Aim: Monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) are believed to be pharmacologically important for the antiseptic herbal injection XueBiJing. This study was designed to characterize the pharmacokinetics and disposition of monoterpene glycosides. Methods: Systemic exposure to Chishao monoterpene glycosides was assessed in human subjects receiving an intravenous infusion and multiple infusions of XueBiJing injection, followed by assessment of the pharmacokinetics of the major circulating compounds. Supportive rat studies were also performed. Membrane permeability and plasma-protein binding were assessed in vitro. Results: A total of 18 monoterpene glycosides were detected in XueBiJing injection (content levels, 0.001-2.47 mmol/L), and paeoniflorin accounted for 85.5% of the total dose of monoterpene glycosides detected. In human subjects, unchanged paeoniflorin exhibited considerable levels of systemic exposure with elimination half-lives of 1.2-1.3 h; no significant metabolite was detected. Oxypaeoniflorin and albiflorin exhibited low exposure levels, and the remaining minor monoterpene glycosides were negligible or undetected. Glomerular-filtration-based renal excretion was the major elimination pathway of paeoniflorin, which was poorly bound to plasma protein. In rats, the systemic exposure level of paeoniflorin increased proportionally as the dose was increased. Rat lung, heart, and liver exposure levels of paeoniflorin were lower than the plasma level, with the exception of the kidney level, which was 4.3-fold greater than the plasma level; brain penetration was limited by the poor membrane permeability. Conclusion: Due to its significant systemic exposure and appropriate pharmacokinetic profile, as well as previously reported antiseptic properties, paeoniflorin is a promising XueBiJing constituent of therapeutic importance.

It has been reported that dogs are capable of identifying cancer in humans by detecting a specific odor: bladder cancer by detecting urine odor and other cancers by detecting exhaled breath odor. However, no odor recognized by dogs that indicates cancer has been identified. In this study, we examined whether bladder cancer could be detected by gas chromatography-mass spectrometry (GC-MS)-based metabolomics analysis of urine odor. Nine patients with bladder cancer and 7 healthy controls were recruited as participants. Patients collected urine 3 d before and for 3-7 d after surgery. The concentrated urine odor was analyzed by GC-MS and principal component analysis (PCA). Results indicated 12 metabolites of urine odor. Score plots of 7 of the preoperative bladder cancer patients were clearly different from those of controls on the PCA map. The distribution of controls was in the negative domain of principal component (PC) 1, whereas the distribution of preoperative patients was in the positive domain of PC1. Bladder cancer was diagnosed in 5 of the 9 patients on the basis of urinary cytology. The findings indicate the potential to screen bladder cancer by analyzing urine odor. Moreover, diagnosis of bladder cancer on the basis of urine odor might have higher sensitivity than screening by urinary cytology. Key words metabolomics; urine odor; bladder cancer; GC-MSThe annual incidence of bladder cancer in men and women is showing a gradual tendency to increase. 1) Urinary tract epithelial cancer is the main bladder cancer and is conventionally detected by hematuria. Screening examinations include urinary cytology, and imaging by cystoscopy, and definitive pathological diagnosis is made by transurethral bladder biopsy. But they have high invasiveness. The bladder cancer is classified roughly into a permeative cancer of the intramural muscular layer and a superficial (muscular layer non-permeation) bladder cancer. When permeative cancer of bladder was discovered, a patient needs all bladder enucleation which is normal treatment that causes urinary passage change. Decline of the quality of life (QOL) is an important problem for patients. On the other hand, when superficial bladder cancer was discovered, a transurethral resection of bladder tumor (TURBT) is considered first-choice treatment. By receiving TURBT, the patient can still keep the bladder. Survival rates for five years of the patient become more than 95%. The life convalescence of the patient is good, too.2) However, many patients have a relapse of a cancer intravesically after a surgery early. It becomes necessary to perform the enforcement of the bladder cancer screening examinations including a purpose to detect a recurrence frequently. For such a reason, the physical, mental and financial burden for the patient is big, and development of the noninvasive screening is urgent business. Therefore, we decided to develop a new screening system for indentifying urinary tract epithelial cancer by metabolomics analysis of urinary odor.The identification of bladder c...

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BackgroundAt present, the incidence of alcoholic fatty liver disease (AFLD) is increasing year by year, and numerous studies have confirmed that liver diseases are closely related to intestinal flora. Seabuckthorn and Astragalus membranaceus, as traditional Chinese medicine (TCM) with the homology of medicine and food, have good liver protection, and their polysaccharides can regulate the intestinal flora. Here, we studied the effects of HRP, APS and the combination of the two polysaccharides on the intestinal flora of AFLD mice, which provided scientific basis for the treatment of AFLD with the two polysaccharides.Materials and methodsThirty Kunming (KM) mice were randomly divided into the control group (Con), the model group (Mod), the HRP treatment group (HRP), the APS treatment group (APS), and HRP+APS treatment group (HRP+APS), with six mice in each group. The AFLD model was constructed by continuous intragastric administration of 42% vol Niulanshan ethanol solution for 28 days, and the mice in each polysaccharide group were given corresponding drugs. The levels of AST, ALT, TC and TG in serum of mice were measured. 16S rRNA amplicon sequencing technique was used to determine the diversity and richness of intestinal flora, and the relative abundance of intestinal flora at phylum level and genus level of the mice in each group.ResultsHRP, APS and HRP+APS could reduce the serum levels of AST, ALT, TC and TG in mice. In addition, HRP, APS and HRP + APS restored the diversity, relative abundance and community structure of intestinal mucosa bacteria in AFLD mice to a certain extent. Specifically, HRP, APS and HRP+APS remarkably decreased the ratio of Firmicutes to Bacteroidetes, and ultimately increased the abundance of beneficial bacteria and reduced the abundance of pathogenic bacteria.ConclusionHRP, APS, and HRP+APS can improve the intestinal microecology of AFLD model mice, alleviate liver injury, and maintain normal intestinal function in different degrees.