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Baicalin
As baicalin is a flavone glycoside, it is a flavonoid. It is the glucuronide of baicalein. Natural occurrences Baicalin is found in several species in the genus ''Scutellaria'', including ''Scutellaria baicalensis'', and '' Scutellaria lateriflora''. There are 10 mg/g baicalin in '' Scutellaria galericulata'' leaves.P.H. and Horhammer, L., Hager's Handbuch der Pharmazeutischen Praxis, Vols. 2-6, Springer-Verlag, Berlin, 1969-1979 It is also present in the bark isolate of the '' Oroxylum indicum'' tree. Medical uses Baicalin is one of the chemical ingredients of at least two herbal supplements: Shuanghuanglian and Sho-Saiko-To, which is a Chinese classic herbal formula, and listed in Japan as Kampo medicine. Baicalin, along with its aglycone baicalein, is a positive allosteric modulator of the benzodiazepine site and/or a non-benzodiazepine site of the GABAA receptor. In mice, baicalin produces anxiolytic effects without sedative or myorelaxant A muscle relaxant ...
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Prolyl Endopeptidase
Prolyl endopeptidase (PE) also known as prolyl oligopeptidase or post-proline cleaving enzyme is an enzyme that in humans is encoded by the ''PREP'' gene. Function Prolyl endopeptidase is a large cytosolic enzyme that belongs to a distinct class of serine peptidases. It was first described in the cytosol of rabbit brain as an oligopeptidase, which degrades the nonapeptide bradykinin at the Pro-Phe bond. The enzyme is involved in the maturation and degradation of peptide hormones and neuropeptides such as alpha-melanocyte-stimulating hormone, luteinizing hormone-releasing hormone (LH-RH), thyrotropin-releasing hormone, angiotensin, neurotensin, oxytocin, substance P and vasopressin. PREP cleaves peptide bonds at the C-terminal side of proline residues. Its activity is confined to action on oligopeptides of less than 10 kD and it has an absolute requirement for the trans-configuration of the peptide bond preceding proline. Prolyl endopeptidases are involved in the maturation ...
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Baicalein
Baicalein (5,6,7-trihydroxyflavone) is a flavone, a type of flavonoid, originally isolated from the roots of '' Scutellaria baicalensis'' and '' Scutellaria lateriflora''. It is also reported in '' Oroxylum indicum'' (Indian trumpetflower) and ''Thyme''. It is the aglycone of baicalin. Baicalein is one of the active ingredients of Sho-Saiko-To, which is a Chinese classic herbal formula, and listed in Japan as Kampo medicine. As a Chinese herbal supplement, it is believed to enhance liver health. Baicalein, along with its analogue baicalin, is a positive allosteric modulator of the benzodiazepine site and/or a non-benzodiazepine site of the GABAA receptor. It displays subtype selectivity for α2 and α3 subunit-containing GABAA receptors. In accordance, baicalein shows anxiolytic effects in mice without incidence of sedation or myorelaxation. It is thought that baicalein, along with other flavonoids, may underlie the anxiolytic effects of ''S. baicalensis'' and ''S. late ...
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Benzodiazepine Site
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV). ...
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Baicalein
Baicalein (5,6,7-trihydroxyflavone) is a flavone, a type of flavonoid, originally isolated from the roots of '' Scutellaria baicalensis'' and '' Scutellaria lateriflora''. It is also reported in '' Oroxylum indicum'' (Indian trumpetflower) and ''Thyme''. It is the aglycone of baicalin. Baicalein is one of the active ingredients of Sho-Saiko-To, which is a Chinese classic herbal formula, and listed in Japan as Kampo medicine. As a Chinese herbal supplement, it is believed to enhance liver health. Baicalein, along with its analogue baicalin, is a positive allosteric modulator of the benzodiazepine site and/or a non-benzodiazepine site of the GABAA receptor. It displays subtype selectivity for α2 and α3 subunit-containing GABAA receptors. In accordance, baicalein shows anxiolytic effects in mice without incidence of sedation or myorelaxation. It is thought that baicalein, along with other flavonoids, may underlie the anxiolytic effects of ''S. baicalensis'' and ''S. late ...
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Bark Isolate
Bark isolates are chemicals which have been extracted from bark. Prominent medical examples are salicylic acid (active metabolite of aspirin) and paclitaxel Paclitaxel (PTX), sold under the brand name Taxol among others, is a chemotherapy medication used to treat a number of types of cancer. This includes ovarian cancer, esophageal cancer, breast cancer, lung cancer, Kaposi's sarcoma, cervical ca ... (Taxol). The pharmacology of bark isolates is an ongoing topic of medical research. See also Notes {{Reflist Trees Pharmaceutical isolates ...
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Shuanghuanglian
''Shuanghuanglian'' (Chinese: 双黄连) is a traditional Chinese medicine with a long history for treating respiratory tract infection in China. Some of its active ingredients are Wogonin, Baicalin and baicalein. It is derived from three Chinese herbal medicines, namely, '' Lonicera japonica Thunb.'', '' Scutellaria baicalensis Georgi'', and '' Forsythia suspense (Thunb.) Vahl''. It has been used for the treatment of acute respiratory tract infections since 1973. It is mentioned in the '' Chinese Pharmacopoeia''. The substance has been shown ''in vitro'' to be cytotoxic "against a clinical isolate of SARS-CoV-2". History In July 2020, Su et al reported on an ''in vitro'' experiment of its effect on COVID-19 Coronavirus disease 2019 (COVID-19) is a contagious disease caused by a virus, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The first known case was identified in Wuhan, China, in December 2019. The disease quickly .... Following the releas ...
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GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV ...
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Flavonoid Glucuronides
Flavonoids (or bioflavonoids; from the Latin word ''flavus'', meaning yellow, their color in nature) are a class of polyphenolic secondary metabolites found in plants, and thus commonly consumed in the diets of humans. Chemically, flavonoids have the general structure of a 15-carbon skeleton, which consists of two phenyl rings (A and B) and a heterocyclic ring (C, the ring containing the embedded oxygen). This carbon structure can be abbreviated C6-C3-C6. According to the IUPAC nomenclature, they can be classified into: *flavonoids or bioflavonoids *isoflavonoids, derived from 3-phenyl chromen-4-one (3-phenyl-1,4-benzopyrone) structure *neoflavonoids, derived from 4-phenylcoumarine (4-phenyl-1,2-benzopyrone) structure The three flavonoid classes above are all ketone-containing compounds and as such, anthoxanthins ( flavones and flavonols). This class was the first to be termed bioflavonoids. The terms flavonoid and bioflavonoid have also been more loosely used to describe non ...
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Flavone Glycosides
Flavone is an organic compound with the formula . A white solid, flavone is a derivative of chromone with a phenyl (Ph) substituent adjacent to the ether group. The compound is of little direct practical importance, but susbstituted derivatives, the flavones and flavonoids are a large class of nutritionally important natural products. Flavone can be prepared in the laboratory by cyclization of 2-hydroxacetophenone. Isomeric with flavone is isoflavone Isoflavones are substituted derivatives of isoflavone, a type of naturally occurring isoflavonoids, many of which act as phytoestrogens in mammals. Isoflavones are produced almost exclusively by the members of the bean family, Fabaceae (Leguminosae) ..., where the phenyl group is adjacent to the ketone. References {{Flavones ...
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Anxiolytics
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are a ...
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Pancreatic Cancer
Pancreatic cancer arises when cells in the pancreas, a glandular organ behind the stomach, begin to multiply out of control and form a mass. These cancerous cells have the ability to invade other parts of the body. A number of types of pancreatic cancer are known. The most common, pancreatic adenocarcinoma, accounts for about 90% of cases, and the term "pancreatic cancer" is sometimes used to refer only to that type. These adenocarcinomas start within the part of the pancreas that makes digestive enzymes. Several other types of cancer, which collectively represent the majority of the non-adenocarcinomas, can also arise from these cells. About 1–2% of cases of pancreatic cancer are neuroendocrine tumors, which arise from the hormone-producing cells of the pancreas. These are generally less aggressive than pancreatic adenocarcinoma. Signs and symptoms of the most-common form of pancreatic cancer may include yellow skin, abdominal or back pain, unexplained weight loss, ...
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Apoptosis
Apoptosis (from grc, ἀπόπτωσις, apóptōsis, 'falling off') is a form of programmed cell death that occurs in multicellular organisms. Biochemical events lead to characteristic cell changes ( morphology) and death. These changes include blebbing, cell shrinkage, nuclear fragmentation, chromatin condensation, DNA fragmentation, and mRNA decay. The average adult human loses between 50 and 70 billion cells each day due to apoptosis. For an average human child between eight and fourteen years old, approximately twenty to thirty billion cells die per day. In contrast to necrosis, which is a form of traumatic cell death that results from acute cellular injury, apoptosis is a highly regulated and controlled process that confers advantages during an organism's life cycle. For example, the separation of fingers and toes in a developing human embryo occurs because cells between the digits undergo apoptosis. Unlike necrosis, apoptosis produces cell fragments called apop ...
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