ameliorate

5-Hydroxy-1-methylhydantoin (HD-003) is an antioxidant potentially for the treatment of renal failure. A creatinine metabolite, 5-Hydroxy-1-methylhydantoin , a hydroxyl radical scavenger, has previously been shown to confer renoprotection by inhibiting the progression of chronic kidney disease in rats. 5-Hydroxy-1-methylhydantoin is a novel anti-oxidant drug completely suppressed the expression of B2-kinin receptors (B2KR) in response to high glucose (25 mM) stimulation in VSMC and was also shown to attenuate the effects of BK on VSMC remodeling. 5-Hydroxy-1-methylhydantoin inhibited the BK-induced increase in MAPK phosphorylation and attenuated the increase in connective tissue growth factor (CTGF) protein levels in VSMC. These findings suggest that 5-Hydroxy-1-methylhydantoin may confer vascular protection against high glucose concentrations and BK-stimulation to ameliorate vascular injury and remodeling through its anti-oxidant properties.

3,4,5-Trimethoxybenzoic acid (Gallic acid trimethyl ether) are potent antioxidants and inhibitor of cytokine production. It can ameliorate chronic stress-induced various behavioral and biochemical alterations in mice. It also exerts hepatoprotective effects in CCl4-induced rats, specifically by modulating oxidative-nitrosative stress and inflammation.

Epalrestat (ONO2235), an aldose reductase inhibitor, is well tolerated in Long-term therapy. It can effectually ameliorate the associated symptoms of diabetic neuropathy and delay the progression of the disease, particularly in patients with limited microangiopathy and good glycemic control.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Acetamide, N-[2-[(5-chloro-2 methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]-inhibits pro-matrix metalloproteinase activation and can be used to prevent, treat or ameliorate MMP9 and or MMP13-mediated syndromes.

Isolicoflavonol is a potential cancer chemopreventive agent.

WJ-39 is an orally active aldose reductase (AR) inhibitor that ameliorates renal lesions in diabetic nephropathy through activation of Nrf2 signaling, and may be used to ameliorate renal insufficiency and fibrosis.WJ-39 inhibits oxidative stress and inhibits the activation of the inflammatory vesicle of the oligomerization structural domain-like receptor family, pyrin structural domain 3 (NLRP3).

Corynoxine B (Cory B), a natural alkaloid isolated from Uncaria rhynchophylla (Miq. ), is an autophagy inducer that enhances the activity of Beclin 1 VPS34 complex and increases autophagy by facilitating the interaction between Beclin 1 and HMGB1 2, which may ameliorate Alzheimer's disease. NVP-BAG956 (NVP-BAG956)

Symetine dihydrochloride (L 16726 dihydrochloride) is the bis-hydrochloride form of Symetine. It exhibits antiprotozoal activity against Entamoeba histolytica and can ameliorate amoebic liver abscesses in guinea pigs.

Pronuciferine ameliorate the glucose and lipid metabolism in insulin-resistant 3T3-L1 adipocytes.

AVE-9488 is a novel endothelial NO synthase (eNOS) enhancer that upregulates eNOS expression, induces NO production, and may ameliorate portal hypertension.

7-(4-Hydroxyphenyl)-1-phenyl-4-hepten-3-one as a beneficial compound to ameliorate the deleterious effects of Aβ on dendrite integrity and cell survival, and may provide new insights on drug discovery of Alzheimer's disease (AD).

Bay 60-7550 is a selective and potent PDE2 inhibitor (Ki: 3.8 nM) that exerts positive inotropic effects on rat heart by increasing PKA-mediated phosphorylation and can be used to ameliorate cognitive impairments and memory disorders.

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.

NS-3-008 hydrochloride (NS-3-008 HCl) is a transcriptional G0 G1 switch 2 (G0s2) inhibitor( IC50 of 2.25 μM).

The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein.

O-GlcNAcase-IN-2 (compound 81) is an orally active, brain-penetrant inhibitor of O-GlcNAcase, demonstrating an IC50 value of 4.93 nM. It has shown potential in elevating protein O-GlcNAcylation levels and promoting phosphorylation of tau (p-Ser199, p-Thr205, p-Ser396) in an OA-impacted SH-SY5Y cell model. Additionally, O-GlcNAcase-IN-2 has been observed to ameliorate cognitive deficits in APP PS1 mice, suggesting its potential utility in combating Alzheimer's disease (AD).

Neoechinulin A has anti-inflammatory effect against LPS-stimulated RAW264.7 macrophages through inhibition of the NF-κB and p38 MAPK pathways, it may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regu

CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1].

RO5461111, a highly specific and orally active Cathepsin S antagonist, exhibits potent inhibitory effects with IC50 values of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. It effectively suppresses the activation of antigen-specific T cells and B cells, and can ameliorate pulmonary inflammation and lupus nephritis.

ML-193 (CID 1261822) is a potent and selective GPR55 antagonist (IC50: 221 nM) with over 27-fold selectivity for GPR55 over GPR35, CB1, and CB2. It can ameliorate motor and sensorimotor deficits in Parkinson's disease (PD) rats.

Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.

Kansuiphorin C (KPC) is a natural product with a number of bioactivity. KPC could ameliorate malignant ascites by modulating gut microbiota mainly containing the increase of Lactobacillus and the decrease of Helicobacter and related carbohydrate and amino acid metabolism.

Exendin (5-39) is a potent antagonist of the glucagon-like peptide 1 (GLP-1) receptor that can ameliorate memory impairment in rats treated with β-amyloid protein.