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Fungal Isolates
Fungal isolates have been researched for decades. Because fungi often exist in thin mycelial monolayers, with no protective shell, immune system, and limited mobility, they have developed the ability to synthesize a variety of unusual compounds for survival. Researchers have discovered fungal isolates with anticancer, antimicrobial, immunomodulatory, and other bio-active properties. The first statins, β-Lactam antibiotics, as well as a few important antifungals, were discovered in fungi. Chemotherapeutic isolates BMS manufactures paclitaxel using ''Penicillium'' and plant cell fermentation. Fungi can synthesize podophyllotoxin and camptothecin, precursors to etoposide, teniposide, topotecan, and irinotecan. Lentinan, PSK, and PSP, are registered anticancer immunologic adjuvants. Irofulven and acylfulvene are anticancer derivatives of illudin S. Clavaric acid is a reversible farnesyltransferase inhibitor. ''Inonotus obliquus'' creates betulinic acid precursor betulin. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fungus
A fungus ( : fungi or funguses) is any member of the group of eukaryotic organisms that includes microorganisms such as yeasts and molds, as well as the more familiar mushrooms. These organisms are classified as a kingdom, separately from the other eukaryotic kingdoms, which by one traditional classification include Plantae, Animalia, Protozoa, and Chromista. A characteristic that places fungi in a different kingdom from plants, bacteria, and some protists is chitin in their cell walls. Fungi, like animals, are heterotrophs; they acquire their food by absorbing dissolved molecules, typically by secreting digestive enzymes into their environment. Fungi do not photosynthesize. Growth is their means of mobility, except for spores (a few of which are flagellated), which may travel through the air or water. Fungi are the principal decomposers in ecological systems. These and other differences place fungi in a single group of related organisms, named the ''Eumycota'' (''true f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Irinotecan
Irinotecan, sold under the brand name Camptosar among others, is a medication used to treat colon cancer, and small cell lung cancer. For colon cancer it is used either alone or with fluorouracil. For small cell lung cancer it is used with cisplatin. It is given intravenously. Common side effects include diarrhea, vomiting, bone marrow suppression, hair loss, shortness of breath, and fever. Other severe side effects include blood clots, colon inflammation, and allergic reactions. Those with two copies of the UGT1A1*28 gene variant are at higher risk for side effects. Use during pregnancy can result in harm to the baby. Irinotecan is a topoisomerase inhibitor—it blocks the topoisomerase I enzyme, resulting in DNA damage and cell death. Irinotecan was approved for medical use in the United States in 1996. It is on the World Health Organization's List of Essential Medicines. It is made from the natural compound camptothecin which is found in the Chinese ornamental tree ''Campt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mevastatin
Mevastatin (compactin, ML-236B) is a hypolipidemic agent that belongs to the statins class. It was isolated from the mold ''Penicillium citrinum'' by Akira Endo in the 1970s, and he identified it as a HMG-CoA reductase inhibitor, i.e., a statin. Mevastatin might be considered the first statin drug; clinical trials on mevastatin were performed in the late 1970s in Japan, but it was never marketed. The first statin drug available to the general public was lovastatin. Mevastatin has since been derivatized to the compound pravastatin, which is a pharmaceutical used in the lowering of cholesterol and preventing cardiovascular disease. ''In vitro'', it has antiproliferative properties. A British group isolated the same compound from ''Penicillium brevicompactum'', named it ''compactin'', and published their results in 1976. The British group mentions antifungal properties with no mention of HMG-CoA reductase inhibition. High doses inhibit growth and proliferation of melanoma cells ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lovastatin
Lovastatin, sold under the brand name Mevacor among others, is a statin medication, to treat hypercholesterolemia, high blood cholesterol and reduce the risk of cardiovascular disease. Its use is recommended together with lifestyle changes. It is taken by mouth. Common side effects include diarrhea, constipation, headache, muscles pains, rash, and trouble sleeping. Serious side effects may include liver problems, rhabdomyolysis, muscle breakdown, and kidney failure. Use during pregnancy may harm the baby and use during breastfeeding is not recommended. It works by decreasing the liver's ability to produce cholesterol by blocking the enzyme HMG-CoA reductase. Lovastatin was patented in 1979 and approved for medical use in 1987. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. It is available as a generic medication. In 2020, it was the 99th most commonly prescribed medication in the United States, with more than 7mill ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Plinabulin
Plinabulin (provisional name BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and is in a world-wide Phase 3 clinical trial for non-small cell lung cancer. Plinabulin is being investigated for the reduction of chemotherapy-induced neutropenia and for anti-cancer effects in combination with immune checkpoint inhibitors and in KRAS mutated tumors. Plinabulin blocks the polymerization of tubulin Tubulin in molecular biology can refer either to the tubulin protein superfamily of globular proteins, or one of the member proteins of that superfamily. α- and β-tubulins polymerize into microtubules, a major component of the eukaryotic cytoske ... in a unique manner, resulting in multi-factorial effects including an enhanced immune-oncology response, activation of the JNK pathway and disruption of the tumor blood supply. References {{reflist Diketopiperazines Imidazoles Experimental cancer drugs Tert-butyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Asparaginase
Asparaginase is an enzyme that is used as a medication and in food manufacturing. As a medication, L-asparaginase is used to treat acute lymphoblastic leukemia (ALL) and lymphoblastic lymphoma (LBL). It is given by injection into a vein, muscle, or under the skin. A pegylated version is also available. In food manufacturing it is used to decrease acrylamide. Common side effects when used by injection include allergic reactions, pancreatitis, blood clotting problems, high blood sugar, kidney problems, and liver dysfunction. Use in pregnancy may harm the baby. As a food it is generally recognized as safe. Asparaginase works by breaking down the amino acid known as asparagine without which the cancer cells cannot make protein. The most common nonhematological adverse reactions of asparaginase erwinia chrysanthemi (recombinant) include abnormal liver test, nausea, musculoskeletal pain, infection, fatigue, headache, febrile neutropenia, pyrexia, hemorrhage (bleeding), stomatitis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Betulin
Betulin is an abundant, naturally occurring triterpene. It is commonly isolated from the bark of birch trees. It forms up to 30% of the dry weight of silver birch bark. It is also found in birch sap. '' Inonotus obliquus'' and red alder also contain betulin. The compound in the bark gives the tree its white color which appears to protect the tree from mid-winter overheating by the sun. As a result, birches are some of the northernmost occurring deciduous trees. It can be converted to betulinic acid (the alcohol group replaced by a carboxylic acid group), which is biologically more active than betulin itself. History Betulin was discovered in 1788 by German-Russian chemist Johann Tobias Lowitz. Chemistry Chemically, betulin is a triterpenoid of lupane structure. It has a pentacyclic ring structure, and hydroxyl groups in positions C3 and C28. Biological activities Preliminary ''in vitro'' studies have shown that betulin demonstrates anti-cancer properties against a variety ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Betulinic Acid
Betulinic acid is a naturally occurring pentacyclic triterpenoid which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase. It is found in the bark of several species of plants, principally the white birch (''Betula pubescens'') from which it gets its name, but also the ber tree (''Ziziphus mauritiana''), selfheal (''Prunella vulgaris''), the tropical carnivorous plants '' Triphyophyllum peltatum'' and ''Ancistrocladus heyneanus'', '' Diospyros leucomelas'', a member of the persimmon family, '' Tetracera boiviniana'', the jambul (''Syzygium formosanum''), flowering quince (''Pseudocydonia sinensis'', former ''Chaenomeles sinensis KOEHNE''), (''Chaenomeles sinensis KOEHNE'' is now named ''Pseudocydonia sinensis'') rosemary, and ''Pulsatilla chinensis''. Antitumor activity In 1995, betulinic acid was reported as a selective inhibitor of human melanoma. Then i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clavaric Acid
Clavaric acid is a triterpenoid produced by the mushroom '' Hypholoma sublateritium''. Clavaric acid was discovered by Merck Research Laboratories in a random screening of natural extracts. Clavaric acid is a reversible farnesyltransferase inhibitor The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in ... with an IC50 of 1.3 μM. References {{Reflist Lanostanes Triterpenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Illudin S
The illudins are a family of sesquiterpenes with antitumor antibiotic properties produced by some mushrooms. In their isolated form, illudins show selective toxicity for myelocytic leukemia and other carcinoma cells. Illudins are highly toxic, with little apparent therapeutic value in their natural form. Illudins are thought to be responsible for the toxicity of various ''Omphalotus'' species such as '' O. olearius'' and '' O. illudens'' (Jack o' Lantern mushrooms), and '' O. nidiformis'' (Australian ghost fungus). Active metabolites of illudins damage DNA via an unknown mechanism. In addition, genetic analysis suggests that the illudin-mediated DNA damage is ignored by global excision repair systems unless the lesions occur within stalled replication or transcription Transcription refers to the process of converting sounds (voice, music etc.) into letters or musical notes, or producing a copy of something in another medium, including: Genetics * Transcription (biology), the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acylfulvene
Acylfulvene is a class of cytotoxic semi-synthetic derivatives of illudin, a natural product that can be extracted from the jack o'lantern mushroom ''(Omphalotus olearius)''. One important acylfulvene, 6-hydroxymethylacylfulvene (irofulven), has been evaluated for the treatment of a wide assortment of cancers and tumors. It is thought that acylfulvene compounds kill cancer cells by DNA alkylation (see DNA methylation DNA methylation is a biological process by which methyl groups are added to the DNA molecule. Methylation can change the activity of a DNA segment without changing the sequence. When located in a gene promoter, DNA methylation typically acts t ...).Woynarowski, Jan M.; Napier, Cheryl; Koester, Steven K.; Chen, Shih-Fong; Troyer, Dean; Chapman, William; Macdonald, John R. Biochemical Pharmacology (1997), 54 (11), 1181-1193 CODEN: BCPCA6; . (Elsevier Science Inc.) References {{DEFAULTSORT:Acylfulvene Enones Tertiary alcohols Spiro compounds Cyclopropanes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Irofulven
Irofulven or 6-hydroxymethylacylfulvene (also known as HMAF of MGI-114) is an experimental antitumor agent. It belongs to the family of drugs called alkylating agents. It inhibits the replication of DNA in cell culture. Irofulven is an analogue of illudin S, a sesquiterpene toxin found in the Jack 'o' Lantern mushroom (''Omphalotus illudens''). The compound was originally synthesized by Dr. Trevor McMorris and found to have anticancer properties in mice by Dr. Michael J Kelner. __TOC__ Licensing and Clinical development The drug was created and patented by the University of California, San Diego (UCSD), and subsequently licensed to the US biotech company MGI Pharma. Eisai acquired MGI in 2007, and the license was returned to UCSD, which then re-licensed the potential cancer drug to Lantern Pharma in 2015. Soon after, the drug was again sub-licensed to Oncology Venture. The drug has undergone a number of clinical trials, mostly for late-stage tumors as well as ovarian and pros ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
