Traditional uses, botany, phytochemistry, and pharmacology of Lonicerae japonicae flos and Lonicerae flos: A systematic comparative review.

ETHNOPHARMACOLOGICAL RELEVANCE: Lonicerae japonicae flos (LJF) and Lonicerae flos (LF) belong to different genera of Caprifoliaceae with analogous appearances and functions. Historically, they have been used as herbal medicines to treat various diseases with confirmed wind-heat evacuation, heat-clearing, and detoxification effects. However, the Chinese Pharmacopoeia (2005 Edition) lists LJF and LF under different categories. AIM OF THE STUDY: Few studies have systematically compared the similarities and dissimilarities of LJF and LF concerning their research achievements. This systematic review and comparison of the traditional use, identification, and phytochemical and pharmacological properties of LJF and LF provides valuable insights for their further application and clinical safety. MATERIALS AND METHODS: Related document information was collected from databases that included Web of Science, X-MOL, Science Direct, PubMed, and the China National Knowledge Infrastructure. RESULTS: The chemical constituents and pharmacological effects of LJF and LF were similar. A total of 337 and 242 chemical constituents were isolated and identified in LJF and LF, respectively. These included volatile oils, cyclic ether terpenes, flavonoids, phenolic acids, triterpenoids, and their saponins. Additionally, LJF plants contain more iridoids and flavonoids than LF plants. The latter have a variety of triterpenoid saponins and significantly higher chlorogenic acid content than LJF plants. Pharmacological studies have shown that LJF and LF have various anti-inflammatory, antiviral, antibacterial, anti-endotoxic, antioxidant, anti-tumor, anti-platelet, myocardial protective, and hepatoprotective effects. CONCLUSIONS: This review was undertaken to explore whether LJF and LF should be listed separately in the Chinese Pharmacopoeia in terms of their disease prevention and treatment strategies. Although LJF and LF showed promising effects, their action mechanisms remains unclear. Specifically, their impact on gut microbiota, gastrointestinal tract, and blood parameters requires further investigation. These studies will provide the foundation for scientific utilization and clinical/non-clinical applications of LJF and LF, and the maximum benefits from their mutual use.

[Comparison of active components in different parts of Perilla frutescens and its pharmacological effects].

Perilla frutescens is a widely used medicinal and edible plant with a rich chemical composition throughout its whole plant. The Chinese Pharmacopoeia categorizes P. frutescens leaves(Perillae Folium), seeds(Perillae Fructus), and stems(Perillae Caulis) as three distinct medicinal parts due to the differences in types and content of active components. Over 350 different bioactive compounds have been reported so far, including volatile oils, flavonoids, phenolic acids, triterpenes, sterols, and fatty acids. Due to the complexity of its chemical composition, P. frutescens exhibits diverse pharmacological effects, including antibacterial, anti-inflammatory, anti-allergic, antidepressant, and antitumor activities. While scholars have conducted a substantial amount of research on different parts of P. frutescens, including analysis of their chemical components and pharmacological mechanisms of action, there has yet to be a systematic comparison and summary of chemical components, pharmacological effects, and mechanisms of action. Therefore, this study overviewed the chemical composition and structures of Perillae Folium, Perillae Fructus, and Perillae Caulis, and summarized the pharmacological effects and mechanisms of P. frutescens to provide a reference for better development and utilization of this valuable plant.

[Research status of common processing technology of traditional Chinese medicine "maintaining medicinal properties after carbonisatus" and supramolecular "imprinting template" characterization technology].

Based on the characteristics of biological supramolecules and the law of " imprinting template",the research status and common problems in " maintaining medicinal properties after carbonisatus" in traditional Chinese medicine( TCM) were analyzed,and the further countermeasures were put forward. According to the historical evolution of " maintaining medicinal properties after carbonisatus" in TCM processing,the origin of its common problems was clarified by using the theory of biosupramolecular chemistry. TCM is a megacomplex biological supramolecular system,so TCM processing is just the processing of megacomplex biological supramolecular system,and its essence is a TCM pharmaceutical technology with chemical changes in host and guest of biological supramolecular system with or without adjuvant material under high temperature and humidity. In this study on pharmaceutical technology,host molecule was destructed in the process of carbonizing,but guest molecule was retained. The changing law of the host and guest molecule was controlled by the " imprinting template",which was reflected in the degree of change in the drug properties and efficacy of the decoction pieces. Supramolecular chemistry ran through the whole process,and the " imprinting template" of charcoal medicine was characterized by the supramolecular topological structure characteristics and imprinting behavior. After being combined with the quantitative mathematical model of heating degree in processing,it can realize the accurate processing of " maintaining medicinal properties after carbonisatus" from the source,quantitatively control the quality of carbonic herbs,and formulate stable and controllable quality standards.

[Dynamic chromatopharmacokinetics model for components in Chinese medicine and validation in Buyang Huanwu Decoction].

The Chinese medicine is mostly derived from plants or animals, highly polymorphic, with dynamic components which are reflected by the characteristic peaks and fingerprint peaks in chromatographic fingerprints. The chromatopharmacokinetics method for determined components is not applicable due to dynamic changes of chromatopharmacokinetics. Based on the preliminary study, dynamic pharmacokinetics mathematical model for multiple components in Chinese medicine was set up and verified by Buyang Huanwu Decoction as the model drug, applying the principle of the total quantum statistical moment(TQSM), superimposing or subtracting the relevant statistical parameters in blood samples and blank samples. This provided a new method for the chromatopharmacokinetic study of Chinese medicine. HPLC was used to determine the TQSM parameters in blood and blank sample fingerprints of Buyang Huanwu Decoction at each point, and the overall TQSM parameters of drug-containing blood sample and blank samples were obtained with addition calculation of TQSM; while the initial TQSM of the pure drug can be obtained with subtraction calculation. The metabolic and absorption equilibrium constants were calculated iteratively to a steady state using the estimated metabolic equilibrium constants, then the metabolic chromatopharmacokinetic parameters in rats were obtained: VUC_T 1.262×10~8 mAu·s, MRT_T 37.48 h, VRT_T 9.016×10~2 h~2, CL_T 25.79 mL·h~(-1)·kg~(-1), Vs 1.586×10~2 mL·kg~(-1), t_(T,0.5) 6.15 h, respectively. This suggested that 95% of the compounds in whole recipe were metabolized and secreted from the body after 0-96.33 h. The experiment verified that the established mathematical model and the total quantum moment statistics parameters can represent the dose-time relationship of Buyang Huanwu Decoction, which can be used to study on in vivo metabolism dynamics for Chinese medicine.

Novel mathematic models for quantitative transitivity of quality-markers in extraction process of the Buyanghuanwu decoction.

BACKGROUND: Nowadays, to research and formulate an efficiency extraction system for Chinese herbal medicine, scientists have always been facing a great challenge for quality management, so that the transitivity of Q-markers in quantitative analysis of TCM was proposed by Prof. Liu recently. In order to improve the quality of extraction from raw medicinal materials for clinical preparations, a series of integrated mathematic models for transitivity of Q-markers in quantitative analysis of TCM were established. Buyanghuanwu decoction (BYHWD) was a commonly TCMs prescription, which was used to prevent and treat the ischemic heart and brain diseases. In this paper, we selected BYHWD as an extraction experimental subject to study the quantitative transitivity of TCM. STUDY DESIGN: Based on theory of Fick's Rule and Noyes-Whitney equation, novel kinetic models were established for extraction of active components. Meanwhile, fitting out kinetic equations of extracted models and then calculating the inherent parameters in material piece and Q-marker quantitative transfer coefficients, which were considered as indexes to evaluate transitivity of Q-markers in quantitative analysis of the extraction process of BYHWD. METHODS: HPLC was applied to screen and analyze the potential Q-markers in the extraction process. Fick's Rule and Noyes-Whitney equation were adopted for mathematically modeling extraction process. Kinetic parameters were fitted and calculated by the Statistical Program for Social Sciences 20.0 software. The transferable efficiency was described and evaluated by potential Q-markers transfer trajectory via transitivity availability AUC, extraction ratio P, and decomposition ratio D respectively. The Q-marker was identified with AUC, P, D. RESULTS: Astragaloside IV, laetrile, paeoniflorin, and ferulic acid were studied as potential Q-markers from BYHWD. The relative technologic parameters were presented by mathematic models, which could adequately illustrate the inherent properties of raw materials preparation and affection of Q-markers transitivity in equilibrium processing. AUC, P, D for potential Q-markers of AST-IV, laetrile, paeoniflorin, and FA were obtained, with the results of 289.9 mAu s, 46.24%, 22.35%; 1730 mAu s, 84.48%, 1.963%; 5600 mAu s, 70.22%, 0.4752%; 7810 mAu s, 24.29%, 4.235%, respectively. CONCLUSION: The results showed that the suitable Q-markers were laetrile and paeoniflorin in our study, which exhibited acceptable traceability and transitivity in the extraction process of TCMs. Therefore, these novel mathematic models might be developed as a new standard to control TCMs quality process from raw medicinal materials to product manufacturing.

A novel concept of Q-markers: Molecular connectivity index.

BACKGROUND: Drugs derived from botany have been playing essential role in both clinical treatment and pharmaceutical industry, unfortunately our worry is still that its quality and therapeutic efficacy are inconsistent. Recently many scientists launched a new project on quality (Q)-marker of medicinal herbs, this study was thus designed to generate a novel concept of quality (Q)-markers: molecular connectivity index (MCI), and to test and verify the new concept of molecular connectivity index (MCI). METHODS: The first-order term (1χ) was selected to calculate and study quality (Q)-marker for TCM. Houttuynia cordata Thunb. (HCT) was adopted as a model to verify the hypothesis. Volatile oils of HCT were determined using gas chromatography-mass (GC-MS). SIMCA 13.0 and SPSS 21.0 were used to deal with the data. RESULTS: The minimum of the MCI values was 1.273, belonging to the peak 15, but the maximum (12.822) belonged to the peak 34, and the average value of fifty volatile oils was 5.798. The results demonstrated that MCI was the principle component, and monoterpenoid and sesquiterpenoid were also the principle components in oils. Fig. 2a shows peak 5, 24, 34 were the significant ingredients, while Fig. 2b shows peak 2, 5, 24 were the significant components. CONCLUSION: The data demonstrated that MCI was associated with the structure of molecules and the therapeutic efficacy, MCI could directly exhibit the relationship between ingredients and effectiveness of Traditional Chinese Medicine (TCM). So MCI could be a potential and promising parameter for quality (Q)-marker. Therefore, MCI may be developed as a novel potential concept to control the quality of TCM.

Application of TQSM polypharmacokinetics and its similarity approach to ascertain Q-marker by analyses of transitivity in vivo of five candidates in Buyanghuanwu injection.

BACKGROUND: It is well-known that the public still have been facing on a severe issue about the inconsistency of quality and therapeutic efficacy of traditional medicines. Recently, Professor Chang-Xiao Liu has created a new promising concept for identifying relevant quality-markers (Q-marker) from herbs, their formulas and manufacturing products. Therefore, building up a new approach is necessary for us to bridge over quality to efficacy of pharmaceutical products. STUDY DESIGN: In this paper, five candidate Q-markers, astragaloside IV, paeonflorin, amygdalin, tetramethylpyrazine, ferulic acid in Buyanghuanwu injection (BYHWI) had been designed to carry out in rat by using single and polypharmacokinetic models for total quanta to ascertain adequate Q-marker. METHODS: The Q-marker transitivity in vivo was studied with polypharmacokinetic model and its similarity approach, which were modeled with TQSM principle. The Q-marker was ascertained with transitive similarity and bioavailability in polypharmacokinetics. Their concentrations in plasma sample of white rat were determined by RP-HPLC. Data analyses were used by the DAS software for singles and myself-written-program with EXCEL for multiples. RESULTS: In BYHWI, five candidate Q-marker pharmacokinetic profiles were singly fixed to two compartmental models in rat using classical compartmental analysis, but there were tremendous differences among which the candidate parameters were fluctuated from nearly 3552 folds to equivalency. The theoretical value of TQSM polypharmacokinetic parameters such as AUCT, MRTT, VRTT, CLT, VT over the mixure of five drugs were 110.8 ±â€¯51.91 mg min ml-1, 176.0 ±â€¯36.5 min, 39,921 ±â€¯4311 min2, 0.3116 ±â€¯0.02347 ml min-1 kg-1, 54.83 ±â€¯7.683 ml kg-1 respectively. The TQSM polypharmacokinetic parameters in astragaloside Ⅳ ordered by AUCT, MRTT, VRTT, CLT, VT were 110.8 ±â€¯51.91 mg min ml-1, 176.0 ±â€¯36.5 min, 39,921 ±â€¯4311 min2, 0.3116 ±â€¯0.02347 ml min-1 kg-1, 54.83 ±â€¯7.683 ml kg-1, respectively, which were closed to the theoretical values. TQSM similarity versus astragaloside Ⅳ was 0.9661. CONCLUSION: The results represented that the optimum Q-marker in BYHWI is astragaloside Ⅳ, whose transitivity in vivo similarity was close to the behavior of polypharmacokinetics with maximum bioavailability to the total quanta. It is feasible for Q-marker in CMMs to screen on the comparison of single pharmacokinetic behavior and bioavailability to the total quanta.