arthritic

Clozic (ICI 55897) exhibits reversible anti-proliferative effects and can be used in studies about serving as a potential anti-arthritic agent.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).

Resolvin D3 (RvD3) is a dysregulated mediator originating from docosahexaenoic acid (DHA). It plays a crucial role in reducing arthritic inflammation.

Clematichinenoside AR exerts anti-inflammatory and immunosuppressive properties, it has anti-arthritic effects on PI3K/Akt signaling pathway and TNF-α± associated with collagen-induced arthritis.

Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity.1 It inhibits prostaglandin synthetase (IC50 = 424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.2 |1. Lema, W.J., Blankenship, J.W., and Malone, M.H. Prostaglandin synthetase inhibition by alkaloids of Heimia salicifolia. J. Ethnopharmacol. 15(2), 161-167 (1986).|2. Kosersky, D.S., Brown, J.K., and Malone, M.H. Effects of cryogenine on adjuvant-induced arthritis and serum turbidity in rats. J. Pharm. Sci. 62(12), 1965-1971 (1973).

RC-3095 acetate is an antagonist of bombesin/gastrin-releasing peptide receptor (GRPR). It exerts protective effects by reducing gastric oxidative injury in the arthritic mice.

Luteolin-7-rutinoside has both antifungal activities and anti-arthritic, can result in a combination therapy for the treatment of fungal arthritis due to C. albicans infection.

Tiaprofenic acid (Acido tiaprofenico) is a non-steroidal anti-inflammatory drug used to treat pain, especially arthritic pain.

1. Kirenol (Kirel) has anti-oxidant, anti-inflammatory, anti-allergic, and anti-arthritic activities. 2. Kirenol is effective against gram-positive bacteria. 3. Kirenol possesses antitumor action on human chronic myeloid leukemia K562 cells in vitro. 4. Kirenol is capable of promoting osteoblast differentiation in MC3T3-E1 cells through activation of the BMP and Wnt/β-catenin signaling pathways. 5. Kirenol treatment reduces pro-inflammatory cytokine secretion, increases anti-inflammatory cytokine production, inhibits cell proliferation and induces apoptosis of CII-specific lymphocytes in vitro.

BMS-751324, a p38α MAPK inhibitor, features a carbamyl-methyl linkage precursor with esters and phosphate functional groups from hydroxyphenylacetic acid (HPA). It effectively reduces foot swelling and suppresses LPS-induced TNFα production in an arthritic rat model.

Lonicerin has antioxidant, anti-arthritic and antifungal activities, it can result in a combination therapy for the treatment of fungal arthritis due to C. albicans infection.

3'-Sialyllactose (3'-SL), a prebiotic with anti-inflammatory and anti-arthritic properties, plays a role in maintaining immune homeostasis. As a common carbohydrate with the lowest toxicity level, it is utilized in inflammation research.

PDE4-IN-6 is a safe, potent and moderately selective inhibitor of PDE4, acting on PDE4B (IC50: 0.125 μM) and PDE4D (IC50: 0.43 μM). PDE4-IN-6 is able to down-regulate TNF-α and IL-6 expression levels, exhibits anti-inflammatory and anti-arthritic effects, and has potent immunomodulatory activity. PDE4-IN-6 has potential for anti-rheumatoid arthritis studies.

Aurantiamide acetate (Asperglaucide) was isolated from the fermentation broth of Aspergillus penicilloides for the first time. Aurantiamide acetate is a selective and orally active cathepsin inhibitor. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases[1][2].

beta-Amyrin acetate inhibits HMG-CoA Reductase (HMGCR) and sEH activity with IC50 of 3.4 μM. beta-Amyrin acetate has anti-inflammatory, antifungal, antioxidant, and anti-hyperlipidemic activities.

Suprofen (Suprol) is an IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.

1. Pristimerin (Celastrol methyl ester) has anticancer activity , treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. 2. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS/IKK/NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.

IRAK4-IN-18 is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4) (IC50: 15 nM). IRAK4-IN-18 inhibits LPS-induced IL23 production in THP and DC cells and blocks the development of arthritis in rats, a model of arthritis. IRAK4-IN-18 can be used to study arthritic diseases.

Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic transmission[2]. Rp-cAMPS (10 μM, 15 min) decreases the monosynaptic EPSCs evoked at the PB-CeLC and BLA-CeLC synapses in slices from arthritic rats but not in control neurons from normal animals. The inhibitory effect of Rp-cAMPS is significant compared to predrug (ACSF) control values obtained in the same neurons[2]. [1]. R J de Wit, et al. Inhibitory action of certain cyclophosphate derivatives of cAMP on cAMP-dependent protein kinases. Eur J Biochem. 1984 Jul 16;142(2):255-60. [2]. Rothermel JD, et al. A mechanistic and kinetic analysis of the interactions of the diastereoisomers of adenosine 3’,5’-(cyclic)phosphorothioate with purified cyclic AMP-dependent protein kinase. Biochem J. 1988 May 1;251(3):757-62.[3]. Fu Y, et al. PKA and ERK, but not PKC, in the amygdala contribute to pain-related synaptic plasticity and behavior. Mol Pain. 2008 Jul 16;4:26.[4]. Kuriyama S, et al. Isoproterenol inhibits rod outer segment phagocytosis by both cAMP-dependent and independent pathways. Invest Ophthalmol Vis Sci. 1995 Mar;36(3):730-6.[5]. Dostmann WR, et al. Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3’,5’-cyclic phosphorothioates. J Biol Chem. 1990 Jun 25;265(18):10484-91.[6]. Van Haastert PJ, et al. Competitive cAMP antagonists for cAMP-receptor proteins. J Biol Chem. 1984 Aug 25;259(16):10020-4.

Glaucine has antitussive, antioxidative potential and antiviral activities, it may be an anti-arthritic agent, it can enhance LPS and zymosan-induced IL-10 production. Glaucine can inhibit the migration and invasion of human breast cancer cells by MMP-9 i

IRAK4-IN-19 is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4) (IC50: 4.3 nM).IRAK4-IN-19 inhibits LPS-induced IL23 production in THP and DC cells and suppresses the development of arthritis in arthritis model rats.IRAK4-IN-19 can be used to study arthritic diseases.

AHR-15010 is a novel anti-arthritic agent.

RC-3095, a selective GRPR antagonist, has been shown to have anti-inflammatory properties in different models of inflammation.

RC-3095 TFA (RC-3095 (TFA)) is a bombesin/gastrin-releasing peptide (BN/GRP) antagonist with potential anticancer activity.