mortality

Gizzerosine, a biogenic amine formed during feed processing, is a toxicant that induces mortality in livestock.

Zoliprofen is a potent and orally available non-steroidal anti-inflammatory agent with anti-inflammatory, antipyretic and analgesic activity, and inhibits carobolin, mycobacterium, and knife-ball protein A-induced rat paw oedema, as well as anti-rat serum-induced fracture or dorsal skin oedema. Zoliprofen is 20 times more effective than ibuprofen and fenoprofen against collagen- or arachidonic acid-induced platelet aggregation in rats and rabbits. Zoliprofen was 20 times more effective than ibuprofen and fenoprofen in inhibiting endotoxin-induced diarrhoea in mice and arachidonic acid-induced acute mortality in rabbits.

Penciclovir (BRL 39123) is a Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor. In HSV infected cells, penciclovir is phosphorylated by viral thymidine kinase and subsequently converted by cellular kinases into the active metabolite, penciclovir triphosphate, which competitively inhibits viral HSV polymerase by blocking deoxyguanosine triphosphate substrate binding. As a result, herpes viral DNA synthesis and replication are selectively inhibited.

Homovanillyl alcohol, a biological metabolite of Hydroxytyrosol, is a phenolic compound found in virgin olive oil (VOO) and wine. It exhibits high scavenging activities, protects red blood cells from hemolysis in a dose-dependent manner, and has a protective effect on cardiovascular disease and total mortality.

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki values of 0.55 μM in rabbit platelet membranes and 0.1 μM in guinea pig cerebellum membranes.

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb- -) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb- - macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb- - mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

Fervenulin is isolated from a nematicidal actinomycete Streptomyces sp. CMU-MH021 with nematicidal activity. It also inhibits egg hatch and J2 mortality of M. incognita (MICs: 30 μg mL and 120 μg mL, respectively).

UMB24 is an effective antagonist of the σ2 receptor, exhibiting dissociation constants (Ki values) of 170 nM for the σ2 receptor and 322 nM for the σ1 receptor. This compound mitigates cocaine-induced convulsions and hyperactivity without causing mortality.

(±)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.

Odoratone shows insecticidal activities, it shows mortality on fourth instar larvae of mosquitoes (Anopheles stephensi) with LC(50) values of 154 ppm. Odoratone exhibits strong antifeedant activity against Pieris brassicae.

GABA-IN-2 (Compound 5), a GABA inhibitor, exhibits both larvicidal and insecticidal properties, achieving an 87% mortality rate at a concentration of 50 mg L [1].

Maculatin 1.1 TFA, an antimicrobial peptide, exhibits a minimum inhibitory concentration (MIC) of 7 μM against Staphylococcus aureus and induces bacterial mortality by perforating the organism's membrane [1].

MurB-IN-1 (compound 44) is a potent inhibitor of MurB, an essential enzyme involved in the synthesis of the bacterial cell wall. With a binding affinity of Kd 3.57 μM, MurB-IN-1 effectively hinders MurB activity, presenting a promising therapeutic option against P. aeruginosa, a highly virulent and opportunistic pathogen associated with severe infections and mortality [1].

1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+ Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

3'-Ethoxy-5,6-dihydrospinosyn J 17-pseudoaglycone is a potent insecticidal derivative of spinosyn. At a concentration of 500 mg L, it achieves a 100% mortality rate against armyworms, aphids, and red spider mites.

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.

Neospiramycin I is a macrolide antibiotic and derivative of spiramycin I.1It is active against the macrolide-sensitive KB210, but not the macrolide-resistant KB224, strain ofS. aureus(MICs = 3.12 and >100 μg/ml, respectively), as well asB. cereus,B. subtilis,M. luteus,E. coli, andK. pneumoniae(MICs = 1.56, 3.12, 3.12, 0.2, 50, and 12.5 μg/ml, respectively). Neospiramycin I binds toE. coliribosomes with an IC50value of 1.2 μM. It protects against mortality in a mouse model ofS. pneumoniaetype III infection (ED50= 399.8 mg/kg).2

Orfamide A, a lipopeptide biosurfactant isolated from P. protegens, exhibits multifaceted bioactivity. With an LC50 of 34.5 μg/ml, it significantly increases mortality in adult green peach aphids. Additionally, at a concentration of 50 μM, Orfamide A inhibits appressoria formation in M. oryzae isolates and decreases the prevalence of sporulating blast lesions in M. oryzae-infected plants. Furthermore, it demonstrates efficacy against T. b. brucei, with an IC50 value of 6 µM.

SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma

Antifungal agent 31 is an orally active, triazole antifungal agent possessing a pyrrolizinone scaffold that exhibits some antifungal activity against Candida and filamentous fungi.Antifungal agent 31 significantly reduced mortality and renal fungal burden in two mouse models of lethal systemic infection.

Tat-beclin 1 TFA, a peptide derived from a segment of the autophagy protein beclin 1, effectively induces autophagy and interacts with the autophagy negative regulator GAPR-1 (GLIPR2). It reduces the accumulation of polyglutamine expansion protein aggregates and limits the in vitro replication of various pathogens, including HIV-1. Additionally, Tat-beclin 1 TFA has been shown to decrease mortality rates in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].

DSM43 is a dihydroorotate dehydrogenase (DHODH) inhibitor. Malaria puts at risk nearly half the world's population and causes high mortality in sub-Saharan Africa, while drug resistance threatens current therapies. The pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) is a validated target for malaria treatmen