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Aloe emodin is a anthraquinone present in aloe latex, an exudate from the aloe plant. It has a strong stimulant-laxative action.
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Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- 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
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Emodin is a purgative resin, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). It belongs to a family of compounds called anthraquinones, which have shown anti-inflammatory and anticancer effects
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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autophagy inhibitor
Monensin sodium is an ionophore and inhibitor of autophagy commercially used in livestock feed. It inhibits autophagy, interfering with the fusion of the autophagosome and the lysosome. - Pyrazinamide is an antimycobacterial compound that inhibits the growth of the human M. tuberculosis H37Rv strain.
- Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases???LOX, IC50=2.7 μM???, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.
- Wafa Naji Shnaikat, .et al. , Iraqi J Pharm Sci, 2023, 31(Suppl.):92-99
- Ha T. Tran, .et al. , PLoS One, 2017, 12(3): e0173373 PMID: 28278187
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Autophagy/PI3K Inhibitor
3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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K+/Na+/Ca+ Channel Blocker
Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents. -
autophagy inducer
Flubendazole is an anthelmintic used for protection against internal parasites and worms in dogs and cats. - Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
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neuromuscular blocking agent
Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission. - TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.
- Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)
- Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
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Autophagy Inhibitor
Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
- Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
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Glutaminase inhibitor
CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.
- Beatriz Giesen, .et al. , Pharmaceutics, 2021, Feb 23;13(2):295 PMID: 33672398
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anti-cancer agent
Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity. -
anti-bacterial agent
Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 ?g/ml . Pogostone induces cell apoptosis and autophagy. -
ULK1 inhibitor
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .- SR Bonam, .et al. , Cells, 2020, May; 9(5): 1321 PMID: 32466347
- Altea Rocchi, .et al. , PLoS Genet, 2017, Aug; 13(8): e1006962 PMID: 28806762
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Autophagy inhibitor
Lys05 is a potent lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. - Azithromycin Dihydrate is an acid stable orally administered macrolide antimicrobial drug, structurally related to erythromycin.
- Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Egawa Y, .et al. , PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
- Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
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Autophagy inhibitor
Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34. -
tricyclic antidepressant
Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression. - Lumefantrine, also known as HSDB 7210, is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with artemether for improved efficacy. This combination therapy exerts its effects against the erythrocytic stages of Plasmodium spp. and may be used to treat infections caused by P. falciparum and unidentified Plasmodium species, including infections acquired in chloroquine-resistant areas.
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nucleoside analog
Cytarabine hydrochloride, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. -
CoA reductase inhibitor
Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor. -
iron chelator
Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions. -
mitophagy regulator
P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing δ??m and retains activity in cells devoid of a fully functional PINK1/Parkin pathway. - Oxyphenisatin acetate, the pro-drug of oxyphenisatin, is used to be a laxative.
- Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
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ULK1/ULK2 inhibitor
MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. -
lysosomal autophagy inhibitor
Lys01 trihydrochloride (Lys05) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay. -
natural pterostilbene analogue
3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 ?M for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy.