Study on Metabolism of Miao Medicine Laportea bulbifera Extract in Isolated Human Intestinal Flora / 中国药房

OBJECTIVE：To explore the metabolic charact eristics of Miao medicine Laportea bulbifera extract in isolated human intestinal flora. METHODS ：L. bulbifera was extracted with 70％ ethanol reflux extraction. After concentration，extraction with n-butanol and drying ，L. bulbifera extract was obtained. Taking 0.05 g/mL L. bulbifera extract 1 mL mixed with isolated human intestinal flora fluid 10 mL and cultured for 36 h in anaerobic environment （setting up blank control without drugs or human intestinal bacterial solution ），so as to simulate the metabolic process of the extract in human intestine. The metabolites were detected by UPLC-Q-TOF/MS. The determination was performed on Agilent Eclipse Plus C 18 RRHD column with mobile phase consisted of 0.01％ formic acid water solution- 0.01％ formic acid acetonitrile solution （gradient eluetion ）at the flow rate of 0.25 mL/min. The column temperature was set at 40 ℃，and the sample size was 1 µL. ESI detection was adopted and scanned by negative ion mode （ESI－）；the capillary voltage was 4.5 kV，the ion source temperature was 120 ℃，the collision energy was 15-32 V，and the scanning range was m/z 50-1 000. The “Strip”module of MassLynx V 4.1 software was used to analyze the differential chromatograms between the reaction solution and the blank control of L. bulbifera extract. Mass spectrum data and UNIFI so ftware were used to predict relative molecular weight and formula ；based on the information of substance control and related literature reports ， the structure and biotransformation pathway of L. bulbifera metabolites in isolated human intestinal flora were predicted and analyzed. RESULTS & CONCLUSIONS ： A total of 3 prototype ： products（rutin，quercetin，kaempferol-3-O-rutinoside）and 22metabolites （mainly the metabolites of quercetin ，mono- caffeoylquinic acid ，isoquercitrin，etc.） were detected after metabolized in isolated human intestinal flora. Itsbiotransformation pathway is phase Ⅰ reaction，which mainly consisted of reduction ，oxidation and hydrolysis.

Study on metabolites of Laportea bulbifera extract in rat feces based on UHPLC-Q-TOF-MS~E technique / 中国中药杂志

This project is to study the metabolites of Laportea bulbifera extract in rat feces. After the SD rats were gavaged with the extract(136 g·kg~(-1), according to the crude drug dose), the metabolites in their feces were detected by UHPLC-Q-TOF-MS~E technique, and the obtained mass spectrometry data was combined with UNIFI software for prediction. The prototype components and metabolites in rat feces were identified with reference materials and related literature. A total of 43 metabolites were identified(including 8 prototype components and 35 metabolites). The metabolic pathways mainly include monocaffeoylquinic acid(hydrogenation reduction, ring-opening cracking, sulfation, hydroxylation, glucuronidation), quercetin(O-C2 bond ring-opening cleavage, C2-C3 double bond reduction, rutin carbonylation) and so on. The metabolites and metabolic process of L. bulbifera extract in rat feces were clarified, which provided a basis for the study of the active substances and its mechanism of action.

Differences in intestinal absorption characteristics of Laportea bulbifera extract in normal and rheumatoid arthritis model rats by isolated everted intestine model / 中国中药杂志

This work aimed to investigate the intestinal absorption characteristics of Laportea bulbifera extract in normal and rheumatoid arthritis model rats. The contents of neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, rutin, kaempferol-3-O-rutinoside, galuteolin, quercetin and isoquercetin in intestinal absorption solution samples were detected by UPLC-MS/MS with 5.0 g·L~(-1) as the absorption concentration. The cumulative absorption(Q) and absorption rate constant(K_a) were calculated, and the absorption characteristics of different components of L. bulbifera in intestinal absorption solution of normal rats and rheumatoid arthritis rats were compared. The results showed that all the eight index components in the extract of L. bulbifera could be absorbed into the intestinal capsule, the cumulative absorption-time curve of each component showed an upward trend without saturation, and the correlation regression coefficient(R~2) was greater than 0.92, which is consistent with the zero-order absorption rate process. It was speculated that the possible absorption mode of each component was passive diffusion. In normal condition, the absorption of ileum was the best(except chlorogenic acid), and in pathological condition, duodenum was the best. The total absorption of 8 components in each intestinal segment of RA rats was better than that of normal rats, which speculated that rheumatoid arthritis may change the specific site of drug absorption. The experimental results showed that rheumatoid arthritis could change the intestinal absorption of the extract of L. bulbifera, and its mechanism needs further study.

Research Progress of Laportea bulbifera / 中国实验方剂学杂志

The research literature of Laportea bulbifera was summarized and analyzed, and its distribution of literature, chemical composition, pharmacological activity, quality control, clinical application and patent approval were summarized, this study can provide reference for the follow-up clinical application and development and utilization of the herb. Taking CNKI and PubMed database as the retrieval platform, keywords and full text as the search items, the Honghema, Honghuoma, Zhuya Aima, Laportea bulbifera (Siebold & Zuccarini) Weddell. and Laportea bulbifera as the search terms, the domestic and foreign paper reports and patent approvals of L. bulbifera from 1989 to 2018 were retrieved. A total of 41 papers and 63 patents were reviewed, the contents of these papers were pharmacological activity, chemical composition and quality control research, the majority of patents were compound. At present, 73 chemical constituents have been isolated and identified from L. bulbifera, and most of them were flavonoids. Flavonoids, catechins and coumarins were selected as the quality control indexes, and most of the pharmacological activities were anti-inflammatory, analgesic and anti-rheumatism. L. bulbifera is highly competitive in the market because of its remarkable pharmacological activities, however, its quality control level in local standard is low and testing items are incomplete. The determination reported in the literature lacks specific indexes to evaluate the quality of L. bulbifera, at the same time, it is necessary to further study its anti-inflammatory mechanism, explore its quality markers and establish the spectrum-effect relationship, so as to effectively control the quality of L. bulbifera and provide documentation for its comprehensive utilization and resource development.

Chemical Constituents from Laportea bulbifera, a Zhuang Medicine / 中国药学杂志

OBJECTIVE: To study the chemical constituents from Laportea bulbifera. METHODS: The 60% ethanol extract from L. bulbifera was isolated and purified by chromatography on silica, Sephadex LH-20, and ODS, recrystallization, and semi-preparative HPLC. Their chemical structures were elucidated by physicochemical properties and spectroscopic methods. RESULTS These compounds were determined as β-sitosterol(1), protocatechuic acid ethyl ester(2), scopoletin (3), trans-cinnamic acid (4),trans-p-hydroxycinnamic acid(5), kaempferol 7-O-rhamnoside(6), luteolin(7), ethyl gallate(8), (+)-isolarisiresinol 3a-O-β-D-glucopyranoside(9), and kaempferitrin(10). CONCLUSION Compounds 2, 5, 7-9 are isolated from genus Laportea for the first time, and compounds 2-5,7-9 are isolated from this plant for the first time.