Research Interests: Complementary and Alternative Medicine, Biology, Inflammation, Medicine, Humans, and 15 moreIntestinal Mucosa, Brassicaceae, Animals, Male, Jejunum, Behavioral Animal Models, mRna expression levels, Angiosperms, Monocytes, Motor Function, Gastrointestinal motility, Ileum, Interleukin, Drug combinations, and mRNA expression
Nachdem 2015 / 2016 die ersten 4 Module der Fortbildungsreihe „Phytopharmaka und Phytotherapie“ erfolgreich durchgeführt wurden und 11 Teilnehmer ihr Zertifikat „Phytotherapeut“ (siehe Zeitschrift für Phytotherapie 2 / 2017) erhielten,... more
Nachdem 2015 / 2016 die ersten 4 Module der Fortbildungsreihe „Phytopharmaka und Phytotherapie“ erfolgreich durchgeführt wurden und 11 Teilnehmer ihr Zertifikat „Phytotherapeut“ (siehe Zeitschrift für Phytotherapie 2 / 2017) erhielten, fand das 1. Modul der neuen Serie vom 31.3.–2.4.2017 wiederum im Lindner Sport & Aktiv Hotel Kranichhöhe, Much / Bergisches Land statt, an dem 13 Teilnehmer begrüßt werden konnten.
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
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The mechanical activity of longitudinal and circular smooth muscle preparations from fundus, corpus, and antrum of guinea pig stomach and distal ileum of guinea pig were recorded and the effect of substance P (SP) was measured. In... more
The mechanical activity of longitudinal and circular smooth muscle preparations from fundus, corpus, and antrum of guinea pig stomach and distal ileum of guinea pig were recorded and the effect of substance P (SP) was measured. In physiological concentrations (10(-13) - 10(-7) mol/l) SP activates the tone of circular muscle strips from fundus and corpus of guinea pig stomach. Quite opposite is the situation with respect to the SP tonic activation in the muscle layers of guinea pig ileum. Here SP activates only the tone of longitudinal muscle layers. In these concentrations SP induces no or only very small contractile response in longitudinal muscle strips of fundus and corpus and in circular muscle preparations of distal ileum. The greater sensitivity to SP appears to result for the longitudinal muscle layer of ileum followed by the circular layer of fundus and corpus.
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Research Interests: Animals, Male, Pharmazie, Rats, Time Factors, and 3 moreMuscle contraction, Naloxone, and Portal vein
The undecapeptide substance P(SP) and its C-terminal sequence SP-5-11 induced a dose-dependent contraction of the isolated guinea pig trachea. SP-5-11 had a more potent bronchoconstrictive action than SP-1-11. The distal part of the... more
The undecapeptide substance P(SP) and its C-terminal sequence SP-5-11 induced a dose-dependent contraction of the isolated guinea pig trachea. SP-5-11 had a more potent bronchoconstrictive action than SP-1-11. The distal part of the isolated guinea pig trachea showed a greater reagibility to SP-5-11 than the proximal one. There was a continuous increase of the amplitude of the SP-1-11-induced contractions when the neuropeptide was added several times at one-hour intervals. Incubation with 10(-6) M SP-1-11 for 5 h reduced the reagibility of the isolated guinea pig trachea to acetylcholine.
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The effects of chronic immobilization stress on the physiological responses of male rats were studied. The results indicate that the SP-like immunoreactivity (SPLIR) is diminished in the adrenals and pituitary after chronic stress. In... more
The effects of chronic immobilization stress on the physiological responses of male rats were studied. The results indicate that the SP-like immunoreactivity (SPLIR) is diminished in the adrenals and pituitary after chronic stress. In vitro noradrenaline (NA) release from adrenals was increased. The i.p. administration of SP during the stress procedure normalized the increased NA release in vitro indicating that the catecholamine secretion may be influenced by SP. On the other hand, in demedullated animals the SPLIR in the pituitary was partly reduced and the blood pressure was increased. In such animals chronic stress resulted in an increase of SPLIR in the pituitary in comparison with nonstressed, demedullated animals, but was without effect on the blood pressure. It is concluded that exposure to SP and the resulting decrease of noradrenaline release may have a significant influence on the pituitary-adrenal responsiveness to stress.
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Substance P (SP) is localized in sensory nerves of the respiratory tract in close connection to the effector cells of inflammatory and allergic bronchial diseases. SP is proposed to play an important role in the pathogenesis of bronchial... more
Substance P (SP) is localized in sensory nerves of the respiratory tract in close connection to the effector cells of inflammatory and allergic bronchial diseases. SP is proposed to play an important role in the pathogenesis of bronchial asthma because of its ability to induce bronchoconstriction, vasodilatation and an edema of the mucous membrane and to enhance the secretion of tracheobronchial glands. Furthermore inflammatory and immune cells are influenced by SP. SP seems to have a complex action in the regulation of the bronchial tonus. Especially differences in the action of partial sequences of the peptide may be important in the pathogenesis of asthma.
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Cholecystokinin 7 (CCK 7), a synthetic analogue of cholecystokinin/pancreozymin (CCK 33), increased in a dose-dependent manner the tone of the guinea-pig ileal, gastric and gall bladder smooth muscle preparations. In all these... more
Cholecystokinin 7 (CCK 7), a synthetic analogue of cholecystokinin/pancreozymin (CCK 33), increased in a dose-dependent manner the tone of the guinea-pig ileal, gastric and gall bladder smooth muscle preparations. In all these preparations CCK 7 was more potent than CCK 8 and CCK 33 and all three cholecystokinins were more potent than acetylcholine (ACH). Atropine and tetrodotoxin (TTX) did not influence the CCK 7 action in fundus and gall bladder muscle strips but reduced non-competitively its effect in ileal muscle strips. Neither GE 410 nor dbcGMP affected the ACH and histamine (His) response of the muscle strips but both antagonists shifted the dose-response curve of CCK 7 to the right, GE 410 (cholecystokinin antagonist) being a much more potent antagonist of CCK 7 as compared to dbcGMP. In all muscle strips a competitive action on the CCK 7 responses was found for GE 410. In gastric muscle strips a competitive influence on the CCK 7 responses was found for dbcGMP at low concentration (1 x 10(-5)M) and a non-competitive influence at high concentration (5 x 10(-4)M). The results suggest that the contractile effects of CCK 7 in the isolated ileal smooth muscle are realized by cholinergic and direct myogenic mechanisms, whereas in the isolated gall bladder and gastric smooth muscles, by a direct myogenic mechanism only.
Research Interests: Smooth muscle, Female, Animals, Male, Gallbladder, and 4 moreTetrodotoxin, Atropine, Stomach, and Ileum
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Substance P (SP)/Neurokinin 1 (NK1) receptor pathways have been repeatedly implicated in the pathophysiology of central, pulmonary, and gastric disorders. A large body of evidence that has been generated from animal experiments indicates... more
Substance P (SP)/Neurokinin 1 (NK1) receptor pathways have been repeatedly implicated in the pathophysiology of central, pulmonary, and gastric disorders. A large body of evidence that has been generated from animal experiments indicates that treatment with selective NK1 receptor antagonists might be effective in the treatment of certain forms of disorders, analgesia, depression, migraine, asthma, or gastrointestinal disorders. Accordingly, numerous NK1 receptor antagonists have either been synthesized and are under clinical development, or have already been tested in clinical trials. However, the initial encouraging clinical results were followed by repeated demonstration of a lack of effectiveness. Up to now, only one NK1 receptor antagonist, aprepitant, is available for therapeutical use. Aprepitant is a selective high-affinity human SP/NK1 receptor antagonist approved by the FDA in 2003. Aprepitant is indicated for prophylaxis of acute- and delayed-phase nausea and emesis caused by chemotherapy regimens. It is used in combination with a 5-hydroxytryptamine (5-HT3) antagonist and a corticosteroid. It is the first antiemetic agent that acts by binding the NK1 receptor. Research continues and novel molecules may show better pharmacokinetic and pharmacodynamic properties and, therefore, may achieve therapeutic success.
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Synthesized in 1990 as an anticonvulsant agent, pregabalin was designed as a lipophilic gamma-aminobutyric acid (GABA) analog substituted at the 3'-position in order to facilitate diffusion across the blood-brain barrier. It is an... more
Synthesized in 1990 as an anticonvulsant agent, pregabalin was designed as a lipophilic gamma-aminobutyric acid (GABA) analog substituted at the 3'-position in order to facilitate diffusion across the blood-brain barrier. It is an alpha2delta1 ligand that binds to, and modulates, voltage-gated calcium channels. This modulation is characterized by a reduction of the excessive neurotransmitter release that is observed in certain neurologic and psychotic disorders. Pregabalin has analgetic, anticonvulsant, and anxiolytic activity and has demonstrated efficacy in the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, and as adjuvant therapy for adult patients with partial onset seizures. Pregabalin was significantly more effective than placebo for the treatment of generalized anxiety disorder as well as of fibromyalgia and was well tolerated by most of the patients.
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Postmarketing surveillance of prescription medicines is a routine practice, yet similar evaluation of non-prescription medicines is uncommon. In order to get insights into the validity of pharmacy-based observational studies 22... more
Postmarketing surveillance of prescription medicines is a routine practice, yet similar evaluation of non-prescription medicines is uncommon. In order to get insights into the validity of pharmacy-based observational studies 22 postmarketing surveillance studies in the German community of pharmacies involving non-prescription medications have been investigated. The objective was to evaluate their contribution to the knowledge about drug use in self-medication. The results of the comparative evolution show that postmarketing surveillance studies with non-prescription medications deliver valid and meaningful findings about the usage, effectiveness and safety. Statements to the efficacy of the drug often serve marketing interests.
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Irritable bowel syndrome is a common functional disorder of the gut. The cause is not known. Symptoms can be quite variable and include abdominal pain, bloating, and sometimes bouts of diarrhea and/or constipation. It causes a great deal... more
Irritable bowel syndrome is a common functional disorder of the gut. The cause is not known. Symptoms can be quite variable and include abdominal pain, bloating, and sometimes bouts of diarrhea and/or constipation. It causes a great deal of discomfort and distress, but it does not permanently harm the intestine and does not lead to a serious disease, such as cancer. There are numerous treatment options in functional gastrointestinal disorders acting peripherally by influencing motility and visceral sensitivity. However, older 5-HT4 receptor agonists had limited clinical success because they were associated with changes in the cardiac function. New generation 5-HT4 receptor agonists, 5-HT, antagonists or partial antagonists are promising approaches to treat gastrointestinal dysmotility, particularly colonic diseases. A further new approach is the activation of chloride cannels within the gastrointestinal wall by the prostaglandin E metabolite lubiprostone. In patients with chronic co...
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Page 1. ORIGINAL PAPER Adenosine A1 receptor: Functional receptor-receptor interactions in the brain Kathrin Sichardt & Karen Nieber Received: 23 July 2007 /Accepted: 24 July 2007 / Published online: 5 September 2007 © Springer... more
Page 1. ORIGINAL PAPER Adenosine A1 receptor: Functional receptor-receptor interactions in the brain Kathrin Sichardt & Karen Nieber Received: 23 July 2007 /Accepted: 24 July 2007 / Published online: 5 September 2007 © Springer Science + Business Media BV 2007 ...
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Research Interests: Pharmacology and Germany
Patients with functional gastrointestinal disorders constitute the majority of patients seeking healthcare for gastrointestinal symptoms in primary and secondary care. Of these disorders irritable bowel syndrome (IBS) is one of the most... more
Patients with functional gastrointestinal disorders constitute the majority of patients seeking healthcare for gastrointestinal symptoms in primary and secondary care. Of these disorders irritable bowel syndrome (IBS) is one of the most common and affects 10-20% in the Western world. IBS is a functional bowel disorder characterized by chronic abdominal pain, discomfort, bloating, and alteration of bowel habits in the absence of any detectable organic cause. Sex and gender aspects are important in understanding differences between men and women in their risk and experience of IBS. Relative to men, women are diagnosed more frequently with IBS. Female patients are more likely to be constipated, complain of abdominal distension and of certain extracolonic symptoms. Given the variability of IBS, the most successful treatment will be comprehensive, involving multiple strategies. Efficacy, safety and tolerability are important in the evaluation of IBS therapies, as patients are likely to r...
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Myrrh is the oleo-gum resin of mainly Commiphora molmol and as a powdered substance, one compound in the traditional medicinal product Myrrhinil-Intest®, which has been used for the treatment of unspecific, inflammatory intestinal... more
Myrrh is the oleo-gum resin of mainly Commiphora molmol and as a powdered substance, one compound in the traditional medicinal product Myrrhinil-Intest®, which has been used for the treatment of unspecific, inflammatory intestinal disorders. The aim of the present study was to evaluate the antispasmodic effect of myrrh under healthy and inflamed conditions, and to evaluate a calcium-antagonistic effect as a possible mode of action. Therefore, an ethanolic myrrh extract was tested for its effects on muscle tone and acetylcholine-induced contractions in untreated and inflamed rat ileum/jejunum preparations. Inflammation was experimentally induced by 2,4,6-trinitrobenzene sulfonic acid (10 mM, 30 min). Additionally, the effect of the calcium channel agonist Bay K8644 in the presence of varying myrrh extract concentrations was examined. Myrrh extract (0.99 mg/mL) suppressed the acetylcholine-induced contraction down to 25.8 % in untreated and 15.2 % in inflamed preparations. Myrrh extract (0.15; 0.25 and 0.35 mg/mL) induced a concentration-dependent rightward shift of the Bay K8644 concentration-response curve in untreated and inflamed preparations with a significant EC50 shift. Schild analysis resulted in a pA2 value of 0.93 for untreated preparations. Increasing myrrh extract concentrations induced a concentration-dependent decrease of the agonistic maximum effect in untreated and inflamed preparations down to 15.8 % and 25.8 %, respectively, for the highest concentration leading to a pD2 value of 0.58. Myrrh extract reduced intestinal muscle tone and acetylcholine-induced contraction of untreated and inflamed ileum/jejunum preparations based on dual calcium antagonism characterized by a right shift of the agonistic dose-response curve and a depression of the maximum effect. The resulting reduction of intestinal motility and spasmolytic effects provide a rationale for the symptom treatment of intestinal disorders such as irritable bowel syndrome.
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Traumatic brain injury is a leading cause of death and disability in children. Studies using adult animal models showed alterations of the central cholinergic neurotransmission as a result of trauma. However, there is a lack of knowledge... more
Traumatic brain injury is a leading cause of death and disability in children. Studies using adult animal models showed alterations of the central cholinergic neurotransmission as a result of trauma. However, there is a lack of knowledge about consequences of brain trauma on cholinergic function in the immature brain. It is hypothesized that trauma affects the relative acetylcholine esterase activity and causes a loss of cholinergic neurons in the immature brain. Severe fluid percussion trauma (FP-TBI, 3.8+/-0.3atm) was induced in 15 female newborn piglets, monitored for 6h and compared with 12 control animals. The hemispheres ipsilateral to FP-TBI obtained from seven piglets were used for acetylcholine esterase histochemistry on frozen sagittal slices, while regional cerebral blood flow and oxygen availability was determined in the remaining eight FP-TBI animals. Post-fixed slices were immunohistochemically labelled for choline acetyltransferase as well as for low-affinity neurotro...
Research Interests: Cognitive Science, Traumatic Brain Injury, Developmental neuroscience, Immunohistochemistry, Brain, and 17 moreFemale, Animals, Acetylcholinesterase, Animal Model, Acetylcholine, Basal forebrain, Neurons, Fluorescent Antibody Technique, Oxygen, Time Factors, Swine, Regional Cerebral Blood Flow, Neurosciences, Oxidation-Reduction, Choline Acetyltransferase, Fluid Percussion Injury, and Brain injuries
Research Interests: Inflammation, Drug interactions, Cell line, Humans, Lung, and 15 moreHYDROCARBONS, IL, Polycyclic aromatic hydrocarbons (PAHs), VOC, Epithelial cells, Tumor necrosis factor-alpha, In Vitro Toxicology, Thiazoles, Cell Survival, Enzyme Linked Immunosorbent Assay, Organic Chemicals, Volatile organic compound, Indoor air, Volatilization, and Interleukin
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ABSTRACT
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Herbal medicinal products have been used since several decades for the health care of children. Nevertheless, well-controlled clinical studies with herbal medicinal products for children are rare. The authors' objective... more
Herbal medicinal products have been used since several decades for the health care of children. Nevertheless, well-controlled clinical studies with herbal medicinal products for children are rare. The authors' objective therefore was to evaluate clinical trials with herbal medicinal products in children, based on a literature search in PubMed and Web of Science. A total of 133 trials were identified. 90 studies were randomized, 32.2% were randomized and double-blinded. Most studies were performed in China, in the age group 6-12 years, and in children with respiratory diseases, most often herbal medicinal products with Hedera helix were tested. The analysis revealed that studies on herbal medicinal products were feasible in children. Although clinical trials have been found, this literature search have limitations and did not cover all studies performed. However, only few clinical trials of high quality were identified. Further studies therefore are urgently needed to support the good empirical findings.
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In this study we evaluated the adenosine A1 receptor-mediated effect of valerian extract (Ze 911) on postsynaptic potentials (PSPs) in pyramidal cells of the rat cingulate cortex in a slice preparation. We first observed that... more
In this study we evaluated the adenosine A1 receptor-mediated effect of valerian extract (Ze 911) on postsynaptic potentials (PSPs) in pyramidal cells of the rat cingulate cortex in a slice preparation. We first observed that N6-cyclopentyladenosine (CPA, 0.01 - 10 microM), an adenosine A1 receptor agonist, inhibited PSPs in a concentration-dependent manner. The CPA (10 microM)-induced inhibition was antagonized by 1,3-dipropyl-8-cyclopentylxanthine (DPCPX, 0.1 microM), an adenosine A1 receptor antagonist. Ze 911 concentration dependently (0.1 - 15 mg/mL) inhibited PSPs in the presence of the adenosine A2A receptor antagonist 1,3,7-trimethyl-8-(3-chlorostyryl)xanthine (CSC, 0.2 microM) and adenosine deaminase (1 U/mL). The maximal inhibition induced by 10 mg/mL was completely antagonised by DPCPX (0.1 microM), an A1 receptor blocker. The data suggest that activation of adenosine A1 receptors is involved in the pharmacological effects of the valerian extract Ze 911.
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Valeriana officinalis (valerian) is used traditionally as a mild sedative. Research into valerian is sparse, and studies differ greatly with respect to design, measures and preparations used. This study compares the action of a methanol... more
Valeriana officinalis (valerian) is used traditionally as a mild sedative. Research into valerian is sparse, and studies differ greatly with respect to design, measures and preparations used. This study compares the action of a methanol (M-E), ethanol (E-E) and an extract macerated with ethylacetate (EA-E) from roots of valerian (Valeriana officinalis L., Valerianaceae) on postsynaptic potentials (PSPs) in cortical neurons. Intracellular recordings were performed in rat brain slice preparations containing pyramidal cells of the cingulate cortex. PSPs were induced by electrical field stimulation. The M-E induced strong inhibition in the concentration range 0.1-15 mg/mL, whereas the E-E (1-10 mg/mL) did not influence significantly the PSPs. The maximum inhibition induced by the M-E was completely antagonized by 1,3-dipropyl-8-cyclopentylxanthine (DPCPX, 0.1 microm), an antagonist on the adenosine A(1) receptor. Contrary to the M-E, the EA-E (10 mg/mL) induced an increase of the PSPs, which was completely blocked by the GABA(A) receptor antagonist picrotoxin (100 microm). The data suggest that activation of adenosine A(1) and GABA(A) receptors is mediated by different components within the valerian extract. The two mechanisms may contribute independently to the sleep-inducing effect of valerian.