Guttiferae

Hyperoside is a NF-κB inhibitor, found from Hypericum monogynum. Hyperoside shows anti-tumor, antifungal, anti-inflammatory, anti-viral, and anti-oxidative activities, and can induce apoptosis.

Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.

Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC₅₀s of 0.66 μM and 7.39 μM, respectively. Garcinol also inhibits histone acetyltransferases (HATs, IC₅₀= 7 μM) and p300/CPB-associated factor (PCAF, IC₅₀ = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity.

Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC₅₀s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.

Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.

Kolaflavanone is an allosteric inhibitor of Eg5. Kolaflavanone inhibits the ATPase and tyrosinase activities of Eg5 under both basal and microtubule-activated conditions, suppresses microtubule sliding activity, binds to the L5/α2/α3 allosteric pocket of Eg5, induces conformational changes of Eg5 and microtubule dissociation, interacts with aldehyde dehydrogenase, inhibits the ATPase activity of kinesin-1, and binds to HSA via pH-dependent forces. Kolaflavanone exhibits antihepatotoxic activity and can be used in studies related to Phalloidin (HY-P0028)-induced liver injury.

Gambogin is an α-glucosidase inhibitor, found in the resin and dry latex of Garcinia hanburyi. Gambogin exists as an inseparable diastereomeric pair of C-2 epimers (8a and 8b), with 8a having an α-glucosidase inhibitory IC₅₀ of 209.2 μM and 8b showing α-glucosidase inhibitory IC₅₀ > 300 μM. Gambogin can be used for the research of type 2 diabetes and cervical cancer.

Deoxymorellin is a caged xanthone found in resins and fruits of Garcinia hanburyi hook. f.. Deoxymorellin exhibits cytotoxicity. Deoxymorellin can be used for research of Methicillin (HY-121544)-resistant or Methicillin-susceptible Staphylococcus aureus.

Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes.

Hydroxycitric acid is an orally active, multi-target, multi-bioactive organic acid. activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Hydroxycitric acid activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Hydroxycitric acid activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation.

Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer.

Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.

beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC₅₀ of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).

Stigmastanol is a 6-amino derivative. Stigmastanol can be isolated from Hypericum riparium. Stigmastanol increases the secretion of IL-2 and IL-10. Stigmastanol reduces the maximum mitochondrial respiration of cells. Stigmastanol has beneficial effects on the weakened immune function of asthma.

Citric acid tripotassium hydrate (Potassium citrate monohydrate) is a natural preservative and food tartness enhancer. Citric acid tripotassium hydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid tripotassium hydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid tripotassium hydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries.

Xanthone is a monoamine oxidase A (MAO-A) inhibitor with an IC₅₀ of 0.84 µM. Xanthon inhibits Norepinephrine (HY-13715) and high-K⁺-induced vasoconstriction with IC₅₀ values of 60.26 μM and 82.9 μM, respectively. Xanthon increases intracellular cyclic adenosine 3′,5′-monophosphate (cAMP) content and blocks Ca²⁺ channels. Xanthone is the scaffold of several pharmacologically active compounds.

Protohypericin is a compound that can be extracted from Hypericum perforatum. Protohypericin has low photocytotoxicity but can be efficiently photoconverted into Hypericin (HY-N0453) with high phototoxicity under visible light. Protohypericin can be used in cancer research.

Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC₅₀ for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer.

Macurin is a xanthone that can be isolated from Garcinia lancilimba.

Garcinia cambogia extract is an orally active anti-obesity agent. Garcinia cambogia extract upregulates the gene expression of aP2, SREBP1c, PPARγ2 and C/EBPα. Garcinia cambogia extract reduces the rate of body weight gain, visceral fat accumulation, lipid levels in blood and liver, as well as plasma insulin and leptin levels. Garcinia cambogia extract ameliorates high-fat diet-induced obesity.