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Tyrosinase inhibitor
Aloin (Barbaloin) is a yellow crystalline substance obtained from aloe and is reported to be a potent inhibitors of tyrosinase. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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cytochrome oxidase inhibitor
Artesunate is a semisynthetic derivative of artemisinin used to treat malaria. It has also been shown to effective against other parasites such as liver flukes. Artesunate also demonstrates cytotoxic action against cancer cell lines of different tumor types. Artesunate has been shown to inhibit TNF--induced production of proinflammatory cytokines via inhibition of NF-B and PI3 kinase/Akt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes. -
Biochanin A is an antiproliferative and anti-inflammatory agent that inhibits iNOS expression and lipopolysacharide (LPS)-induced nitric oxide production in macrophages. Additionally, Biochanin A displays the ability to block phosphorylation of IκBα and p38 MAPK, which prevents NF-κB activation. Furthermore, Biochanin A has been observed to suppress IL-6, IL-1β, and TNF-α production.
- Capsaicin is an active component of chili peppers, which are plants belonging to the genus Capsicum.
- Xiao-Yan Liu, .et al. , Sci Rep, 2022, 12: 11996 PMID: 35835852
- Thieu X. Phan, .et al. , bioRxiv, 2021, February 27
- Thieu X Phan, .et al. , J Physiol, 2020, Sep 17 PMID: 32944976
- Jun Hai, .et al. , Biosci Biotechnol Biochem, 2020, Jul 7;1-7 PMID: 32633621
- Thieu X. Phan, .et al. , bioRxiv, 2020, February 04
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Celastrol is a triterpenoid antioxidant compound isolated from the Chinese Thunder of God vine (T. wilfordii). In an isolated rat liver assay of lipid peroxidation, celastrol had an IC50 value of 7 µM, equivalent to about 15 times the antioxidant potency of α-tocopherol.
- Xuechun Wang, .et al. , Int J Mol Sci, 2023, Mar 8;24(6):5204 PMID: 36982279
- R. San Gil, .et al. , bioRxiv, 2020, Jan
- Abdin AA, .et al. , Eur J Pharmacol., 2014, 742:102-12 PMID: 25218987
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. - Cytisine is a nicotinic acetylcholine receptor agonist, and as a pharmaceutical preparation it is available for the treatment of nicotinism. It is a pyridine-like alkaloid that can be toxic in high doses. Pharmacologically it exhibits similar effects to nicotine due to structural similarity of the two molecules.
- Daidzein belongs to the group of isoflavones. Daidzein and other isoflavone compounds, such as genistein, are present in a number of plants and herbs. Soy isoflavones are a group of compounds found in and isolated from the soybean. Besides functioning as antioxidants, many isoflavones have been shown to interact with animal and human estrogen receptors, and therefore are known as phytoestrogens.
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
- Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate, artemether, etc.) and is also available as a drug in itself. It is a semi-synthetic derivative of artemisinin and is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs.
- Xinyu Zhou, .et al. , Cancers (Basel), 2020, Sep; 12(9): 2514 PMID: 32899699
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15-PGDH inhibitor
Glycyrrhetinic acid inhibits the enzymes (15-hydroxyprostaglandin dehydrogenase and delta-13-prostaglandin) that metabolize the prostaglandins PGE-2 and PGF-2α to their respective 15-keto-13,14-dihydro metabolites which are inactive. - Fisetin is a flavonol, a structurally distinct chemical substance that belongs to the flavonoid group of polyphenols. It can be found in many plants, where it serves as a colouring agent. Possible anti-aging, anti-inflammatory, anti-cancer, and anti-viral properties of fisetin are under active scientific investigation.
- Bih-Cheng Chen, .et al. , Phytomedicine, 2019, Apr; 57:1-8
- Jeng LB, .et al. , J Cell Physiol, 2018, Sep;233(9):7134-7142 PMID: 29574877
- Kuan-Ho Lin, .et al. , Journal of Functional Foods, 2018, 52: 212-218
- Gastrodin (Gastrodine) is a polyphenol. It is the glucoside of 4-hydroxybenzyl alcohol (gastrodigenin).
- Glycyrrhizic acid is a widely used anti-inflammatory agent isolated from the licorice root.
- Indole-3-carbinol is produced by the breakdown of the glucosinolate glucobrassicin, which can be found at relatively high levels in cruciferous vegetables.
- L(+)-Rhamnose (Rham) is a naturally-occurring deoxy sugar. It can be classified as either a methyl-pentose or a 6-deoxy-hexose.
- Lappaconite Hydrobromide is a kind of alkaloid extracted from Aconitum sinomontanum Nakai and has anti-inflammatory effects.
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PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. - Morin hydrate is a chemical compound. Morin can be used to test for the presence of aluminum or tin in a solution, since it forms characteristically fluorescent coordination complexes with them.
- Myricetin (Cannabiscetin) is a naturally occurring flavonol, a flavonoid found in many grapes, berries, fruits, vegetables, herbs, as well as other plants.
- Naringin (Naringoside) is a flavanone glycoside and is a major flavonoid in grapefruit and gives the grapefruit juice its bitter taste.
- Naringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin.
- Flavanone glycoside with neuroprotective and antioxidant properties. Does not inhibit oral carcinogenesis in a rat model unlike other citrus flavanones, but does exert a protective effect against gastritis and gastric lesions.
- Neohesperidin dihydrochalcone (Nhdc) is a flavonoid sweetening agent with potent antioxidant activity.
- Nobiletin is a chemical compound. It is an O-methylated flavone, a flavonoid isolated from citrus peels like in tangerine. Nobiletin was found to have anti-inflammatory and anti-tumor invasion, proliferation, and metastasis in vitro and in vivo. Nobiletin was also found to potentially inhibit cartilage degradation.
- Yi-Hsin Lo, .et al. , Biomedicines, 2022, Mar 3;10(3):595 PMID: 35327397
- Oxymatrine (Matrine N-oxide) is one of components of the root of Sophora flavescens.
- Paeonol (Peonol) is a major component extracted from Chinese herbs moutan cortex and Cynanchum paniculatum .
- Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, along with chavicine (an isomer of piperine). It has also been used in some forms of traditional medicine and as an insecticide.
- Rhein is a substance in the anthraquinone group found in rhubarb species like Rheum undulatum or Rheum palmatum or in Cassia reticulata.
- Ryota Kitakami, .et al. , Bioorg Med Chem, 2021, Jun 26;44:116292 PMID: 34225167
- Rheochrysidin is one of the major components of Da-Cheng-Qi decoction used in the treatment of inflammation.
- Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs, which has shown a variety of intriguing biological properties such as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity and thermoregulatory, vasorelaxing activity, as well as effects on the cardiovascular and endocrine systems.
- Salidroside (Rhodioloside) is a glucoside of tyrosol found in the plant Rhodiola rosea. It is thought to be one of the compounds responsible for the antidepressant and anxiolytic actions of this plant, along with rosavin.
- Silymarin (Silibinin B) inhibits chemically induced urinary bladder tumor growth and progression possibly by inhibiting cell proliferation and enhancing apoptosis.
- Sinomenine(Cucoline) is traditionally used in herbal medicine in these countries, as a treatment for rheumatism and arthritis.
- Zheng Sun, .et al. , Drug Des Devel Ther, 2018, 12: 2413-2421 PMID: 30122899
- Tangeretin (Tangeritin) is an O-polymethoxylated flavone that is found in tangerine and other citrus peels. Tangeretin (Tangeritin) strengthens the cell wall and acts as a plant's defensive mechanism against disease-causing pathogens. Tangeretin (Tangeritin) also shows enormous potential as an anti cancer agent.
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Phospholipase inhibitor
Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.- Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
- Tanshinone IIA (TIIA) is one of the major extracts obtained from Salvia miltiorrhiza BUNGE, which has anti-inflammatory and anti-apoptotic effects on many diseases.
- Judith Schaf, .et al. , Cell Death Discov, 2023, May 19;9(1):172 PMID: 37202382
- Williams R, .et al. , Research Square, 2022, NOV 21
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VEGFR-2 Inhibitor
Taxifolin is found to bind at the ATP-binding site on VEGFR-2 kinase with large value of binding energy and act as type I competitive inhibitor.- Keji Yu, .et al. , Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. , Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. , Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
- Troxerutin(Trihydroxyethylrutin) is a flavonol, a type of flavonoid. It is more accurately a hydroxyethylrutoside. It can be isolated from Sophora japonica, the japanese pagoda tree.It is used as a vasoprotective.
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5-alpha reductase inhibitor
β-sitosterol reduces blood levels of cholesterol, and is sometimes used in treating hypercholesterolemia. β-Sitosterol inhibits cholesterol absorption in the intestine. When the sterol is absorbed in the intestine, it is transported by lipoproteins and incorporated into the cellular membrane. -
Ca2+ signaling modulator
Astragaloside A is a novel regulator of HIF-1α and angiogenesis through the PI3K/Akt pathway in HUVECs that are exposed to hypoxia. - Schisandrin B is the most abundant dibenzocyclooctadiene isolated from the fruit of Schisandra chinensis (Turcz) Baillon or Wu-Wei-Zi (transliterally meaning "the fruit of five tastes" in Chinese), which is a commonly used tonic herb in Chinese medicine, particularly for the treatment of liver ailments.
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Topoisomerase
(S)-10-Hydroxycamptothecin is a camptothecin derivative that inhibits DNA topoisomerase by enacting strand breaks in chromosomal DNA and inducing apoptosis. -
PKC inhibitor
Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity. - Catechin is a natural flavonoid that has chemopreventive and antitumor properties.
- Rashmi Rawat, .et al. , Food Chemistry Advances, 2022, 1: 100092
- Vergne MJ, .et al. , J Food Sci, 2018, May;83(5):1258-1264 PMID: 29668030
- Md Shajedul Islam, .et al. , Innovative food science & emerging technologies, 2016, v.34 pp. 344-351
- Islam MS, .et al. , J Agric Food Chem, 2016, Oct 10 PMID: 27632812
- Eleutheroside E(EE) has anti-inflammatory and protective effects in ischemia heart, the beneficial effect of EE may provide an effective and powerful strategy to alleviate behavioral alterations induced by sleep deprivation, it may influence to immune-enhancing through increasing the physical endurance capacity and immune cell activation. EE significantly decreases the inflammatory cell infiltration, pannus formation, cartilage damage, bone erosion of CIA mice, the generation of TNF-α and IL-6, the metabolism of drugs metabolized via CYP2C9 and CYP2E1.