mitochondrial dysfunction

Triheptanoin (IND 106011) is a fatty acid metabolic modulator. It potentially for the treatment of fatty acid oxidation disorders and GLUT1.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

USP30 inhibitor 11 (USP30-IN-11) is a selective USP30 inhibitor (IC50: 0.01 µΜ) that inhibits SVA and can be used in studies of cancer, mitochondrial dysfunction and Parkinson's.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent generated by the reaction of linoleic acid with plant and mammalian lipoxygenases. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.

Sonlicromanol hydrochloride (KH176 hydrochloride) is a ROS-redox modulator that crosses the blood-brain barrier, has potential anticancer activity, improves m.3243A>G heterogeneity in iPSC-derived neurons associated with It has potential anticancer activity, ameliorates neuronal network dysfunction and transcriptomic changes associated with m.3243A>G heterogeneity in iPSC-derived neurons, and can be used for the treatment of mitochondrial diseases.

Anti-inflammatory agent 49 is a potent inhibitor of Drp1-Fis1 interaction, inhibits GTPase, and can be used in the study of diseases caused by mitochondrial dysfunction.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

1. Oxyresveratro can inhibit tyrosinase activity. 2. Oxyresveratro is useful to trauma models, as toxicity to glia could be beneficial by inhibiting reactive gliosis. 3. Oxyresveratrol (trans-Oxyresveratrol) has antioxidant activity, can reduce neuronal oxidative damage and protect hepatocytes against oxidative stress and mitochondrial dysfunction, which may be associated with activation of Nrf2.

Nerol (Neryl alcohol) is a monoterpene found in many essential oils, such as lemon balm and hop.Nerol can lessened the severity of ouabain-triggered arrhythmias in mammalian heart.

Nigericin is a polyether antibiotic with potent antimicrobial, antimalarial, anticoronaviral and anticancer activities. It is capable of promoting cellular potassium efflux, inducing Caspase-1 GSDMD and Caspase-3-mediated cellular pyroptosis and apoptosis in triple-negative breast cancer, and inducing apoptosis in PEL (primary exudative lymphoma) cells through mitochondrial dysfunction and Wnt β-catenin signaling downregulation.

MitoTEMPOL is a mitochondria-targeted antioxidant that prevents septal dysfunction by reversing sepsis-induced decreases in mitochondrial function, activation of protein hydrolysis pathways, and reductions in myosin heavy chain content, as well as eliminating cytokine-induced increases in muscle cell superoxide production and decreases in cell size.

Ginsenoside F2 has antiproliferative activity against breast cancer stem cells (CSCs). It induces apoptosis in breast CSCs by activating the intrinsic apoptotic pathway and mitochondrial dysfunction.

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

Isolongifolene ((-)-Isolongifolene), a tricyclic sesquiterpene isolated from Murraya koenigii, exhibits antioxidant, anti-inflammatory, anticancer, and neuroprotective properties. It mitigates Rotenone-induced oxidative stress, mitochondrial dysfunction, and apoptosis by modulating the PI3K AKT GSK-3β signaling pathways.

Mito-apocynin (C11) is a mitochondria-targeting antioxidant that works by targeting and neutralizing reactive oxygen species (ROS) produced during cellular respiration. Triphenylphosphonium bromide has been found to be effective in preventing mitochondrial dysfunction, which is a major cause of the aging process and various diseases. It has anti-inflammatory, anti-apoptotic and antioxidant activities.

AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 protects against mitochondrial dysfunction[1]. AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis.

KL1333 (NQO1 activator 1) enhances energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. Elevated NAD+ levels trigger the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 is an orally available NAD+ modulator. It reacts with NAD(P)H: NQO1 as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation.

Fenchlorphos (Dermafos) is a cholinesterase inhibitor, used as an insecticide.

Oleuroside can protect against mitochondrial dysfunction in models of early Alzheimer's disease and brain ageing.

Apoptosisinducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with an IC50 range of 1.2-4.8 μM. It arrests the cell cycle at the G2 M phase, induces apoptosis in BGC-823 cells, and causes mitochondrial dysfunction. In mice, Apoptosisinducer 24 exhibits antitumor activity without significant toxicity, having an LD50 of 91.2 mg kg.

Apoptosisinducer 25 (Compound 4H) demonstrates potent anticancer capabilities by inhibiting the proliferation of BGC-823 cancer cells with an IC50 of 0.37 μM. It induces apoptosis in BGC-823 cells, causes mitochondrial dysfunction, and arrests the cell cycle at the G2 M phase. Additionally, Apoptosisinducer 25 exhibits favorable pharmacokinetic properties in rats.

BPU17 interacts with PHB1 and disrupts the PHB1-PHB2 interaction, causing slight mitochondrial dysfunction. This damage hinders transcription dependent on SRF CArG-box, thereby inhibiting epithelial-mesenchymal transition (EMT) in retinal pigment epithelial cells (RPEs). BPU17 has demonstrated anti-fibrotic activity in vivo. It holds potential as a research agent for anti-angiogenic age-related macular degeneration (nAMD).

IIQLPEIVVV TFA serves as a specific inhibitor targeting the Drp1-Mff interaction. This compound discriminates between physiological and pathological fission, hindering physiological fission which leads to mitochondrial dysfunction. IIQLPEIVVV TFA is also utilized in research related to Huntington's disease.

SIRT3 Activator 1 (Compound 5v) is a selective activator of SIRT3. It enhances the expression of SIRT3, leading to upregulation of SOD2 and OPA1. This activity effectively mitigates mitochondrial dysfunction, alleviates oxidative stress, and maintains the vitality of cardiac myocytes. SIRT3 Activator 1 is useful in the study of cardiovascular diseases.