a dose of 0.58 g/kg or 1.74 g/kg twice daily for 7 or 14 consecutive days. A cocktail of caffeine (1.0 mg/kg), tolbutamide (1.0 mg/kg), omeprazole (2.0 mg/kg), chlorzoxazone (4.0 mg/kg) and midazolam (4.0 mg/kg) was then administered on the eighth or fifteenth day to evaluate the effects of Polygonum capitatum on CYP1A2, 2C9, 2C19, 2E1, and 3A4, respectively. Blood samples were collected at a range of time-points and the plasma concentrations of the probe drugs were simultaneously quantified using ultra high-performance liquid chromatography–tandem mass spectrometry. Pharmacokinetic parameters were calculated to evaluate the effects of Polygonum capitatum on the activities of these CYP enzymes in rats. Results Polygonum capitatum pre-treatment had no significant effect on the pharmacokinetic parameters of caffeine, omeprazole or chlorzoxazone. However, the pharmacokinetics of tolbutamide and midazolam were affected significantly ( P <0.05) by Polygonum capitatum , which induced more rapid metabolism of these probe compounds. Conclusions These results suggested that Polygonum capitatum could induce CYP2C9 and CYP3A4, and did not influence CYP1A2, CYP2C19 or CYP2E1. Therefore, the clinical dose of drugs metabolized by human CYP2C9 or CYP3A4 may need to be adjusted in patients taking Polygonum capitatum , as this herbal medication may result in reduced effective concentrations of these drugs. [ABSTRACT FROM AUTHOR]