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Hyaluronan (HA) synthesis inhibitor
4-Methylumbelliferone is a selective inhibitor of Hyaluronan (HA) synthesis which is thought to function as an inhibitor via the depletion of UDP-glucuronic acid, the common substrate for HA synthesis. -
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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Tyrosinase inhibitor
Arbutin is a glycosylated hydroquinone used in traditional Chinese medicine (TCM). Arbutin inhibits melanin formation due to its tyrosinase inhibitory activity.
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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. -
Protein synthesis inhibitor
Azomycin(2-Nitroimidazole) is an antimicrobial antibiotic produced by a strain of Nocardia mesenterica, which is active against aerobic Gram-positive and Gram-negative bacteria. -
Lipoxygenase Inhibitor
Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 µM.
- Wafa Naji Shnaikat, .et al. , Iraqi J Pharm Sci, 2023, 31(Suppl.):92-99
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Aromatase Inhibitor
Chrysin is a naturally occurring flavone chemically extracted from the blue passion flower (Passiflora caerulea). It has been shown to induce an anti-inflammatory effect, most likely by inhibition of COX-2 expression and via IL-6 signaling. In rodent in vivo studies, chrysin was found anxiolytic. -
EGFR inhibitor
Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. -
Stat3 inhibitor
Cryptotanshinone, a natural compound isolated from the roots of Salvia miltiorrhiza Bunge (Danshen), dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of ~5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR. -
Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
Pdia3/ERp57 activator, STAT3 inhibitor
Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills.It is the product of hydrolysis by acids, strong bases, or enzymes of saponins, extracted from the tubers of Dioscorea wild yam, such as the Kokoro.- Rashmi Rawat, .et al. , Food Chemistry Advances, 2022, 1: 100092
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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. -
PDE4 inhibitor
Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer. -
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. -
CFTR Inhibitor
Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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SGLT1/SGLT2 inhibitor
Phlorizin is a competitive inhibitor of SGLT1 and SGLT2; this reduces renal glucose transport, lowering the amount of glucose in the blood.- Subramaniam M, .et al. , Am J Physiol Regul Integr Comp Physiol, 2019, Nov 20 PMID: 31746628
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PLA inhibitor
Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.- Darshika Pathiraja, .et al. , Food Chem, 2023, May 1;407:135145 PMID: 36521391
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MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
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
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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
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Hydroxylase inhibitor
Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons. -
Calcium Channel inhibitor
Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis. -
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. -
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. -
COX-1 inhibitor
(-)-Epicatechin is a natural product from green tea. (-)Epicatechin is an inhibitor of Cox-1- Grace Northrop, .et al. , Food Funct, 2022, Apr 4;13(7):3894-3904 PMID: 35285840
- A S D'Costa, .et al. , Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Mihaela Tudorache, .et al. , Food Hydrocoll, 2019, 97, Dec, 105193
- 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
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CDK336 Inhibitor
Pseudolaric Acid A is a diterpene acid isolated from Pseudolarix kaempferi, has antifungal, cytotoxic and antifertile activities. -
Carbonic anhydrase inhibitor
Punicalagin is an ellagitannin, a type of phenolic compounds. It is a highly active carbonic anhydrase inhibitor.- Elizabeth Read, .et al. , ANIM FEED SCI TECH, 2019, May, 251(187-197)
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HMG-CoA reductase inhibitor
Swertiamarin has shown potential as antiatherogenic agent by inhibiting HMG-CoA reductase activity in high cholesterol fed rats. -
plant growth inhibitor
Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. -
Pdia3/ERp57 activator, STAT3 inhibitor
Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis . -
Proteasome Inhibitor
Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.- Tarantelli C, .et al. , Clin Cancer Res, 2018, Jan 1;24(1):120-129 PMID: 29066507
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5-lipoxygenase inhibitor
Esculetin, a phenolic compound, acts as a 5-LO (5-lipoxygenase, 5-LOX) inhibitor. -
BACE1 Inhibitor
Timosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage. -
Microtubule polymerization inhibitor
Cucurbitacin B, a natural triterpenoid is well-known for its strong anticancer activity, and recent studies showed that the compound inhibits JAK/STAT3 pathway. Also it is an potent Microtubule polymerization inhibitor -
STAT inhibitor
Nitidine chloride, a natural benzophenanthridine alkaloid, has been shown to inhibit cancer growth via induction of cell apoptosis and suppression of cancer angiogenesis. -
Bcl-2 Inhibitor
Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic. -
ATPase and GTPase inhibitor
Etidronate Disodium is a bisphosphonate bone resorption inhibitor.