respiration

Mitochondrial respiration-IN-3, a fluorine derivative of Dalfopristin, possesses cell membrane permeability and exhibits the capability to inhibit mitochondrial translation in glioblastoma stem cells. This compound is utilized in cancer research [1].

Mitochondrial respiration-IN-1 hydrobromide (compound 49) is a potent mitochondrial inhibitor (IC50 = 8.8 mg mL) and significantly reduces mitochondrial respiration in platelets [1].

Mitochondrial respiration-IN-2, a fluorine derivative of Virginiamycin M1, inhibits the mitochondrial translation of glioblastoma stem cells [1].

Imeglimin hydrochloride (EMD 387008 hydrochloride) prevents human endothelial cell death by inhibiting mitochondrial permeability transition without inhibiting mitochondrial respiration.

Riboflavin (Vitamin B2) is a natural product, an endogenous human metabolite, and a micronutrient. Riboflavin is essential for the formation of two major coenzymes, flavin mononucleotide and flavin adenine dinucleotide. Riboflavin is involved in energy metabolism, cellular respiration, and antibody production, as well as normal growth and development.

(S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a tart-tasting organic dicarboxylic acid found in many sour foods, such as apples, and contributes to the sourness of green apples and tartness of wine, although its concentration decreases with fruit ripeness (wikipedia). In its ionized form, it is called malate, an intermediate in the TCA cycle alongside fumarate, and can be formed from pyruvate through anaplerotic reactions. In humans, malic acid is derived from food sources and synthesized in the body via the citric acid cycle in mitochondria, playing a crucial role in energy production under both aerobic and anaerobic conditions. Under aerobic conditions, malate is oxidized to oxaloacetate, providing reducing equivalents via the malate-aspartate redox shuttle, while during anaerobic conditions, its simultaneous reduction to succinate and oxidation to oxaloacetate removes excess reducing equivalents, reversing hypoxia’s inhibition of glycolysis and energy production. Studies on rats have shown that tissue malate depletes following exhaustive physical activity, suggesting that malic acid deficiency may cause physical exhaustion. Administering malic acid to rats has been shown to elevate mitochondrial malate, increasing mitochondrial respiration and energy production.

Adenine (6-Aminopurine), a purine derivative, is a nucleobase essential in biochemistry, participating in cellular respiration through ATP, NAD, and FAD, and in protein synthesis as a component of DNA and RNA.

Boscalid is a broad-spectrum carboxamide fungicide that inhibits fungal respiration by binding to the ubiquinone site of mitochondrial complex II/succinate dehydrogenase.1It suppresses mycelial growth ofS. minorby 87 to 100% and ofS. sclerotiorumby 77 to 100% when used at a concentration of 1 μg/ml.2In field studies, boscalid applied at 5.6 μg/cm2provides 55.5 and 30.4% disease control for lettuce drop caused byS. minorandS. sclerotiorum, respectively. It decreases cell viability of mouse primary cortical neurons following long-term exposure but is not cytotoxic (LC50= >100 μM for acute and continuous exposure). Formulations containing boscalid have been used in agriculture to prevent fungal growth on crops. 1.Wang, Y., Duan, Y., Wang, J., et al.A new point mutation in the iron-sulfur subunit of succinate dehydrogenase confers resistance to boscalid in Sclerotinia sclerotiorumMol. Plant Pathol.16(7)653-661(2015) 2.Matheron, M.E., and Porchas, M.Activity of boscalid, fenhexamid, fluazinam, fludioxonil, and vinclozolin on growth of Sclerotinia minor and S. sclerotiorum and development of lettuce dropPlant Dis.88(6)665-668(2004)

1-Hexanol (hexan-1-ol) is a natural product.1-Hexanol, a primary alcohol, is a surfactant that can be employed in industrial processes to enhance interfacial properties[1]. 1-Hexanol uncouples mitochondrial respiration by a non-protonophoric mechanism[2].

Riboflavin phosphate sodium (FMN) is the sodium phosphate form of riboflavin, a water-soluble and essential micronutrient that is the primary growth promoter of the naturally occurring vitamin B complex. Riboflavin phosphate sodium is converted into 2 coenzymes, flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD), which produce energy by aiding in the metabolism of fats, carbohydrates, and proteins, and are required for red blood cell formation and respiration, antibody production, and regulation of growth and reproduction in the body.

Mitochondrial fusion promoter M1, a modulator of mitochondrial dynamics, enhances mitochondrial function and cellular respiration, and has shown efficacy in reducing brain and cardiac damage in rats suffering from cardiac ischemia/reperfusion injury.

Aumitin, a diaminopyrimidine-based autophagy inhibitor, dose-dependently inhibits starvation- and rapamycin-induced autophagy with IC50s of 0.12 μM and 0.24 μM, respectively [1], and also inhibits mitochondrial respiration by targeting complex I.

CCI-006, a selective inhibitor and chemosensitizer for MLL-rearranged leukemia cells, disrupts mitochondrial respiration. This action leads to irreversible mitochondrial depolarization and triggers a pro-apoptotic unfolded protein response in specific MLL-r leukemia cells.

Licochalcone C (LICOCHALCONEC) has potent antioxidant properties and inhibition of bacterial growth and cellular respiration. It has cardioprotection effect, via antioxidant, anti-inflammatory, and anti-apoptotic activities. Licochalcone C exhibit inhibitory activity with cytotoxicity in a rat basophilic leukaemia cell line, RBL-2H3. Licochalcone C induces apoptosis via B-cell lymphoma 2 family proteins in T24 cells, it may be a potential adjuvant therapeutic agent for bladder cancer.

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

Compound 5C, referred to as Pkm2-in-4, is a selective PKM2 inhibitor (IC50 = 0.35 µM) that modulates pyruvate-dependent respiration and promotes mitochondrial H2O2 production rate and electron transport system coupling [1].

(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.

Piragliatin, also known as RO4389620, is a glucokinase activator. Piragliatin greatly enhances glucose-induced pancreatic islet respiration and insulin release. Piragliatin lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus. Piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of β-cell function and through fasting restricted changes in glucose turnover.

SLU-PP-332 is a pan-estrogen receptor-related receptor (ERR) agonist with high affinity for ERRα, ERRβ, and ERRγ, exhibiting EC50 values of 98, 230, and 430 nM, respectively. SLU-PP-332 enhances mitochondrial function and cellular respiration, increases type IIa oxidized skeletal muscle fibers, and enhances exercise tolerance in skeletal muscle cell lines. It has potential applications in the study of metabolic diseases, improvement of muscle function, and amelioration of metabolic disorders and aging.

Ninerafaxstat trihydrochloride shifts cellular metabolism to glucose oxidation from fatty acid oxidation. Ninerafaxstat trihydrochloride improves overall mitochondrial respiration and reduces fatty acid oxidation, thereby inhibiting the proliferation and growth of cancer cells.

Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial electron transport chain (ETC). Antimycin A prevents the transfer of electrons between the b-cytochromes and ubiquinone at the Q(inner) site of complex III. This results in the stabilization of the ubisemiquinone radical at the Q(outer) site of complex III, leading to increased production of superoxide. Antimycin A is widely used in research to shunt electron flow through the ETC to study the chemical details of oxygen respiration. Additionally, antimycin A has been shown to inhibit Bcl-2 and Bcl-xL proteins, inducing apoptosis.

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) were found to be potent inhibitors of mitochondrial respiration supported by pyruvate

Antifungal agent 47 (compound 3b) exhibits potent and broad-spectrum fungicidal properties, notably inhibiting respiration and adenosine 5′-triphosphate synthesis, demonstrating its potential as an effective fungicide [1].

Azoxystrobin (Bankit) is a broad-spectrum fungicide. Azoxystrobin induces ROS production, cell apoptosis and mitochondrial respiration by blocking electron transfer between cytochromes b and c1.

Picoxystrobin, a prominent primary strobilurin fungicide, is extensively utilized for efficient plant disease management. By obstructing electron transfer at the Qo center of cytochrome b and c1, picoxystrobin effectively halts mitochondrial respiration[1].

Dalapon is a selective herbicide used to control perennial grasses. The major use of dalapon is on food crops including sugarcane and sugar beets. Its use is no longer authorized in France. The National Institute for Occupational Safety and Health in the

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.

Penthiopyrad (MTF-753) shows a broad spectrum of antifungal activity and suppresses fungal respiration. Penthiopyrad can be used in studies about foliar and soil-borne plant diseases.

Adenine-2-d1 is a deuterated compound of Adenine. Adenine has a CAS number of 73-24-5. Adenine, a purine derivative, is a nucleobase with various roles in biochemistry including cellular respiration, in the form of both the energy-rich ATP and NAD and FAD, and protein synthesis, as a chemical component of DNA and RNA.

Hexafluoro is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrates activity in Vemurafenib-resistant melanoma in vivo.

Diuron is a Phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (25 nM/ml) decreases total respiration in roots of wheat by 50% and ground respiration by 100%. Diuron (2,500 ppm, dietary) increases the inc

Butalamine is a vasodilator (peripheral) with local anesthetic effects. It suppresses state 3 respiration and decreases ADP/O in the rat liver.

Cyanidin-3-O-arabinoside chloride has antioxidant activity. It reduces the peroxynitrite-induced suppression of mitochondrial respiration, DNA damage, PARS activation and vascular dysfunction in HUVECs.

Cefaloglycin (Cephaloglycin), an orally active, nephrotoxic β-lactam cephalosporin antibiotic, exhibits antibacterial activity primarily against Gram-Positive cocci, excluding enterococci. It impairs mitochondrial substrate uptake and respiration, underscoring its toxicity [1] [2] [3].

Ethofumesate is a chiral herbicide. Ethofumesate acts by inhibiting mitosis and reducing photosynthesis and plant respiration.

Coenzyme Q10 is a component of the electron transport chain and participates in aerobic cellular respiration, generating energy in the form of ATP. In its reduced form, it acts as an antioxidant. Coenzyme Q2 is a precursor of coenzyme Q10 that has 2, rather than 10, isoprenoid units on the ubiquinone base. It can act as an electron acceptor for bacterial Complex I. In mammalian cells, exogenous coenzyme Q2 prevents the production of reactive oxygen species associated with Complex I activity. Forms of coenzyme Q with shorter isoprenoid chains, including coenzyme Q2, induce p53-dependent apoptosis in human B-cell acute lymphoblastoid leukemia BALL-1 cells.

Vitamin B15 is a natural product and can used be as an agent stimulating cellular respiration, and is an immune-correcting agent.

Netzahualcoyone inhibited the respiration of intact cells of B. subtilis but had no effect on the respiration of E. coli.

Acyl coenzyme A synthetase (ACS), also known as acetyl coenzyme A synthetase, catalyzes the activation of fatty acids via coenzyme A through a two-step thioesterification process, forming acyl coenzyme A. It is crucial in anabolic and catabolic lipid metabolism pathways and contributes to the tricarboxylic acid (TCA) cycle during aerobic respiration [1].

GSK1733953A can be used as a small molecule Mycobacterium tuberculosis respiration inhibitor with an inhibitory effect on MenG activity and an IC50 value of 2.6 ± 0.6 μM.GSK1733953A is a selective biphenylbenzamide with an inhibitory effect on the catalytic methylation of the Mycobacterium tuberculosis desmethylnaphthoquinone methyltransferase, and the MIC of GSK1733953A against Mycobacterium tuberculosis H4Rv was 8.37 μg/ml. MIC of 8.37 μg/ml and MIC of 1.2 to 9.6 μg/ml against drug-resistant strains.GSK1733953A is a candidate compound for the treatment of tuberculosis.

Filipin II is a polyene and an active component of the polyene antibiotic filipin complex . [1] It has broad-spectrum antifungal activity, reducing growth of various fungi, including B. dermatitidis, C. neoformans, and H. capsulatum (MICs = 1-10 μg/ml). Filipin II inhibits ADP-stimulated respiration in rat liver mitochondria when used at a concentration of 3.5 mg/ml. [2] It also induces hemolysis of liposomes in a cholesterol-independent manner (IC50 = 0.5 μg/ml).[3]

Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.

Acefylline piperazine is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular......

6-Benzylthioinosine, a broad-spectrum metabolic inhibitor, inhibits glucose uptake, decreases glycolysis and ATP concentration with minimal changes in ROS and mitochondrial respiration.

Mtb-IN-4 (compound 17h) is a non-toxic isoxazole that exhibits anti-Mycobacterium tuberculosis (Mtb) activity with an IC50 value of 0.70 μM. It impedes Mtb respiration and biofilm formation within macrophages and augments the efficacy of the antibiotic isoniazid (INH) against INH-resistant Mtb mutants [1].

Mtb-IN-5 (compound (-)17j) is an isoxazole with anti-Mycobacterium tuberculosis (Mtb) activity, inhibiting Mtb respiration and biofilm formation within macrophages, and enhancing the efficacy of the antibiotic isoniazid (INH) against INH-resistant Mtb mutants [1].

8-Azido-ADP (disodium) is a covalently bound inhibitor of mitochondrial adenine nucleotide translocation that prevents the ADP-induced 4 to 3 shift in mitochondrial respiration. Additionally, in a light-dependent reaction, 8-Azido-ADP (disodium) irreversibly inhibits adenine nucleotide exchange.

Z16078526 enhances thermogenesis in mice by inducing endogenous Ucp1 expression, promoting p38 MAPK phosphorylation, and stimulating lipolysis in primary mouse brown adipocytes. Additionally, it activates thermogenic gene expression and mitochondrial activity, specifically uncoupled respiration, in these cells.

ROCK-IN-4 is a potent ROCK inhibitor that maintains NO release capacity, reversibly depolymerizes F-actin, and blocks mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be utilized to study glaucoma or high intraocular pressure.

Honokiol DCA is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrating activity in Vemurafenib-resistant melanoma in vivo.

Adenine hydrochloride (6-Aminopurine hydrochloride) is a hydrochloride salt form of adenine which is a nucleobase with a variety of roles in biochemistry.

Adenine monohydrochloride hemihydrate is a high affinity adenine receptor agonist (Ki = 18 nM at rat adenine receptor). It inhibits forskolin-stimulated cAMP formation in CHO cells transfected with the adenine receptor and also stimulates GTPγS binding (pEC50 values are 8.54 and 7.21 respectively).

Adenine hemisulfate (Diadenine sulphate) is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.