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Rottlerin
Rottlerin (mallotoxin) is a polyphenol natural product isolated from the Asian tree ''Mallotus philippensis''. Rottlerin displays a complex spectrum of pharmacology. Effects Uncoupler of oxidative phosphorylation Rottlerin has been shown to be an uncoupler of mitochondrial oxidative phosphorylation. Potassium channel opener Rottlerin is a potent large conductance potassium channel (BKCa++) opener.Clements RT, Cordeiro B, Feng J, Bianchi C, Sellke FW. "Rottlerin increases cardiac contractile performance and coronary perfusion through BKCa++ channel activation after cold cardioplegic arrest in isolated hearts. ''Circulation'' 2011 Sep 13; 124(11 Suppl):S55-61 BKCa++ is found in the inner mitochondrial membrane of cardiomyocytes.Zakharov SI, Morrow JP, Liu G, Yang L, Marx SO. Activation of the BK (SLO1) potassium channel by mallotoxin" ''J Biol Chem'' 2005;280: 30882–30887 Opening these channels is beneficial for post-ischemic changes in vasodilation. Other BKCa++ chann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kamala Tree
''Mallotus philippensis'' is a plant in the spurge family. It is known as the kamala tree or red kamala or kumkum tree, due to the fruit covering, which produces a red dye. However, it must be distinguished from kamala meaning "lotus" in many Indian languages, an unrelated plant, flower, and sometimes metonymic spiritual or artistic concept. ''Mallotus philippensis'' has many other local names. This kamala often appears in rainforest margins. Or in disturbed areas free from fire, in moderate to high rainfall areas. It occurs in South Asia, Southeast Asia, as well as Afghanistan and Australia. The southernmost limit of natural distribution is Mount Keira, south of Sydney. The species name refers to the type specimen being collected in the Philippines, where it is known as ''banato''. Description A bush to small or medium-sized tree, up to 25 metres tall and a trunk diameter of 40 cm. The trunk is fluted and irregular at the base. The grey bark is smooth, or with occasio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mallotus Philippensis
''Mallotus philippensis'' is a plant in the spurge family. It is known as the kamala tree or red kamala or kumkum tree, due to the fruit covering, which produces a red dye. However, it must be distinguished from kamala meaning "lotus" in many Indian languages, an unrelated plant, flower, and sometimes metonymic spiritual or artistic concept. ''Mallotus philippensis'' has many other local names. This kamala often appears in rainforest margins. Or in disturbed areas free from fire, in moderate to high rainfall areas. It occurs in South Asia, Southeast Asia, as well as Afghanistan and Australia. The southernmost limit of natural distribution is Mount Keira, south of Sydney. The species name refers to the type specimen being collected in the Philippines, where it is known as ''banato''. Description A bush to small or medium-sized tree, up to 25 metres tall and a trunk diameter of 40 cm. The trunk is fluted and irregular at the base. The grey bark is smooth, or with occasio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Polyphenol
Polyphenols () are a large family of naturally occurring organic compounds characterized by multiples of phenol units. They are abundant in plants and structurally diverse. Polyphenols include flavonoids, tannic acid, and ellagitannin, some of which have been used historically as dyes and for tanning garments. Etymology The name derives from the Ancient Greek word (''polus'', meaning "many, much") and the word phenol which refers to a chemical structure formed by attaching to an aromatic benzenoid (phenyl) ring to a hydroxyl (-OH) group as is found in alcohols (hence the ''-ol'' suffix). The term polyphenol has been in use at least since 1894. Definition The term polyphenol is not well-defined, but is generally agreed that they are natural products "having a polyphenol structure (i.e., several hydroxyl groups on aromatic rings)" including four principal classes: "phenolic acids, flavonoids, stilbenes, and lignans". *Flavonoids include flavones, flavonols, flavanols, f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mitochondrial
A mitochondrion (; ) is an organelle found in the cells of most Eukaryotes, such as animals, plants and fungi. Mitochondria have a double membrane structure and use aerobic respiration to generate adenosine triphosphate (ATP), which is used throughout the cell as a source of chemical energy. They were discovered by Albert von Kölliker in 1857 in the voluntary muscles of insects. The term ''mitochondrion'' was coined by Carl Benda in 1898. The mitochondrion is popularly nicknamed the "powerhouse of the cell", a phrase coined by Philip Siekevitz in a 1957 article of the same name. Some cells in some multicellular organisms lack mitochondria (for example, mature mammalian red blood cells). A large number of unicellular organisms, such as microsporidia, parabasalids and diplomonads, have reduced or transformed their mitochondria into other structures. One eukaryote, ''Monocercomonoides'', is known to have completely lost its mitochondria, and one multicellular organism, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxidative Phosphorylation
Oxidative phosphorylation (UK , US ) or electron transport-linked phosphorylation or terminal oxidation is the metabolic pathway in which cells use enzymes to oxidize nutrients, thereby releasing chemical energy in order to produce adenosine triphosphate (ATP). In eukaryotes, this takes place inside mitochondria. Almost all aerobic organisms carry out oxidative phosphorylation. This pathway is so pervasive because it releases more energy than alternative fermentation processes such as anaerobic glycolysis. The energy stored in the chemical bonds of glucose is released by the cell in the citric acid cycle producing carbon dioxide, and the energetic electron donors NADH and FADH. Oxidative phosphorylation uses these molecules and O2 to produce ATP, which is used throughout the cell whenever energy is needed. During oxidative phosphorylation, electrons are transferred from the electron donors to a series of electron acceptors in a series of redox reactions ending in oxygen, who ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potassium Channel Opener
A potassium channel opener is a type of drug which facilitates ion transmission through potassium channels. Examples Some examples include: *Diazoxide vasodilator used for hypertension, smooth muscle relaxing activity *Minoxidil vasodilator used for hypertension, also used to treat hair loss *Nicorandil vasodilator used to treat angina *Pinacidil *Retigabine, an anticonvulsant * Flupirtine, analgesic with muscle relaxant and anticonvulsant properties See also * Potassium channel blocker Potassium channel blockers are agents which interfere with conduction through potassium channels. Medical uses Arrhythmia Potassium channel blockers used in the treatment of cardiac arrhythmia are classified as class III antiarrhythmic age ... References {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cardiac Muscle Cell
Cardiac muscle (also called heart muscle, myocardium, cardiomyocytes and cardiac myocytes) is one of three types of vertebrate muscle tissues, with the other two being skeletal muscle and smooth muscle. It is an involuntary, striated muscle that constitutes the main tissue of the wall of the heart. The cardiac muscle (myocardium) forms a thick middle layer between the outer layer of the heart wall (the pericardium) and the inner layer (the endocardium), with blood supplied via the coronary circulation. It is composed of individual cardiac muscle cells joined by intercalated discs, and encased by collagen fibers and other substances that form the extracellular matrix. Cardiac muscle contracts in a similar manner to skeletal muscle, although with some important differences. Electrical stimulation in the form of a cardiac action potential triggers the release of calcium from the cell's internal calcium store, the sarcoplasmic reticulum. The rise in calcium causes the cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
The Journal Of Pharmacology And Experimental Therapeutics
The ''Journal of Pharmacology and Experimental Therapeutics'' (a.k.a. JPET) is a peer-reviewed scientific journal covering pharmacology. It has been published since 1909 by the American Society for Pharmacology and Experimental Therapeutics (ASPET). The journal publishes mainly original research Research is "creativity, creative and systematic work undertaken to increase the stock of knowledge". It involves the collection, organization and analysis of evidence to increase understanding of a topic, characterized by a particular att ... articles, and accepts papers covering all aspects of the interactions of chemicals with biological systems. John Jacob Abel founded ASPET in December 1908 when he invited 18 pharmacologists to his laboratory in order to organize a new society. At the end of the meeting Abel announced the establishment of JPET. According to the '' Journal Citation Reports'', the journal received a 2021 impact factor of 4.4. Further reading [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PKCδ
Protein kinase C delta type (or PKC-δ) is an enzyme that in humans is encoded by the ''PRKCD'' gene. Function Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by the second messenger diacylglycerol. PKC family members phosphorylate a wide variety of protein targets and are known to be involved in diverse cellular signaling pathways. PKC family members also serve as major receptors for phorbol esters, a class of tumor promoters. Each member of the PKC family has a specific expression profile and is believed to play distinct roles in cells. The protein encoded by this gene is one of the PKC family members. Studies both in human and mice demonstrate that this kinase is involved in B cell signaling and in the regulation of growth, apoptosis, and differentiation of a variety of cell types. Protein kinase C delta is also regulated by phosphorylation on various serine/threonine (e.g. T50, T141, S304, T451, T505, S506, T507, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phloroglucinols
Phloroglucinol is an organic compound with the formula C6H3(OH)3. It is a colorless solid. It is used in the synthesis of pharmaceuticals and explosives. Phloroglucinol is one of three isomeric benzenetriols. The other two isomers are hydroxyquinol (1,2,4-benzenetriol) and pyrogallol (1,2,3-benzenetriol). Phloroglucinol, and its benzenetriol isomers, are still defined as "phenols" according to the IUPAC official nomenclature rules of chemical compounds. Many such monophenolics are often termed "polyphenols" by the cosmetic and parapharmaceutical industries, which does not match the scientifically accepted definition. Synthesis and occurrence In 1855, phloroglucinol was first prepared from phloretin by the Austrian chemist Heinrich Hlasiwetz (1825–1875). A modern synthesis of involves hydrolysis of benzene-1,3,5-triamine and its derivatives. Representative is the following route from trinitrobenzene. : The synthesis is noteworthy because ordinary aniline derivatives are unreac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HERG Activator
hERG (the human '' Ether-à-go-go''-Related Gene) is a gene () that codes for a protein known as Kv11.1, the alpha subunit of a potassium ion channel. This ion channel (sometimes simply denoted as 'hERG') is best known for its contribution to the electrical activity of the heart: the hERG channel mediates the repolarizing ''I''Kr current in the cardiac action potential, which helps coordinate the heart's beating. When this channel's ability to conduct electrical current across the cell membrane is inhibited or compromised, either by application of drugs or by rare mutations in some families, it can result in a potentially fatal disorder called long QT syndrome. Conversely, genetic mutations that increase the current through these channels can lead to the related inherited heart rhythm disorder Short QT syndrome. A number of clinically successful drugs in the market have had the tendency to inhibit hERG, lengthening the QT and potentially leading to a fatal irregularity of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potassium Channel Openers
A potassium channel opener is a type of drug which facilitates ion transmission through potassium channels. Examples Some examples include: *Diazoxide vasodilator used for hypertension, smooth muscle relaxing activity *Minoxidil vasodilator used for hypertension, also used to treat hair loss *Nicorandil vasodilator used to treat angina *Pinacidil *Retigabine, an anticonvulsant * Flupirtine, analgesic with muscle relaxant and anticonvulsant properties See also * Potassium channel blocker Potassium channel blockers are agents which interfere with conduction through potassium channels. Medical uses Arrhythmia Potassium channel blockers used in the treatment of cardiac arrhythmia are classified as class III antiarrhythmic age ... References {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
