Hypericum
Perylene
Phloroglucinol
Plant Extracts
Bicyclo Compounds
Plants, Medicinal
Balkan Peninsula
Theales
Herb-Drug Interactions
Chlorogenic Acid
Quercetin
Effects of Hypericum perforatum extraction on alcohol intake in Marchigian Sardinian alcohol-preferring rats. (1/207)
The present study investigated the effect of acute intragastric (i.g.) administration of dry Hypericum perforatum extract (HPE), containing 0.3% hypericin, on ethanol intake in genetically selected Marchigian Sardinian alcohol-preferring (msP) rats. The i.g. administration of HPE, 125 or 250 mg/kg, induced a 30-40% reduction in ethanol intake in rats offered 10% (v/v) ethanol for 2 h/day. The effect of these doses was selective, since they modified neither food intake nor food-associated drinking; neither did the same doses modify the rat's gross behaviour in the open-field test. A dose of 500 mg/kg frequently induced immobility and a general suppression of ingestive behaviour. In rats offered 10% ethanol for 12 h/day, ethanol intake following treatment with 250 mg/kg HPE was significantly lower than that of controls for up to 10 h. The effect on ethanol intake was not related to the antidepressant-like effect of HPE revealed in the forced swimming test. In this regard, the effect on ethanol intake was observed after a single administration of 125 mg/kg, whereas the antidepressant effect was observed only after repeated treatment with doses higher than 125 mg/kg HPE. The i.g. administration of HPE, 250 mg/kg, did not affect blood-alcohol levels following i.g. treatment with 0.7 g/kg ethanol, the amount usually ingested in a single drinking episode; thus, the effect is not related to changes in the pharmacokinetics of ethanol. The present study shows that HPE markedly reduces ethanol intake in msP rats, without significantly modifying food intake. (+info)Attenuation of alcohol intake by extract of Hypericum perforatum (St. John's Wort) in two different strains of alcohol-preferring rats. (2/207)
Extract of the common plant Hypericum perforatum L. (St John's Wort, SJW) has been used successfully for the treatment of mild to moderate depression since ancient times and has recently been studied clinically. Depression and alcoholism have some neurochemical similarities, such as low brain serotonin activities. Thus, we hypothesized that SJW extract, which contains 0.22% hypericin and 4.05% hyperforin, also may be effective in suppressing alcohol intake. To test this hypothesis, the effects of SJW extract on voluntary alcohol intake were studied in two different genetic animal models of human alcoholism: fawn-hooded (FH) and high-alcohol drinking (HAD) rats. FH and HAD rats received a single oral administration (5 ml/kg) of either vehicle or one of the five doses (100, 200, 400, 600, and 800 mg/kg) of SJW extract. The oral administration of SJW extract significantly (P < 0.0001) reduced alcohol intake in both FH and HAD rats. In a third study, FH rats did not develop tolerance to the suppressant effects of SJW on alcohol intake and preference following oral administration of (400 mg/kg) of the extract for 15 consecutive days. These promising findings suggest that SJW extract should be evaluated clinically as a potential therapeutic agent in the treatment of alcoholism. (+info)Hypericum extract versus imipramine or placebo in patients with moderate depression: randomised multicentre study of treatment for eight weeks. (3/207)
OBJECTIVES: To assess the efficacy and safety of hypericum extract (STEI 300, Steiner Arzneimittel, Berlin) compared with imipramine and placebo in patients in primary care with a current episode of moderate depression. DESIGN: Randomised, double blind, multicentre, parallel group trial for 8 weeks. SETTING: Trained panel of 18 general practitioners from four German states: Bavaria, Berlin, Rhineland Palatinate, and Saxony. PARTICIPANTS: 263 patients (66 men, 197 women) with moderate depression according to ICD-10 (international classification of diseases, 10th revision) codes F32. 1 and F33.1. INTERVENTIONS: 1050 mg hypericum extract (350 mg three times daily), 100 mg imipramine (50 mg, 25 mg, and 25 mg daily), or placebo three times daily. MAIN OUTCOME MEASURES: Change from baseline score on the 17 item version of the Hamilton depression scale, the Hamilton anxiety scale, the clinical global impressions scale, Zung's self rating depression scale, and SF-36, and adverse events profile. RESULTS: Hypericum extract was more effective at reducing Hamilton depression scores than placebo and as effective as imipramine (mean -15.4 (SD 8.1), -12.1 (7.4), and -14.2 (7.3) respectively). Comparable results were found for Hamilton anxiety and clinical global impressions scales and were most pronounced for the Zung self rating depression scale. Quality of life was more improved in the standardised mental component scale of the SF-36 with both active treatments than with placebo but in the physical component scale was improved only by hypericum extract compared with placebo. The rate of adverse events with hypericum extract was in the range of the placebo group but lower than that of the imipramine group (0.5, 0.6, and 1.2 events per patient respectively). CONCLUSIONS: At an average dose of 350 mg three times daily hypericum extract was more effective than placebo and at least as effective as 100 mg imipramine daily in the treatment of moderate depression. Treatment with hypericum extract is safe and improves quality of life. (+info)St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor. (4/207)
St. John's wort (Hypericum perforatum) is an herbal remedy used widely for the treatment of depression. Recent clinical studies demonstrate that hypericum extracts increase the metabolism of various drugs, including combined oral contraceptives, cyclosporin, and indinavir. In this report, we show that hyperforin, a constituent of St. John's wort with antidepressant activity, is a potent ligand (K(i) = 27 nM) for the pregnane X receptor, an orphan nuclear receptor that regulates expression of the cytochrome P450 (CYP) 3A4 monooxygenase. Treatment of primary human hepatocytes with hypericum extracts or hyperforin results in a marked induction of CYP3A4 expression. Because CYP3A4 is involved in the oxidative metabolism of >50% of all drugs, our findings provide a molecular mechanism for the interaction of St. John's wort with drugs and suggest that hypericum extracts are likely to interact with many more drugs than previously had been realized. (+info)Inhibition of human cytochrome P450 enzymes by constituents of St. John's Wort, an herbal preparation used in the treatment of depression. (5/207)
Commercially available St. John's wort (Hypericum perforatum) extracts, preparations that are used in the treatment of depression, were examined for the potential to inhibit human cytochrome P450 (CYP) enzyme activities, specifically CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Crude extracts demonstrated inhibition of each of these five enzymes, with CYP2D6, CYP2C9, and CYP3A4 being more sensitive than CYP1A2 and CYP2C19. Extracts were fractionated by HPLC, and each of the fractions was tested for inhibition of these five CYPs to identify individual constituents with inhibitory activity. Several fractions were shown to possess inhibitory activity, including the fractions containing hyperforin (the putative active antidepressant constituent), I3,II8-biapigenin, and hypericin. Hyperforin and I3,II8-biapigenin were isolated from the extract, and inhibition constants for the five CYP activities were measured. In addition, three other constituents, hypericin, quercetin, and chlorogenic acid, were tested for inhibitory activity toward the CYP enzymes. The flavonoid compound I3,II8-biapigenin was shown to be a potent, competitive inhibitor of CYP3A4, CYP2C9, and CYP1A2 activities with K(i) values of 0.038, 0.32, and 0.95 microM, respectively. Hyperforin was a potent noncompetitive inhibitor of CYP2D6 activity (K(i) = 1.5 microM) and competitive inhibitor of CYP2C9 and CYP3A4 activities (K(i) = 1.8 and 0.48 microM, respectively). Hypericin also demonstrated potent inhibition of several CYP activities. These in vitro data indicate that St. John's wort preparations contain constituents that can potently inhibit the activities of major human drug-metabolizing enzymes and suggest that these preparations should be examined for potential pharmacokinetic drug interactions in vivo. (+info)Inhibition of synaptosomal uptake of 3H-L-glutamate and 3H-GABA by hyperforin, a major constituent of St. John's Wort: the role of amiloride sensitive sodium conductive pathways. (6/207)
Extracts of St. John's Wort are widely used for the treatment of depressive disorders. The active principles have not yet been finally elucidated. We have recently shown that hyperforin, a major active constituent of St. John's Wort, not only inhibits the neuronal uptake of serotonin, norepinephrine and dopamine, but also that of L-glutamate and GABA. No other antidepressant compound exhibits a similar broad uptake inhibiting profile. To investigate this unique kind of property, kinetic analyses were performed regarding the uptake of 3H-L-glutamate and 3H-GABA into synaptosomal preparations of mouse brain. Michaelis-Menten kinetics revealed a reduction of Vmax (8.27 to 1.80 pmol/mg/min for 3H-L-glutamate, 2.76 to 0.77 pmol/mg/min for 3H-GABA) while Km was nearly unchanged in both cases, suggesting non-competitive inhibition. The unselective uptake inhibition by hyperforin could be mimicked by the Na+-ionophore monensin and by the Na+-K+-ATPase inhibitor ouabain. However, both mechanisms can be discarded for hyperforin. Several amiloride derivatives known to affect sodium conductance significantly enhance 3H-GABA and 3H-L-glutamate uptake and inhibit the uptake inhibition by hyperforin, while monensin or ouabain inhibition were not influenced. Selective concentrations of benzamil for amiloride sensitive Na+-channels and selective concentrations of 5'-ethylisopropylamiloride (EIPA) for the Na+-H+-exchangers both had an attenuating effect on the hyperforin inhibition of L-glutamate uptake, suggesting a possible role of amiloride sensitive Na+-channels and Na+-H+-exchangers in the mechanism of action of hyperforin. (+info)Comparison of St John's wort and imipramine for treating depression: randomised controlled trial. (7/207)
OBJECTIVES: To compare the efficacy and tolerability of Hypericum perforatum (St John's wort extract) with imipramine in patients with mild to moderate depression. DESIGN: Randomised, multicentre, double blind, parallel group trial. SETTING: 40 outpatient clinics in Germany. PARTICIPANTS: 324 outpatients with mild to moderate depression. INTERVENTION: 75 mg imipramine twice daily or 250 mg hypericum extract ZE 117 twice daily for 6 weeks. MAIN OUTCOME MEASURES: Hamilton depression rating scale, clinical global impression scale, and patient's global impression scale. RESULTS: Among the 157 participants taking hypericum mean scores on the Hamilton depression scale decreased from 22.4 at baseline to 12.00 at end point; among the 167 participants taking imipramine they fell from 22.1 to 12.75. Mean clinical global impression scores at end point were 2.22 out of 7 for the hypericum group and 2.42 for the imipramine group. On the 7 point self assessments of global improvement completed by participants (score of 1 indicating "very much improved" and 7 indicating "very much deteriorated") mean scores were 2.44 in the hypericum group and 2.60 in the imipramine group. None of the differences between treatment groups were significant. However, the mean score on the anxiety-somatisation subscale of the Hamilton scale (3.79 in the hypericum group and 4.26 in the imipramine group) indicated a significant advantage for hypericum relative to imipramine. Mean scores on the 5 point scale used by participants to assess tolerability (score of 1 indicating excellent tolerability and 5 indicating very poor tolerability) were better for hypericum (1.67) than imipramine (2.35). Adverse events occurred in 62/157 (39%) participants taking hypericum and in 105/167 (63%) taking imipramine. 4 (3%) participants taking hypericum withdrew because of adverse events compared with 26 (16%) taking imipramine. CONCLUSIONS: This Hypericum perforatum extract is therapeutically equivalent to imipramine in treating mild to moderate depression, but patients tolerate hypericum better. (+info)St John's wort, a herbal antidepressant, activates the steroid X receptor. (8/207)
St John's wort (SJW), an extract of the medicinal plant Hypericum perforatum, is widely used as a herbal antidepressant. Recently, this agent has been found to adversely affect the metabolism of various coadministered drugs. Steroid X receptor (SXR), an orphan nuclear receptor, induces hepatic cytochrome P450 gene expression in response to diverse endogenous steroids, xenobiotics and drugs. Here, we report that, when coexpressed with SXR, a reporter construct derived from the cytochrome P450 3A promoter is activated by St John's wort. A GAL4-SXR ligand binding domain (LBD) fusion mediates concentration-dependent transactivation by SJW, whereas a mutant GAL4-SXR fusion, containing substitutions in key residues in a transactivation domain, is inactive. SJW recruits steroid receptor coactivator-1 to SXR in a two-hybrid assay and competes with radiolabelled ligand in binding studies, suggesting it interacts directly with the receptor LBD. Of two constituents of SJW, we find that hyperforin, but not hypericin, mediates both transactivation and coactivator recruitment by SXR. Our observations suggest that SXR activation by St John's wort mediates its adverse interaction with drugs metabolised via the CYP 3A pathway. Future development of SJW derivatives lacking SXR activation, may enable its antidepressant and drug-metabolising properties to be dissociated. (+info)'Hypericum' is a genus of flowering plants, also known as St. John's Wort. While it is primarily used in herbal medicine and not considered a standard medical term, it is important to note that some species of Hypericum have been found to have medicinal properties. The most commonly studied and used species is Hypericum perforatum, which has been found to have potential benefits in treating depression, anxiety, and sleep disorders. However, its use as a medical treatment is still a subject of ongoing research and debate, and it can interact with several medications. Always consult with a healthcare provider before starting any new supplement or medication.
Perylene is not a medical term, but a chemical compound. It is an organic compound that is classified as a polycyclic aromatic hydrocarbon (PAH). PAHs are formed from the incomplete combustion of coal, oil, gas, wood, garbage, or other organic substances.
In medicine, perylene may be used in research and diagnostic settings to study cellular processes and diseases. For example, perylene derivatives have been used as fluorescent probes to investigate the structure and function of lipid membranes, DNA, and proteins. However, perylene itself is not a medical treatment or therapy.
Phloroglucinol is not strictly a medical term, but it is used in medicine and pharmacology. Phloroglucinol is an aromatic organic compound with the formula C6H6(OH)3. It is a white crystalline solid that is soluble in water and polar organic solvents.
In a medical context, phloroglucinol is most commonly used as a smooth muscle relaxant. It is often found in over-the-counter medications used to treat gastrointestinal symptoms such as abdominal cramps, spasms, and pain. Phloroglucinol works by relaxing the smooth muscles of the digestive tract, which can help to reduce spasms and relieve pain.
Phloroglucinol is also used in some countries as a treatment for kidney stones. It is believed to help to relax the ureter, the tube that connects the kidney to the bladder, making it easier to pass small kidney stones. However, its effectiveness for this use is not well established, and it is not approved by the U.S. Food and Drug Administration (FDA) for this purpose.
It's important to note that phloroglucinol should only be used under the guidance of a healthcare provider, as it can have side effects and interact with other medications.
A plant extract is a preparation containing chemical constituents that have been extracted from a plant using a solvent. The resulting extract may contain a single compound or a mixture of several compounds, depending on the extraction process and the specific plant material used. These extracts are often used in various industries including pharmaceuticals, nutraceuticals, cosmetics, and food and beverage, due to their potential therapeutic or beneficial properties. The composition of plant extracts can vary widely, and it is important to ensure their quality, safety, and efficacy before use in any application.
Phytotherapy is the use of extracts of natural origin, especially plants or plant parts, for therapeutic purposes. It is also known as herbal medicine and is a traditional practice in many cultures. The active compounds in these plant extracts are believed to have various medicinal properties, such as anti-inflammatory, analgesic, or sedative effects. Practitioners of phytotherapy may use the whole plant, dried parts, or concentrated extracts to prepare teas, capsules, tinctures, or ointments for therapeutic use. It is important to note that the effectiveness and safety of phytotherapy are not always supported by scientific evidence, and it should be used with caution and preferably under the guidance of a healthcare professional.
Bicyclic compounds are organic molecules that contain two rings in their structure, with at least two common atoms shared between the rings. These compounds can be found in various natural and synthetic substances, including some medications and bioactive molecules. The unique structure of bicyclic compounds can influence their chemical and physical properties, which may impact their biological activity or reactivity.
Medicinal plants are defined as those plants that contain naturally occurring chemical compounds which can be used for therapeutic purposes, either directly or indirectly. These plants have been used for centuries in various traditional systems of medicine, such as Ayurveda, Chinese medicine, and Native American medicine, to prevent or treat various health conditions.
Medicinal plants contain a wide variety of bioactive compounds, including alkaloids, flavonoids, tannins, terpenes, and saponins, among others. These compounds have been found to possess various pharmacological properties, such as anti-inflammatory, analgesic, antimicrobial, antioxidant, and anticancer activities.
Medicinal plants can be used in various forms, including whole plant material, extracts, essential oils, and isolated compounds. They can be administered through different routes, such as oral, topical, or respiratory, depending on the desired therapeutic effect.
It is important to note that while medicinal plants have been used safely and effectively for centuries, they should be used with caution and under the guidance of a healthcare professional. Some medicinal plants can interact with prescription medications or have adverse effects if used inappropriately.
The Balkan Peninsula, also known as the Balkans, is a geographical region located in southeastern Europe. It is surrounded by the Adriatic Sea to the west, the Ionian Sea to the southwest, the Aegean Sea to the south and the Black Sea to the east. The peninsula is made up of several countries including Albania, Bosnia and Herzegovina, Bulgaria, Croatia, Kosovo, Montenegro, North Macedonia, Serbia, Slovenia, and parts of Greece and Romania.
The Balkan Peninsula has a diverse landscape with mountain ranges, rivers, and coastlines. It is home to a variety of cultures, languages, and religions, making it a unique and complex region in Europe. The term "Balkanization" was coined based on the political fragmentation that occurred in this region during the 19th and 20th centuries.
"Theales" is not a medical term, but a taxonomic category in botany. It is an order of flowering plants that includes several families with economically important species, such as those yielding cork (Quercus suber), damask roses (Rosa damascena), and Brazil nuts (Bertholletia excelsa). Some Theales species also produce valuable timber, such as mahogany (Swietenia macrophylla) and teak (Tectona grandis).
The order Theales was established based on shared morphological characters, but recent molecular studies have challenged its monophyly (the idea that it forms a natural group with a single common ancestor). As a result, some families previously classified within Theales have been moved to other orders. Nonetheless, the term "Theales" remains in use as a formal taxonomic category in botany.
Terpenes are a large and diverse class of organic compounds produced by a variety of plants, including cannabis. They are responsible for the distinctive aromas and flavors found in different strains of cannabis. Terpenes have been found to have various therapeutic benefits, such as anti-inflammatory, analgesic, and antimicrobial properties. Some terpenes may also enhance the psychoactive effects of THC, the main psychoactive compound in cannabis. It's important to note that more research is needed to fully understand the potential medical benefits and risks associated with terpenes.
Herb-drug interactions (HDIs) refer to the pharmacological or clinical consequences that occur when a patient takes a herbal product concurrently with a prescribed medication. These interactions can result in various outcomes, such as decreased, increased, or altered drug effects due to changes in the absorption, distribution, metabolism, or excretion of the drug.
Herbs may contain various bioactive compounds that can interact with drugs and affect their pharmacokinetics or pharmacodynamics. For example, some herbs may induce or inhibit drug-metabolizing enzymes, such as cytochrome P450 (CYP) isoenzymes, leading to altered drug metabolism and potentially increased or decreased drug concentrations in the body.
Similarly, herbs can also affect drug transporters, such as P-glycoprotein, which can further alter drug absorption, distribution, and excretion. Moreover, some herbs may have pharmacodynamic interactions with drugs, leading to additive or synergistic effects, or antagonism of the drug's therapeutic action.
Therefore, healthcare providers should be aware of potential HDIs when prescribing medications to patients who use herbal products and consider monitoring their patients' medication responses closely. Patients should also be advised to inform their healthcare providers about any herbal products they are taking, including dosage and frequency of use.
Chlorogenic acid is a type of polyphenolic compound that is found in various plants, including coffee, tea, and several fruits and vegetables. It is a ester of cinnamic acid and quinic acid. Chlorogenic acids are known to have antioxidant properties and may also play a role in regulating glucose metabolism and inhibiting the growth of certain types of cancer cells. However, more research is needed to fully understand the potential health benefits and risks associated with chlorogenic acid consumption.
"Plant preparations" is not a term with a specific medical definition in the field of medicine or pharmacology. However, it is commonly used to refer to various forms of plant material that have been prepared for medicinal use. This can include dried and powdered plant parts, such as leaves, roots, or flowers, as well as extracts or concentrates made from plants. These preparations may be used in traditional medicine or as the basis for modern pharmaceuticals. It is important to note that the safety, effectiveness, and quality of plant preparations can vary widely, and they should only be used under the guidance of a qualified healthcare provider.
Quercetin is a type of flavonoid antioxidant that is found in plant foods, including leafy greens, tomatoes, berries, and broccoli. It has been studied for its potential health benefits, such as reducing inflammation, protecting against damage to cells, and helping to reduce the risk of heart disease and cancer. Quercetin is also known for its ability to stabilize mast cells and prevent the release of histamine, making it a popular natural remedy for allergies. It is available in supplement form, but it is always recommended to consult with a healthcare provider before starting any new supplement regimen.
Xanthones are a type of chemical compound that are found in various plants and fruits. They have a variety of potential health benefits, including anti-inflammatory, antioxidant, and anticancer properties. Some research suggests that xanthones may help to protect against chronic diseases such as heart disease and cancer, but more studies are needed to confirm these effects. Xanthones can be found in small amounts in a variety of foods, including mangosteen fruit, blackberries, and turmeric. They are also available in supplement form.
Imipramine is a tricyclic antidepressant (TCA) medication that is primarily used to treat depression. It works by increasing the levels of certain neurotransmitters, such as serotonin and norepinephrine, in the brain. Imipramine has been found to be effective in treating various types of depression, including major depressive disorder, dysthymia, and depression that is resistant to other treatments.
In addition to its antidepressant effects, imipramine is also used off-label for the treatment of several other conditions, such as anxiety disorders, attention deficit hyperactivity disorder (ADHD), enuresis (bedwetting), and chronic pain.
Imipramine was first synthesized in the 1950s and has been widely used since then. It is available in various forms, including immediate-release tablets, extended-release capsules, and liquid solutions. As with all medications, imipramine can have side effects, which may include dry mouth, blurred vision, constipation, dizziness, and sedation. In rare cases, it can cause more serious side effects, such as cardiac arrhythmias or seizures.
It is important to use imipramine under the close supervision of a healthcare provider, as dosages may need to be adjusted based on individual patient needs and responses to treatment. Additionally, imipramine should not be stopped abruptly, as doing so can lead to withdrawal symptoms or a recurrence of depression.