immunosuppressive effects

Isoflupredone (Isoflupredonum) is a synthetic corticosteroid that acts in vivo by binding to glucocorticoid and corticosteroid receptors in animals (such as horses) to inhibit inflammatory cells and inhibit the expression of inflammatory mediators. Isoflupredone has anti-inflammatory and immunosuppressive effects and can be used to treat a variety of musculoskeletal, allergic and systemic inflammatory diseases.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

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.

Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium (Miochrysin) is a potent and selective inhibitor of oncogenic PKC-ι signaling. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium exhibits potent anti-tumor activity.

CD73-IN-8, a potent CD73 inhibitor, prevents the catalytic activity of CD73, an enzyme responsible for converting extracellular 5'-phosphate adenosine (5'-AMP) to adenosine. Adenosine, once produced, can induce immunosuppressive effects and facilitate tumor proliferation and/or metastasis. Therefore, CD73-IN-8 holds promise in the development of therapeutic interventions for tumor-related diseases[1].

CD73-IN-7 is a potent CD73 inhibitor used for preparing medications for tumor-related diseases. CD73 catalyzes the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), inducing immunosuppressive effects and promoting tumor proliferation and or metastasis [1].

1. Acetylcorynoline (O-Acetylcorynoline) has antifungal、anti-inflammatory activity. 2. Acetylcorynoline may be one of the potent immunosuppressive agents through the blockage of dendritic cells maturation and function. 3. Acetylcorynoline is potential as a possible antiparkinsonian drug. (1) Significantly decreases dopaminergic neuron degeneration induced by 6-hydroxydopamine in BZ555 strain; (2) Prevents α-synuclein aggregation; (3) Restores food-sensing behavior, and dopamine levels; (4) Prolongs life-span in 6-hydroxydopamine-treated N2 strain. 4. Acetylcorynoline may exert its effects by decreasing egl-1 expression to suppress apoptosis pathways and by increasing rpn5 expression to enhance the activity of proteasomes.

Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm

Trinactin is a nonactin homolog that has Immunosuppressive effects.

CD73-IN-9, a potent CD73 inhibitor, is used in preparing medication for tumor-related diseases. CD73 catalyzes the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), which can induce immunosuppressive effects and promote tumor proliferation and or metastasis [1].

NFAT inhibitor. Inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). Also attenuates NO production and Nos2 mRNA expression in LPS-stimulated BMDMs. Improves symptoms in a mouse

Withaphysalin R (compound 5), a withanolide derived from the Solanaceae family, possesses an ergosterol-based steroid ester structure. This compound exhibits notable activities such as cytotoxic, immunosuppressive, antitumor, anti-inflammatory, anticonvulsive, and antioxidant effects [1].

Paramethasone Acetate is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive effects that can be used in the treatment of systemic lupus erythematosus.

Armepavine hydrochloride, (+/-)- is a compound which has been shown to exert immunosuppressive effects on T lymphocytes and on lupus nephritic mice.

Physalin H is an Hh signaling inhibitor blocks GLI1-DNA-complex formation, it also strong quinone reductase induction activity with IR (Induction ratio, QR induction activity) value of 3.74±0.02. Physalin H shows immunosuppressive effects on T cells both

Ptaquiloside shows genotoxicity, it also has carcinogenic effects. Ptaquiloside has immunosuppressive effects, it reduces NK cell activities by enhancing metallothionein expression, which is prevented by selenium.

1. (+)-(3R,8S)-Falcarindiol is a potential new anticancer agent that exerts its activity through inducing ER stress and apoptosis. 2. Falcarindiol induces immunosuppressive effects in vitro and in vivo and might be a novel therapy for autoimmune or allergic diseases. 3. Falcarindiol has protective effect against CCl(4) toxicity , in part, be explained by anti-lipid peroxidation activity associated with the induction of the GSTs including GSTA4.

Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects, including the induction of apoptosis in activated lymph node cells through caspase-3 and PARP activation [1].

Mycophenolic acid sodium is a potent uncompetitive inhibitor of inosine monophosphate dehydrogenase (IMPDH) with an EC50 of 0.24 μM, exhibiting broad antiviral activity against RNA viruses, including influenza, along with immunosuppressive properties and antiangiogenic and antitumor effects [1][2].

Hymenistatin I, a cyclic octapeptide [c-(-Pro-Pro-Tyr-Val-Pro-Leu-Ile-Ile-Ile-)], exhibits immunosuppressive effects on both humoral and cellular immune responses [1].

MP07-66 is a novel FTY720-analog devoid of immunosuppressive effects leads to the reactivation of PP2A, which in turn triggers apoptosis of CLL cells.

Bapotulimab (BAY-1905254) is a fully human IgG2 antibody targeting the immunoglobulin-like domain-containing receptor 2 (ILDR2), and it exhibits antitumor and immunosuppressive effects [1].

EVT801 is an orally active, selective VEGFR-3 inhibitor (IC 50 = 11 nM) with demonstrated antitumor properties. It effectively suppresses VEGF-C-induced human endothelial cell proliferation and tumor (lymphatic) angiogenesis in mouse models. Moreover, EVT801 reduces tumor hypoxia and the production of immunosuppressive cytokines (CCL4, CCL5) and myeloid-derived suppressor cells (MDSC), enhancing the efficacy of immune checkpoint therapy (ICT). This synergy results in improved ICT response rates and more potent anticancer effects in cancer mouse models.

J22352, a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM, enhances anticancer effects in glioblastoma by promoting HDAC6 degradation. It does so by inhibiting autophagy and stimulating the antitumor immune response, further restoring host antitumor activity through the reduction of PD-L1's immunosuppressive activity.

Alpha-Cobratoxin, a neurotoxin isolated from Thai cobra venom, displays neuromodulatory, antiviral, and analgesic activities, as well as potent immunosuppressive effects in the treatment of acute and chronic multiple sclerosis. It is currently under investigation for its potential application in adrenomyeloneuropathy [1].

M1069 is a selective, orally active A2A/A2B diadenosine receptor antagonist that is more than 100-fold more selective than subtypes A1 and A3. M1069 antagonizes the immunosuppressive mechanisms induced by adenosine and exhibits antitumor effects.

ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.