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Parthenolide
Parthenolide is a sesquiterpene lactone of the germacranolide class which occurs naturally in the plant feverfew (''Tanacetum parthenium''), after which it is named, and in the closely related tansy (''Tanacetum vulgare''). It is found in highest concentration in the flowers and fruit. Parthenolide's molecular structure depiction is often incorrect regarding the stereochemistry of the epoxide, although X-ray single crystal structures are available. Lack of solubility in water and bioavailability limits the potential of parthenolide as a drug. ''In vitro'' research Parthenolide has a variety of reported ''in vitro'' biological activities, including: *Inhibition of HDAC1 protein without affecting other class I/II HDACs, which leads to sustained DNA damage response in certain cells (required for apoptosis). *Modulation of the NF-κB-mediated inflammatory responses in experimental atherosclerosis. *Inducing apoptosis in acute myelogenous leukemia (AML) cells, leaving normal bone marr ...
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Tanacetum Parthenium
''Tanacetum parthenium'', known as feverfew, is a flowering plant in the daisy family, Asteraceae. It may be grown as an ornament, and may be identified by its synonyms, ''Chrysanthemum parthenium'' and ''Pyrethrum parthenium''. Description The plant is a herbaceous perennial that grows into a small bush, up to high, with pungently-scented leaves. The leaves are light yellowish green, variously pinnatifid. The conspicuous daisy-like flowers are up to across, borne in lax corymbs. The outer, ray florets have white ligules and the inner, disc florets are yellow and tubular. It spreads rapidly by seed, and will cover a wide area after a few years. Distribution and cultivation Feverfew is native to Eurasia, specifically the Balkan Peninsula, Anatolia, and the Caucasus, but cultivation has spread it around the world and the rest of Europe, North America, and Chile. A perennial herb, it should be planted in full sun, apart, and cut back to the ground in the autumn. It grows u ...
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Sesquiterpene Lactone
Sesquiterpene lactones (SLs) are a class of sesquiterpenoids that contain a lactone ring. They are most often found in plants of the family Asteraceae (daisies, asters). Other plant families with SLs are Umbelliferae (celery, parsley, carrots) and Magnoliaceae (magnolias). A collection of colorless, lipophilic solids, SLs are a rich source of drugs. They can be allergenic and toxic in grazing livestock causing severe neurological problems in horses. Some are also found in corals such as '' Maasella edwardsi''. Types Sesquiterpene lactones can be divided into several main classes including germacranolides, heliangolides, guaianolides, pseudoguaianolides, hypocretenolides, and eudesmanolides. Examples Artemisinin, a new, highly-effective anti-malarial compound, is a sesquiterpene lactone found in ''Artemisia annua''. Lactucin, desoxylactucin, lactucopicrin, lactucin-15-oxalate, lactucopicrin-15-oxalate are some of the most prominent found in lettuce and spinach, giving ...
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Acute Myelogenous Leukemia
Acute myeloid leukemia (AML) is a cancer of the myeloid line of blood cells, characterized by the rapid growth of abnormal cells that build up in the bone marrow and blood and interfere with normal blood cell production. Symptoms may include feeling tired, shortness of breath, easy bruising and bleeding, and increased risk of infection. Occasionally, spread may occur to the brain, skin, or gums. As an acute leukemia, AML progresses rapidly, and is typically fatal within weeks or months if left untreated. Risk factors include smoking, previous chemotherapy or radiation therapy, myelodysplastic syndrome, and exposure to the chemical benzene. The underlying mechanism involves replacement of normal bone marrow with leukemia cells, which results in a drop in red blood cells, platelets, and normal white blood cells. Diagnosis is generally based on bone marrow aspiration and specific blood tests. AML has several subtypes for which treatments and outcomes may vary. The first-l ...
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Epoxides
In organic chemistry, an epoxide is a cyclic ether () with a three-atom ring. This ring approximates an equilateral triangle, which makes it strained, and hence highly reactive, more so than other ethers. They are produced on a large scale for many applications. In general, low molecular weight epoxides are colourless and nonpolar, and often volatile. Nomenclature A compound containing the epoxide functional group can be called an epoxy, epoxide, oxirane, and ethoxyline. Simple epoxides are often referred to as oxides. Thus, the epoxide of ethylene (C2H4) is ethylene oxide (C2H4O). Many compounds have trivial names; for instance, ethylene oxide is called "oxirane". Some names emphasize the presence of the epoxide functional group, as in the compound ''1,2-epoxyheptane'', which can also be called ''1,2-heptene oxide''. A polymer formed from epoxide precursors is called an ''epoxy'', but such materials do not contain epoxide groups (or contain only a few residual epoxy grou ...
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Adiponectin Receptor Agonists
Adiponectin (also referred to as GBP-28, apM1, AdipoQ and Acrp30) is a protein hormone and adipokine, which is involved in regulating glucose levels as well as fatty acid breakdown. In humans it is encoded by the ''ADIPOQ'' gene and it is produced in primarily in adipose tissue, but also in muscle, and even in the brain. Structure Adiponectin is a 244-amino-acid-long polypeptide (protein). There are four distinct regions of adiponectin. The first is a short signal sequence that targets the hormone for secretion outside the cell; next is a short region that varies between species; the third is a 65-amino acid region with similarity to collagenous proteins; the last is a globular domain. Overall this protein shows similarity to the complement 1Q factors (C1Q). However, when the 3-dimensional structure of the globular region was determined, a striking similarity to TNFα was observed, despite unrelated protein sequences. Function Adiponectin is a protein hormone that modulates ...
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Adiponectin Receptor 2
Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ''ADIPOR2'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR2. Structure Similar to G protein-coupled receptors (GPCRs), AdipoR2 also possesses 7 transmembrane domains. However, AdipoR2 is orientated oppositely to GPCRs in the membrane (i.e., cytoplasmic N-terminus, extracellular C-terminus) and does not associate with G proteins. Function The adiponectin receptors, AdipoR1 and AdipoR2, serve as receptors for globular and full-length adiponectin and mediate increased AMPK and PPAR-α ligand activities, as well as fatty acid oxidation and glucose uptake by adiponectin. In 2016, the University of Tokyo announced that it would launch an investigation into claims of fabrication of AdipoR1 and AdipoR2 identification data, as accused by an anonymous person/group called Ordinary_researchers.
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Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive


Types of agonists

can be activated by either endogenous agonists (such as

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Microtubule
Microtubules are polymers of tubulin that form part of the cytoskeleton and provide structure and shape to eukaryotic cells. Microtubules can be as long as 50 micrometres, as wide as 23 to 27  nm and have an inner diameter between 11 and 15 nm. They are formed by the polymerization of a dimer of two globular proteins, alpha and beta tubulin into protofilaments that can then associate laterally to form a hollow tube, the microtubule. The most common form of a microtubule consists of 13 protofilaments in the tubular arrangement. Microtubules play an important role in a number of cellular processes. They are involved in maintaining the structure of the cell and, together with microfilaments and intermediate filaments, they form the cytoskeleton. They also make up the internal structure of cilia and flagella. They provide platforms for intracellular transport and are involved in a variety of cellular processes, including the movement of secretory vesicles, organell ...
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Leishmania Amazonensis
''Leishmania amazonensis'' is a parasite responsible for the disease leishmaniasis. This species has been known to spread by using sandflies Sandfly (or sand fly) is a colloquial name for any species or genus of flying, biting, blood-sucking dipteran (fly) encountered in sandy areas. In the United States, ''sandfly'' may refer to certain horse flies that are also known as "greenhe ... as its vector and a vertebrate as its primary host, just like other species of Leishmania. They have also been known to spread throughout the Brazilian Amazon region due to their ecological niches needed for survival and reproduction. However, when the host is infected, the Leishmania can cause 3 different forms of Leishmaniasis. For this species, it has been known to cause cutaneous leishmaniasis and mucocutaneous leishmaniasis. Cutaneous leishmaniasis is commonly characterized with skin lesions, which can appear localized, or throughout the body. While mucocutaneous leishmaniasis is charact ...
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Stem Cell
In multicellular organisms, stem cells are undifferentiated or partially differentiated cells that can differentiate into various types of cells and proliferate indefinitely to produce more of the same stem cell. They are the earliest type of cell in a cell lineage. They are found in both embryonic and adult organisms, but they have slightly different properties in each. They are usually distinguished from progenitor cells, which cannot divide indefinitely, and precursor or blast cells, which are usually committed to differentiating into one cell type. In mammals, roughly 50–150 cells make up the inner cell mass during the blastocyst stage of embryonic development, around days 5–14. These have stem-cell capability. ''In vivo'', they eventually differentiate into all of the body's cell types (making them pluripotent). This process starts with the differentiation into the three germ layers – the ectoderm, mesoderm and endoderm – at the gastrulation stage. However ...
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NF-κB
Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) is a protein complex that controls transcription of DNA, cytokine production and cell survival. NF-κB is found in almost all animal cell types and is involved in cellular responses to stimuli such as stress, cytokines, free radicals, heavy metals, ultraviolet irradiation, oxidized LDL, and bacterial or viral antigens. NF-κB plays a key role in regulating the immune response to infection. Incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development. NF-κB has also been implicated in processes of synaptic plasticity and memory. Discovery NF-κB was discovered by Ranjan Sen in the lab of Nobel laureate David Baltimore via its interaction with an 11-base pair sequence in the immunoglobulin light-chain enhancer in B cells. Later work by Alexander Poltorak and Bruno Lemaitre in mice and ''Drosophila'' frui ...
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Germacranolide
Germacranolides are a group of natural chemical compounds classified as sesquiterpene lactone Sesquiterpene lactones (SLs) are a class of sesquiterpenoids that contain a lactone ring. They are most often found in plants of the family Asteraceae (daisies, asters). Other plant families with SLs are Umbelliferae (celery, parsley, carrots) ...s. They are found in a variety of plant sources. References Sesquiterpene lactones Oxygen heterocycles {{organic-chemistry-stub ...
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