Modern Pharmacological Research Research Articles

An Ethnopharmacological, Phytochemical and Pharmacological Review of the Genus Meconopsis.

The Meconopsis plants (Chinese: ), belonging to the family Papaveraceae, have been used as traditional Tibetan medicine (TTM) for thousands of years. Meconopsis has the effects of clearing heat, reducing swelling, and easing pain, and is mainly prescribed for heat syndromes, hepatitis, pneumonia, and pain in joints. Phytochemical studies have revealed the presence of major isoquinoline alkaloids and flavonoids. Modern pharmacological research has demonstrated its antitumor, hepatoprotective, analgestic, antimicrobial, anti-oxidant, antitussive, and anti-inflammatory activities. However, resource availability, in-depth in vivo pharmacological study and qualitative and quantitative analysis are still insufficient and deserve further efforts. This paper provides a comprehensive advance on the ethnopharmacological, phytochemical, and pharmacological studies of the genus, in hopes of promoting a better understanding of their medicinal values.

Paresthesia: A Review of Its Definition, Etiology and Treatments in View of the Traditional Medicine.

To search major Islamic Traditional Medicine (ITM) textbooks for definition, etiology and medicinal plants used to manage 'khadar' or 'paresthesia', a common sensory symptom of multiple sclerosis (MS) and peripheral neuropathies. In addition, the conformity of the efficacy of ITM-suggested plants with the findings from modern pharmacological research on MS will be discussed. Data on the medicinal plants used to treat 'khadar' were obtained from major ITM texts. A detailed search in PubMed, ScienceDirect, Scopus and Google Scholar databases was performed to confirm the effects of ITM-mentioned medicinal plants on MS in view of identified pharmacological actions. Moringa oleifera Lam., Aloe vera (L.) Burm.f., Euphorbia species, Citrullus colocynthis (L.) Schrad., and Costus speciosus (Koen ex. Retz) Sm. are among the most effective ITM plants for the management of 'khadar'. Recent experimental evidence confirms the effectiveness of the mentioned plants in ameliorating MS symptoms. Moreover, according to ITM, prolonged exposure to cold and consuming foodstuff with cold temperament might be involved in the etiopathogenesis of MS. The use of traditional knowledge can help finding neglected risk factors as well as effective and safe therapeutic approaches, phytomedicines and dietary habits for the management of paresthesia and related disorders such as MS.

Studies on flavonoids from Derris eriocarpa

Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before. In our further research on the ethyl acetate of this plant, nine flavone compounds were obtained by column chromatography on silica gel, Sephadex LH-20, semi-prep HPLC, polyamide column chromatography and recrystallization for separation and purification. The structures were determined on the basis of extensive spectroscopic analysis, including MS, NMR experiments and comparison with spectroscopic data in the literature, respectively, as diosmetin (1), 3, 3'-di-O-methylquercetin (2), afromosin (3), 6, 3'-dihydroxy-7, 4'-dimethoxyisoflavone (4), odoratin (5), 7, 3'-dihydroxy-8, 4'-dimethoxyisoflavone (6), 6, 4'-dihydroxy-7, 3'-dimethoxyisoflavone (7), 5, 7, 4'-trihydroxy-3, 3', 5'-trimethoxyflavone (8), and alpinumisoflavone (9). All these compounds were isolated from Derris eriocarpa How for the first time. And the in vitro assays showed that compound 2 possessed moderate inhibitory activity against human cancer cells K562 and HEL.

Health Effects of Small Volatile Compounds from East Asian Medicinal Mushrooms

Medicinal fungi, taken whole or as various forms of extracts, have been used to alleviate, cure or prevent human ailments since pre-historic times. In particular, Asian cultures have incorporated a variety of mushrooms into their medical practices. Chemically pure, bioactive metabolites from fungi have been a mainstay of modern pharmacological research and in addition to antibiotics, include anticancer agents, immunosuppressants, enzyme inhibitors, antagonist and agonists of hormones, and a variety of psychotropic substances. However, to date not many studies have focused on the possible health benefits of odorant volatile organic compounds (i.e., gas phase compounds). An analysis of these compounds for their health related effects will expand the range of compounds available for the treatment of chronic and acute diseases. This review highlights phenolic acids and monoterpenes from Asian medicinal mushrooms (AMMs), which not only produce pleasant odors but also have antioxidant and antibacterial effects. Odorant bioactive volatile phase compounds from medicinal mushrooms remain an essentially untapped source for future medicines, and AMMs remain a promising resource for future pharmacological research.

Effect of Rhizoma coptidis (Huang Lian) on Treating Diabetes Mellitus.

The rapidly increasing diabetes mellitus (DM) is becoming a major public health issue globally; considerable progress has been made in the field of western hypoglycemic drug and insulin, but some shortages still exist. As one of the most important parts in complementary and alternative therapies, traditional Chinese medicine (TCM) performs a good clinical practice and is showing a bright future in the treatment of DM. TCM therapy has certain advantages of less toxicity and/or side effects, and Chinese herbal medicine which usually contains various active ingredients could provide multiple therapeutic effects. Huang Lian (Rhizoma coptidis, RC) is a herb frequently used in many traditional formulas for properties of “clearing damp-heat, quenching fire, and counteracting poison” in Asia for centuries. In this review, we summarize the application of RC in the treatment of DM from two aspects of contents. Firstly, theoretical principles are explained, including the properties and related records about RC in ancient references and modern pharmacological researches and pharmacokinetics on RC and its active components. Secondly, the clinical application of RC is mainly reviewed, such as applicable stage and syndrome, the reasonable dose range, the preparation formulations, and the toxicity and/or side effects and solutions to its adverse actions. This review provides scientific evidence about the effective components, pharmacological researches, and toxicity of RC, as well as introducing traditional Chinese medical theory and clinical experience, in order to guide clinician to use RC more suitably and reasonably in the clinical practice.

Breviscapine listed on progress of new varieties and dosage form research

Breviscapine, a flavone glucuronide, is a cardiovascular medicine extracted from a Chinese herb Erigeron breviscapinus. Modern pharmacological research shows breviscapine has a therapeutic effect on cardiovascular diseases such as cerebral thrombus,cerebral ischemia hemiparesis and platelet aggregation et al. However, its poor water solubility and low bioavailability in vivo severely restrict the clinical application. In this article, we reviewed the marketing preparations of breviscapine and its research progress on the new dosage forms.

Study on attenuate and synergistic mechanism between Aconiti Lateralis Praeparata Radix and Glycyrrhizae Radix for toxicity reduction based on metabonomic of MI-RI mouse cardiomyocytes

Sini decoction (SND), a classical traditional Chinese medicine emergency formula recorded in Shanghan Lun (Treatise on Febrile Diseases), which is composed of Aconiti Lateralis Preparata Radix, Glycyrrhizae Preparata Radix and Zingiberis Rhizoma. Modern clinical and pharmacological researches have shown that SND can protect the myocardium effectively during myocardial ischemia reperfusion injury (MI-RI). A myocardial ischemia reperfusion injury model of H9c2 cardiomyocytes in vitro has been established. Four groups, control group, MI-RI Model group, SND group and SND without Glycyrrhizae Radix group, were arranged. The livability, the level of LDH and CK activity in H9c2 cardiomyocytes in different groups were tested. By combining with principal components analysis (PCA), partial least squares discriminant analysis (PLS-DA), orthogonal partial least squares projection of latent structures-discriminant analysis (OPLS-DA), 17 biomarkers in extracellular fluid were identified and 15 of them were related to the pathway of biological processes. The results showed that the attenuate and synergistic mechanism between Aconiti Lateralis Praeparata Radix and Glycyrrhizae Radix for toxicity reduction was related with the glycolysis, lipid metabolism, citrate cycle and nitrogen metabolism of amino acids metabolism. The study proved the effect on H9c2 cardiomyocyte treated by MI-RI injury both SND group and SND without Glycyrrhizae Radix group, and compared with the SND without Glycyrrhizae Radix, the protective effect of myocardial ischemia reperfusion injury model of H9c2 cardiomyocyte from SND was stronger.

Studies on resin purification process optimization of Eucommia ulmoides Oliver and its antihypertensive effect mechanism.

Through research it is found that the barks, stems, fruits and flowers of Eucommia ulmoides contain various compositions, such as lignin, cycloalkane and phenylpropanoids. The modern pharmacological research shows that Eucommia ulmoides has many functions, such as anti-aging, antitumor and bone cell proliferation. This paper studied the resin purification process optimization conditions and antihypertensive effect of Eucommia ulmoides Oliver. The orthogonal experiment method was adopted to determine the purification effect of various macro-porous resins for eucommia ulmoides Oliver, and the SHR model was used to determine antihypertensive level of eucommia ulmoides Oliver. The optimal process of resin extraction and purification of Eucommia ulmoides Oliver was verified through the loading liquid concentration at 6 mg/ml, 20% ethanol used as the eluent; the flow rate control was 3.0, column volume per hour and the diameter-height ratio of adsorption column was 1:6; the extracts of Eucommia ulmoides Oliver can reduce SHR blood pressure, its antihypertensive effect is relatively stable and has no significant impact on HR, but the antihypertensive effect is lower than that of control medicine captopril. Also, the extracts of eucommia ulmoides Oliver can significantly increase the content of serum NO and reduce the content of ET. The Eucommia ulmoides Oliver can relax blood vessels, reduce the peripheral resistance, reduce the returned blood volume, and eventually achieve the antihypertensive effect.

Comparative proteomic analysis of the sun- and freeze-dried earthworm Eisenia fetida with differentially thrombolytic activities

The dried earthworm is a traditional thrombolytic medicine in East Asia. Its thrombolytic mechanism has been extensively studied. However, the effects of drying process on thrombolysis were rarely investigated. Herein, we compared the thrombolytic activity of earthworm Eisenia fetida processed by sun-drying to that by freeze-drying. Fibrin plate and blood clot lysis assays showed that freeze-dried earthworms gave dramatically higher fibrinolytic and thrombolytic activities than the sun-dried earthworms. To address the thrombolytic difference, comparative proteomic analysis was carried out using fibrin zymography and two-dimensional gel electrophoresis (2-DE). The freeze- and sun-dried earthworms generated remarkably different 2-DE protein spot patterns. A total of 126 differential protein spots were detected, 83 of them were identified by matrix-assisted laser desorption/ionization-tandem time-of-flight mass spectrometry and database searching with 13 quantitative changes and 70 qualitative changes. Five of these differential proteins were identified as fibrinolytic proteases (lumbrokinases), responsible for dissolving fibrin, the main protein component of thrombus. The total abundance of these fibrinolytic proteases in the freeze-dried earthworms was significantly higher, consistent with the results of fibrin zymography. Therefore, the higher concentration of fibrinolytic enzymes along with their broad substrate specificity explained the stronger fibrinolytic and thrombolytic activities of the freeze-dried earthworms. This study suggests that freeze-drying represents an improved processing method for earthworm as the thrombolytic therapy in the future. Thrombosis has become one of the biggest concerns all over the world. The dried earthworms have been intensively used as thrombolytic agents. Its thrombotic mechanism has been studied by the modern pharmacological researches. However, the drying procedure of the earthworm and its effects on the thrombolysis were rarely investigated. The present study compared the thrombolytic effects of the freeze-dried and the normal dried earthworm E. fetida. To better understand the underlying mechanisms for differential thrombolytic effects, the fibrin zymography and the two-dimensional gel electrophoresis (2-DE) were employed to identify sets of differential proteins. Therefore, this study provides not only the comparative proteomic analysis but also molecular mechanism underlying the differential thrombolytic effects.

Review of pharmacological activities of Dendrobium officinale based on traditional functions

This review firstly made a summary of ancient literature on traditional functions of Dendrobium, combined with literature of modern pharmacological research and clinical application of D. officinale from CNKI search system, it was summarized that D. officinale had broad bioactivities including immunomodulation, antifatigue activity, antioxidation, digest-promotion, stimulation of salivary secretion, lowering hyperglycemia, anti-hypertension, anti liver injury and antitumor activity, etc. Furthermore, public healty needs and present situation of cooperative product development were analyzed base on tradtional functions, pharmacological actions and related clinical applications of D. officinale, could provide a reference for the further industrial development.

Development and stability of semisolid preparations based on Gardenia jasminoides Ellis extract

The fruit of Gardenia jasminoides Ellis has been traditionally used as a Chinese medicine for centuries in China, as well as in other Asian countries [1]. The major and characteristic constituents of Gardenia fruit are iridoid glycosides such as geniposide, gardenoside, genipin-1-β-gentiobioside, geniposidic acid, acetylgeniposide, scandoside methyl ester, shanzhiside and gardoside. Modern clinical and pharmacological research has revealed that Gardenia fruit has anti-inflammatory properties, cytotoxic effects, as well as protective against oxidative damage [1,2]. In the Chinese Pharmacopoeia a topical application of the fruit of gardenia, powdered and mixed with water is reported [8]. Gardenia fruit also represents the principal effective ingredient of a preparation with antiinflammatory and analgesic properties, „Zhongtong Caji“, a kind of liniment for external use, formulated with more than ten different herbal drugs [3].

English

Mushrooms had long been used for medicinal and food purposes since decades. It is now increasingly recognized that correct diet, controls and modulates many functions of human body and consequently participates in the maintenance of state of good health, necessary to reduce the risk of many diseases. Modern pharmacological research confirms large parts of traditional knowledge regarding the medicinal effects of mushrooms due to their antifungal, antibacterial, antioxidant and antiviral properties, besides being used as functional foods. This paper sums up diverse beneficial health effects of mushrooms to humans, in the form of proteins, carbohydrates, fats, vitamins, minerals, food and drugs, and medicines.    Key words: Mushrooms, medicine, food, properties

Identification of active compounds and their metabolites by high‐performance liquid chromatography/electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry from Xiao‐xu‐ming decoction (XXMD)

Xiao-xu-ming decoction (XXMD) prescription is a traditional Chinese prescription that has been widely used to treat theoplegia and the sequela of theoplegia. Modern pharmacological research has also indicated that the active fraction from XXMD is able to treat cardiovascular diseases and Alzheimer's disease. In the study reported here, high-performance liquid chromatography coupled with Fourier transform ion cyclotron resonance mass spectrometry (HPLC/FTICR-MS) was developed to identify active compounds and their metabolites after oral administration of active fraction from Xiao-xu-ming decoction to rats, using parent mass list triggered data-dependent multiple-stage mass analysis at a resolving power of 100,000 in the external calibration mode. The mass accuracies obtained for full-scan MS were within 2 ppm in most cases. Fifteen constituents were identified in the active fraction from XXMD and the biological samples of rats. The fragmentation behaviors of these constituents were summarized which would be helpful for structural characterization. The profiles of the constituents in the active fraction and biological samples of rats were obtained which provided us with much information for a better understanding of the chemical basis of the pharmacologic actions of XXMD.

Effects of naringin on the proliferation and osteogenic differentiation of human bone mesenchymal stem cell

Rhizoma drynariae is used commonly in the treatment of osteoporosis and bone nonunion in traditional Chinese medicine. Modern pharmacological research indicates that naringin is the main effective component of rhizoma drynariae, which can induce the expression of the osteogenic marker in the osteoblast cell line. However, no former study has described its effect on bone mesenchymal stem cells (BMSCs). In our experiment, we co-cultured human BMSCs with different concentrations of naringin solution, then the osteogenic differentiation markers and proliferation ability were analyzed. The results indicated that a certain concentration (1–100 μg/ml) of the naringin solution may enhance the proliferation and osteogenic differentiation of human BMSCs. Also, our research explains excellently the anti-osteoporotic and bone nonunion treatment mechanism of rhizoma drynariae, thus contributing to the exploration of osteogenic differentiation agents from Chinese herbs.

Dopamine transporter mutant mice in experimental neuropharmacology

An opportunity to perform targeted genetic manipulations in mice has provided another dimension for modern pharmacological research. Genetically modified mice have become important tools to investigate functions of previously unexplored proteins, define mechanism of action of new and known pharmacological drugs, and validate novel targets for treatment of human disorders. One of the best examples of such use of genetic models in experimental pharmacology represents investigations involving mice deficient in the gene encoding the dopamine transporter (DAT). The dopamine transporter tightly regulates the extracellular dynamics of dopamine by recapturing released neurotransmitter into the presynaptic terminals, and genetic deletion of this protein results in profound alterations in both the presynaptic homeostasis and the extracellular dynamics of dopamine. By using this model of severe dopaminergic dysregulation, significant progress has been made in defining the major target of psychotropic drugs, understanding the mechanisms of their action, unraveling novel signaling events relevant for dopaminergic transmission, and mapping neuronal pathways involved in dopamine-related behaviors. Furthermore, DAT mutant mice provided an opportunity to model in vivo conditions of extreme dopaminergic dysfunction that could be relevant for human disorders such as ADHD, schizophrenia, and Parkinson's disease and, thus, could serve as test systems for developing novel treatments for these and related disorders.

Discrete Chemical Release From a Microfluidic Chip

We demonstrate a discrete chemical release method, capable of delivering picoliter volumes of chemical solutions with 100 mum of spatial resolution and 20 mus of response time. The releasing mechanism is based on the transfer of pulsed liquid plugs through a hydrophobic air chamber. A microfluidic chip consisting of such a releasing array (2 times 10) is designed and fabricated. Numerical simulation and experimental testing are performed to verify the working principle. Advantages of this release-on-demand technology include leakage-free, fast response and versatile control of release profile. This new method could be a key enabling technology for precisely controlled release of biochemicals for modern pharmacological and biological research.

Isolated heart perfusion according to Langendorff—Still viable in the new millennium

The isolated perfused mammalian heart preparation was established in 1897 by Oscar Langendorff. The method was developed on the basis of the isolated perfused frog heart established by Elias Cyon at the Carl Ludwig Institute of Physiology in Leipzig, Germany in 1866. Observations made using both methods at the end of the 19th and at the beginning of the 20th century led to important discoveries, forming the basis for our understanding of heart physiology. This included the role of temperature, oxygen and calcium ions for heart contractile function, the origin of cardiac electrical activity in the atrium, the negative chronotropic effect of vagus stimulation and the chemical transmission of impulses in the vagus nerve by acetylcholine. Langendorff himself demonstrated that the heart receives its nutrients and oxygen from blood via the coronary arteries and that cardiac mechanical function is reflected by changes in the coronary circulation. The method underwent many modifications but its general principle remains the same today. Blood, or more commonly crystalloid perfusates, are delivered into the heart through a cannula inserted in the ascending aorta, either at constant pressure or constant flow. Retrograde flow in the aorta closes the leaflets of the aortic valve and as a consequence, the entire perfusate enters the coronary arteries via the ostia at the aortic root. After passing through the coronary circulation the perfusate drains into the right atrium via the coronary sinus. The simplicity of the isolated mammalian heart preparation, the broad spectrum of measurements which can be done using this method, its high reproducibility and relatively low cost make it a very useful tool in modern cardiovascular and pharmacological research, in spite of a few shortcomings. In the last decade the method has brought many important advances in many areas including ischemia–reperfusion injury, cell-based therapy and donor heart preservation for transplant.

The quality and safety of traditional traditional Chinese medicines

Modern chemical and pharmacological research has greatly contributed to our understanding of

Evidence of increased keratinocyte proliferation in air-liquid interface cultures of non-bullous congenital ichthyosiform erythroderma.

Modern pharmacological and dermatological research requires the use of appropriate in vitro models which permit a faithful reproduction of various aspects of the in situ situation. The air-exposed culture of keratinocytes on dead de-epidermized dermis is one of the best models of in vitro epidermal differentiation known at the moment. In this study, we verified the model's validity for the reproduction of a hyperproliferative genodermatosis: non-bullous congenital ichthyosiform erythroderma. We used subcultured epidermal keratinocytes originating from normal and ichthyotic patients. Light and electron microscopy of pathological cultures disclosed, on day 14, a terminally differentiated epidermis with a marked granular layer and hyperkeratosis which, however, was not dramatically different from the normal controls. On day 25, the normal cultures displayed an even more pronounced hyperkeratosis and hypergranulosis, whereas the reconstructed epidermis of pathological origin presented a considerable reduction of the viable non-keratinized compartment and a focal parakeratosis. Indirect immunofluorescence revealed the expression of several differentiation markers which were not observed in the immersed culture models (e.g. the desmosome- and differentiation-related antigens KM48 and G36-19). Abundant keratohyalin granules were stained with AKH1 antibody and observed even in the deep epidermal layers, but no profilaggrin-filaggrin conversion could be detected biochemically.(ABSTRACT TRUNCATED AT 250 WORDS)

Estimation of sound-velocity by the method of coincidences

The isolated perfused mammalian heart preparation was established in 1897 by Oscar Langendorff. The method was developed on the basis of the isolated perfused frog heart established by Elias Cyon at the Carl Ludwig Institute of Physiology in Leipzig, Germany in 1866. Observations made using both methods at the end of the 19th and at the beginning of the 20th century led to important discoveries, forming the basis for our understanding of heart physiology. This included the role of temperature, oxygen and calcium ions for heart contractile function, the origin of cardiac electrical activity in the atrium, the negative chronotropic effect of vagus stimulation and the chemical transmission of impulses in the vagus nerve by acetylcholine. Langendorff himself demonstrated that the heart receives its nutrients and oxygen from blood via the coronary arteries and that cardiac mechanical function is reflected by changes in the coronary circulation.The method underwent many modifications but its general principle remains the same today. Blood, or more commonly crystalloid perfusates, are delivered into the heart through a cannula inserted in the ascending aorta, either at constant pressure or constant flow. Retrograde flow in the aorta closes the leaflets of the aortic valve and as a consequence, the entire perfusate enters the coronary arteries via the ostia at the aortic root. After passing through the coronary circulation the perfusate drains into the right atrium via the coronary sinus.The simplicity of the isolated mammalian heart preparation, the broad spectrum of measurements which can be done using this method, its high reproducibility and relatively low cost make it a very useful tool in modern cardiovascular and pharmacological research, in spite of a few shortcomings. In the last decade the method has brought many important advances in many areas including ischemia–reperfusion injury, cell-based therapy and donor heart preservation for transplant.