Isotope-Labeled Polyketides

(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC₅₀ value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.

Erythromycin-13C2 is a macrolide antibiotic that can be used to treat respiratory infections, skin infections, and chlamydia infections.

Formononetin-d₃-1 is the deuterium-labeled Formononetin (HY-N0183).

Erythromycin-d₃ is the deuterium labeled Erythromycin. Erythromycin is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid. Erythromycin also exhibits antitumor and neuroprotective effect in different fields of research.

Resveratrol-(4-Hydroxyphenyl)-¹³CN₆ is the ¹³C labeled Resveratrol-(4-Hydroxyphenyl).

Hypericin-d₁₀ is the deuterium labeled Hypericin. Hypericin is a photosensitive antiviral with anticancer and antidepressant agent derived from Hypericum perforatum. It can inhibit tyrosine kinases with IC50 of 7.5 μM.

Catechin-¹³C₃ is the ¹³C-labeled Catechin. Catechin ((+)-Catechin) inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.

Doxycycline-d₃ hyclate (major) is the deuterium labeled Doxycycline hyclate (HY-N0565B). Doxycycline hyclate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hyclate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hyclate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hyclate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hyclate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hyclate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.

Azithromycin-¹³C,d₃ is the deuterium and ¹³C labeled Azithromycin.

Quercetin-d3 hydrate is a deuterium labeled Quercetin hydrate (HY-18085A), a flavonoid which can stimulate recombinant SIRT1 and also a PI3K inhibitor with IC₅₀s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Azithromycin-¹³C,d₃-1 is a deuterated labeled Azithromycin.

Fisetin-d5 is a deuterated labeled Fisetin. Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.

(Rac)-Zearalenone-d₆ is the deuterium labled Zearalenone (HY-103447). Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts.

Daidzein-d₆ is a deuterium labeled Daidzein (HY-N0019). Daidzein is a soy isoflavone, which acts as a PPAR activator.

Cyclosporin A-¹³C₂,d₄ (Cyclosporine A-¹³C₂,d₄) is the deuterated, ¹³C-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Cyclosporin A acetate-d₄ (Cyclosporine A acetate-d₄) is the deuterated-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

4',7-Dimethoxyisoflavone-d₆ (Dimethoxydaidzein-d₆) is the deuterium labeled 4',7-Dimethoxyisoflavone (HY-N2145). 4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity.

Physcion-d₃ (Parietin-d₃) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC₅₀ and a K_d of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.

Hypericin-d₂ is deuterium labeled Hypericin.

Minocycline-d₆ sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.