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Essential oils(EOs) from Chinese medicinals, which can be used as adjuvants and exert certain therapeutic effect, are directly used in Chinese medicine formulas. Conventional research strategy for EOs from Chinese medicinals is to compare the efficacy of the prescriptions before and after the addition of EOs, and the penetration-enhancing mechanisms of EOs remain unclear. In modern research on EOs from Chinese medicinals, the method for studying chemical penetration enhancers is often used, which fails to reflect the overall efficacy of EOs. This study clarified the property regularity of EOs from Chinese medicinals as transdermal penetration enhancers, and thereby proposed a research model which integrated the medicinal and adjuvant properties of EOs from Chinese medicinals via "component-delivery-effect" characterization route. The core concept is that constituents of EOs from Chinese medicinals and their delivery process play a key role in their external application. This research model is expected to serve as a reference for further research on EOs from Chinese medicinals for transdermal application.
Subject(s)
Adjuvants, Pharmaceutic , Administration, Cutaneous , China , Drugs, Chinese Herbal/pharmacology , Oils, Volatile/pharmacologyABSTRACT
Decoction is a traditional clinical way of traditional Chinese medicine （TCM） compound. A series of complex physical and chemical changes are often involved in the process of decoction， which presents a mixed-phase system. In most studies on the TCM compound decoction， it has always focused on the amounts of chemical substances in decoction， while the phase properties and existence forms of these components are neglected. Most of the chemical components exist in the mixed-phase system as molecules， ions or other particles. According to the particle size of the contained particles， the differences among the phases， including true solution phase， colloidal phase， suspended phase and precipitated phase， lead to their differences in pharmaceutical and biological effects. Based on the above research background， this paper takes the phase state differences of decoction as the breakthrough point， and systematically reviews the physicochemical properties， the physical structures of the active components and the biological effects of the decoction caused by the phase state differences. The phase state differences of TCM compound decoction have been found to be closely related to their efficacy， which might be a good perspective to investigate the possible mechanism. It might provide a beneficial reference for the exploration of related basic research on TCM compounds.
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Seven emotions of Chinese materia medica (CMM) is the main compatibility form. Metabonomics is mainly to study the differences of metabolic spectrum, analyze the relationship between pathway and physiological and pathological changes of organisms after drug use through the analysis of metabolites, and explain the mechanism of drug action and the function relationship of compatible drugs. The author summarized the characteristics of increasing efficiency, detoxification, drug property changes and action mechanism from the compatibility forms of using a single drug, mutual reinforcement, mutual assistance, mutual restraint, mutual suppression, mutual inhibition and antagonism in the application of CMM by using metabonomics in recent years, in order to provide a basis for the objective interpretation of the compatibility of seven emotions of CMM.
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Objective: In this study, network pharmacology techniques and methods were used to screen the material basis, targets and pathways of the interaction between the pungent-aromatic herbs (Citri Reticulatae Pericarpium, Caryophylli Flos, and Foeniculi Fructus) and olfactory receptor. To explain the molecular mechanism of the expression of pungent properties of the pungent-aromatic herb. Methods: TCMSP database was used to collect the chemical components of Citri Reticulatae Pericarpium, Caryophylli Flos, and Foeniculi Fructus, in order to screen out the effective components and predict the related targets. All the proteins related to olfactory receptors were collected from UniProt database. The selected targets and ORs proteins were uploaded to the online STRING database for protein interaction analysis. The interaction network was drawn by using the software of Cytoscape software, and the key targets was further analyzed by GO functional enrichment analysis and KEGG pathway enrichment analysis. Results: Five active components of Citri Reticulatae Pericarpium, five of Caryophylli Flos and two of Foeniculi Fructus, 224 targets and 515 olfactory receptors were obtained. Protein interaction network showed 25 targets (such as GNB2, CHRM2, CHRM3, GNGT2, ADRA2A) were the key targets for ORs of three pungent-aromatic herbs. The enrichment analysis of GO and KEGG identified 31 biological processes and 78 signaling pathways. Conclusion: Olfactory receptors are mainly activated by volatile oil components of the pungent-aromatic herb. And the classical cAMP signaling pathway may not be the only one after the olfactory receptor activated, which may be involved in the expression of pungent properties of the pungent-aromatic herb together with several other signaling pathways, so as to produce "pungent flavor".
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Ephedra is a classic herb in traditional Chinese medicine( TCM). The new effects of ephedra were gradually found,and the contraindications of the drug were broken in later ages. Because the principles of expanded application were not well elucidated,it is difficult to use in the clinical flexibility. Based on the characteristics of ephedra and its classic clinical application,the authors summarized the possible principles of clinical application of ephedra and the drug property and pharmacological characteristics of ephedra.Studies showed that ephedrine substances are an important material basis for the efficacy of ephedra,and its adrenergic action is the pharmacological basis of its efficacy. It is the key to grasp the autonomic function and the interaction between sympathetic/adrenal medulla and adrenal cortex for the clinical application of ephedra. The authors discussed the principles of clinical application of ephedra and the effects of processing of ephedra. Finally,the authors put forward the basic research process of clinical application of drugs,and provide ideas for the inheritance and further development of TCM experience.
Subject(s)
Ephedra/chemistry , Ephedrine/pharmacology , Medicine, Chinese Traditional , Plant Extracts , Plants, Medicinal/chemistryABSTRACT
Yiqi Fumai Lyophilized Injection is a modern preparation composed of Panax ginseng, Ophiopogon japonicas, and Schisandra chinensis. Clinically, it is mainly used for the treatment of cardiovascular diseases such as angina pectoris of coronary heart disease and chronic cardiac insufficiency. According to the concept of quality markers (Q-markers), the Q-markers of Yiqi Fumai Lyophilized Injection were predicted and analyzed from the aspects of chemical components, drug effect, network pharmacology, pharmacokinetics, and drug property. Based on the above studies, 13 components of ginsenosides Rb1, Rg1, Rf, Rh1, Rc, Rb2, Ro, Rg3, ophiopojaponin C, phiogenin-3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside, pennogenin-3-O-α-L-rhamnopyranosyl-(1→2)- β-D-xylopyranosyl-(1→4)-β-D-glucopyranoside, fructose, and schisandrin A were identified as Q-markers. According to the Q-markers, we established quality system for process control. The study of Yiqi Fumai Lyophilized Injection based on Q-markers can provide new research ideas for quality assessment of traditional Chinese materia medica injection.
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The theory on the property of Chinese materia medica (CMM) is one of the core contents of CMM theory, among which five flavors theory is the core content of CMM theory. The objective characterization of the five flavors of CMM is the key to the theoretical study of CMM, which is an important way to explain the scientific connotation of CMM. Based on the basic definition of five tastes medicinal properties and the interaction of drug molecules-taste, olfactory receptors, authors put forward the research methods using molecular docking technology and the research approach. In this study, the expression of five tastes drug property was systematically discussed from the aspects of biological mechanisms of taste, olfactory perception, molecular docking, homology modeling, and receptor selection, which provides a reference method for the study of drug property theory from the perspective of taste and smell attribute of five tastes.
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The quality of Chinese materia medica (CMM) is the lifeline of Chinese medicine industry. However, many problems are still found in the quality study on CMM, which restricts the healthy development of Chinese medicine industry to a certain extent. Aiming at the problems existing in the quality research on CMM, the research idea, method and approach of quality marker research and quality evaluation of CMM were put forward based on systematic analysis and discussion on the basic properties and clinical features of CMM according to the core concept of quality marker and the combination of research practice, from the perspective of transmission and traceability of quality elements, the relationship between chemical composition and traditional efficacy containing "drug property" and "drug function", composition analysis of endemicity based on pharmacophylogenetic study and biosynthetic approach. Finally, a new integrated mode of CMM quality evaluation and control was established.
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Property and flavor theory of traditional Chinese medicine (TCM) is the core base for clinical treatment of diseases. However, few research about its chemical and biological characterization was performed. In this paper, network pharmacology was adopted to review patterns around the theory of TCM. "Xiaoke" prescription database, which combinations of herb medicines for diabetes therapy, was firstly built to explore prescription regularity and screen core paired-components. The prescription regularity and molecular mechanism of flavor composition were explored through the relationship of "drug-compound-target-pathway-function" by ChEMBL, CTD and KEGG datebase. As a result, the tastes of "Gan" (sweetish taste) and "Ku" (bitter taste) were the popular therapeutic flavor to regulate the disorder of glucose and lipid metabolisms. The mechanism of Xiaoke was summarized from representative traditional Chinese medicine partner "Zhimu-Huangbai" and "Huangqi-Gegen". The key components of "Gan", including saponins stimulated insulin secretion, improve insulin resistance and promote glucose utilization. The components of "Ku", including flavonoids and alkaloids regulate inflammatory cytokines, promoted the utilization of glucose, improve endocrine and metabolism through MAPK, PI3K-Akt, PPAR signal pathway. The TCM therapeutic mechanism about "Xiaoke" was preliminarily summarized to clear "heat" by anti-inflammation and immunoregulation, to regulate glucolipid metabolism for removing the satiation of digestion, and to improve the utilization of insulin and diabetes complications for endocrine adjusting. The results demonstrate that therapeutic principle of TCM for "Xiaoke" is comprehensive via multi pathway. This study provides a new research method and strategy for exploring the mechanism of TCM for diabetes therapy.
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The research of effective components of Chinese materia medica (CMM) is one of the key points of modernization of traditional Chinese medicine (TCM), is the core of interpreting overall efficacy and mechanism of TCM, and is the important foundation of realizing the safety, efficacy, and quality control of CMM. Previous studies mostly focused on the binary research mode of "component-effect". However, in this paper, the triarchic theory of "property-effect-component" was proposed and the research strategy and mode of exploring the mechanism, effective components, and quality markers (Q-Marker) of TCM were established based on the basic properties of TCM, basic concepts and terms of TCM theory and also related with the core contents of TCM theory including syndrome differentiation and treatment, rules of treatment, method of treatment, compatibility regularity, and drug property. The Yuanhu Zhitong Dropping Pills (YZDP) were taken as an example for demonstration research and corydaline, tetrahydropalmatine, protopine, imperatorin, and isoimperatorin were determined to be the Q-Marker of YZDP.
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Penetration enhancers (PE) were usually applied as the optimum strategy to improve the percutaneous absorption of active components from pharmaceutical preparations. Essential oils (EOs) were a kind of PE with satisfactory characteristics. Only 34 of among more than 300 EOs are reported to be used as PE. That is to say, about 90% EOs have not been applied until now and EOs possess great potential to act as PE. However, the research of EOs from Chinese materia medica (CMM) mainly followed the strategy of chemical PE. A large amount of studies were carried out to evaluate the transdermal penetration enhancing efficacy and pharmacological activity, resulting in the limited efficiency. EOs of CMM were also the key material basis of CMM pungent flavor. In the theory of traditional Chinese medicines (TCM), it was accepted that the pungent flavor could open the striae and interstice. The results of literature investigation revealed that the penetration enhancing efficacy of EOs directly related with drug property characteristics of CMM. Therefore, in the present paper, it was proposed that a rule existed between the penetration enhancing efficacy of EOs and drug property characteristics of CMM. A series of studies were then designed to reveal the rule with the aid of data analysis. The resultant rule will help to find the effective PE from various EOs. Moreover, to facilitate the high-throughput screening of EOs, liposomal artificial skin membrane was prepared and applied to the evaluation of in vitro penetration enhancing efficacy of EOs with optimization of the evaluation parameters. Finally, the results of the study will provide a novel strategy for the research of EOs as PE and the research of the application of TCM theory to the modern pharmaceutical study. In addition, the application of microemulsion technique will be the future trends of EOs as PE to solve the stability problems.
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OBJECTIVE: Drug properties have important effect on the drug nanosuspenions/nanocrystal production and can determine the final particle size and production efficiency. A number of papers have referred to the optimizations of processes expecting the smaller achievable particle sizes as well as increased production efficiency. Aspects such as stabilizer selection are those most commonly described in the literature. The aims of this study are to systematically investigate the mechanism of nanocrystal formation and identify the physical properties that can affect the particle size reduction process. METHODS: The influence of drug properties such as degree of crystallinity and particle morphology on particle size reduction was systematically investigated by producing hesperetin as a model drug. Processes ie spray-drying, rotavapor, and quench-cooling were applied to modify the physical properties of hesperetin. Both unmodified drugs and modified drugs were used for production of nanosuspension. RESULTS: The nanosuspension with the smallest particle size was obtained from spray-dried hesperetin. CONCLUSION: An improved crystal morphology of modified starting material obtained through spray-drying may lead to a more efficient homogenization process. The drug exists in the nanosuspensions as crystalline, which means recrystallization has occurred as a result of the high pressure homogenization process.
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According to the current research issues on the drug-properties of Chinese materia medica (CMM), authors presented a research main-line on the "five tastes" (pungent, sweet, sour, bitter, and salty) and mode and idea on the "five elements" with "drug-five tastes-substances-effects-function" for studying the function/efficacy in the theory of traditional Chinese medicines. Based on the idea, authors elaborated a "five tastes" starting point in CMM with invigorating blood circulation and eliminating blood stasis to study the relationship between the chemical substances related with " five tastes" and the biological basis to explain the CMM function-efficacy. Authors believe that in the study on the CMM drug property and the scientific connotation with modern scientific and technological means, the "five elements" is the transformation of the bond and to capture the differences between the "five flavors" and function/efficacy is difficult. Thus, the idea would be beneficial to the development of innovative pharmaceutics of CMM.
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The article is to explore the relationship between the dose of formula and Chinese medicine position of monarch, minister, assistant, and guide. The dose of formula is pretreated. The relationship between the dose of formula and Chinese medicine position of monarch, minister, assistant, and guide is analyzed by method of correlativity. Hypothesis tests are executed. There is negative correlation between the ranking of formula dosage and Chinese medicine position of monarch and minister. There is no correlation between the dose of formula and Chinese medicine position of assistant and guide. The more the dosage of a Chinese herb is n the prescription, the more likely the Chinese herb is the main part of prescription.
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Objective: To investigate the theoretical basis of incompatibility of Euphorbiae pekinensis Radix (EPR) and Glycyrrhizae Radix et Rhizoma (GRR). Methods: In order to compare the effects of EPR used alone and combined with GRR, the diuretic effect was studied by weighing method to observe the urine output of normal mice, while the purgation effect was studied by observing the defecation time, feces pellets, and feces shape after drug administration. Results: In the equivalent dose range of China Pharmacopoeia 2010, the diuretic effect of EPR powder is stronger than its aqueous extract; GRR aqueous extract did not show any promoting or suppressing effect on the diuresis; Within 1 h after coadministration of EPR powder and GRR aqueous extract, urine output was significantly reduced, suggesting that GRR might inhibit the diuretic effect of EPR; The co-detection of EPR and GRR did not cause the obvious changes of urine output. There was no significant purgative effect of EPR powder alone and coadministered with GRR aqueous extract at the same dose level. Conclusion: The diuretic effect of EPR can be suppressed by GRR in the equivalent dose range of China Pharmacopoeia 2010, suggesting that the sweet and mitigation property of GRR relieving the effect of removing water retention by purgation is one of the incompatibility theoretical basis between EPR and GRR.
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Objective: To initially explore the drug biological characteristics of pungent-hot and bitter-cold herbs on the various functions of hypothalamus-hypophysis-target gland axises in Yang-deficiency rats, according to the pungent-hot herbs, Aconiti Lateralis Radix Praeparata (ALRP), Curculiginis Rhizoma (CR), Cinnamomi Cortex (CC), and bitter-cold Phellodendri Chinensis Cortex (PCC), and Gardeniar Fructus (GF) and to investigate their biological expression characteristic on Yang-deficiency state. Methods: The decoctions of ALPR, CR, CC, PCC, and GF were ig administered to Yang-deficiency rats once daily for 7 d. The indexes of thyroid-stimulating hormone (TSH), triiodothyronine (T3), tetraiodothyronine (T4), 17-hydroxycorticosteroids (17-OHCS), cortisol (COR), testosterone (T), and estradiol (E2) in serum of animals in each group were detected. Results: The T3, 17-OHCS, COR, T, and T/E2 values of Yang-deficiency rats in ALRP, CR, and CC groups were obviously increased, while E2 was decreased. ALRP and CC could significantly increase T4 of Yang-deficiency rats, TSH in Yang-deficient rats was decreased by CC, the COR of Yang-deficiency rats in CC and GF groups was decreased, and E2 in Yang-deficiency rats was decreased by CC. Conclusion: The pungent-hot herbs of ALRP, CR, and CC and bitter-cold herbs of PCC, GF show the different drug property in intervention of Yang-deficiency rats. The pungent-hot herbs have an obvious regulation on hypothalamus-hypophysis-target gland axises, while the bitter-cold herbs have no significant role.
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OBJECTIVE:To investigate the effects of water extract of Panax quinque folium(WEAG,of cool property)and Panax ginseng(WERG,of warm property)on MPP+-induced apoptosis of SH-SY5Y cells.METHODS:SH-SY5Y cells were divided into 4 groups:the control group was cultured in complete medium,model group was cultured with 0.5 mmol MPP+;Panax quinque folium group was treated with 0.5 mmol MPP+ plus different concentration of WEAG,and Panax ginseng group was treated with 0.5 mmol MPP+ and different concentration of WERG concomitantly.WEAG and WERG were added for intervention.the morphology of SH-SY5Y cells was observed by Hoechst33258 staining and the apoptotic rate was detected by FCM;the cell survival rate was measured by MTT chromatometry.RESULTS:Compared with model group,WEAG and WERG markedly reversed the apoptotic characteristics of SH-SY5Y cells,markedly up-regulated MTT value and lowered the apoptotic rate,with WERG showing more potent efficacy than WEAG doing.CONCLUSION:Water extracts of both Panax quinque folium(cool)and Panax ginseng(warm)pose protective effects of different degree against MPP+-induced apoptosis of SH-SY5Y cells,with the Chinese materia medica of warm property showing more potent action against apoptosis.Chinese materia medicas of different drug property have different anti-apoptotic action.
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Objective:To study effect of SC-LK on the immune function of immunosuppressive mice and to seek the relationship between drug property of SC-GS and immunoenhancement activity. Methods:The immunosuppressive mice models were established by CTX and administrated with four groups of drugs. The phagocytic ability of macrophage,serum hemolysin level,and proliferative response of T lymphocyte induced by PHA were measured. The activity of in vitro M? and the phagocytizing of CRBC by M? were measured. Results:SC-LK could significantly improve immunological function inhibited by CTX in mice. Conclusion:The improving of immunological function was a common effect in drug effect spectrum(drug property) of SC-LK,but it was not characteristic effect as compared with the other three groups of drugs.
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"Four properties" of Chinese herb is the core content of drug property theory.Modern research on function and substantial property of "four property" has poor progress because there has di erent cognitions,ideas and methods.In this paper,main problems of "four property" are expounded through seven aspects,meanwhile,optional ideas and methods are proposed.