Structure of Nitidine chloride
CAS No.: 13063-04-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Nitidine Chloride can inhibit proliferation and induce apoptosis via the Akt pathway, derived from genus Zanthoxylum.
Synonyms: Nitidine (chloride); NSC 146397
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CAS No. : | 13063-04-2 |
Formula : | C21H18ClNO4 |
M.W : | 383.82 |
SMILES Code : | C[N+]1=CC2=CC(OC)=C(OC)C=C2C(C=CC3=C4)=C1C3=CC5=C4OCO5.[Cl-] |
Synonyms : |
Nitidine (chloride); NSC 146397
|
MDL No. : | MFCD01659688 |
InChI Key : | QLDAACVSUMUMOR-UHFFFAOYSA-M |
Pubchem ID : | 25659 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HeLa | 1-10 µM | 48 hours | Inhibition of cancer cell proliferation | PMC11929923 |
HCT116 | 1-10 µM | 48 hours | Inhibition of cancer cell proliferation | PMC11929923 |
MDCK-hOCT2/hMATE1 cells | 2.5 μM | 120 minutes | To evaluate the transcellular transport and intracellular accumulation of nitidine chloride in MDCK-hOCT2/hMATE1 cells, results showed that MATE1 plays a minor role in the transcellular transport of nitidine chloride | PMC4959954 |
MDCK-hOCT2 cells | 0.1 –4.0 μM | 2 minutes | To evaluate the uptake kinetics of nitidine chloride in MDCK-hOCT2 cells, results showed that nitidine chloride is a high-affinity substrate of hOCT2 with a Km of 0.97 ± 0.10 μM and Vmax of 288.1 ± 12.8 pmol·mg-1·protein·min-1 | PMC4959954 |
Rat primary-cultured proximal tubular (rPCPT) cells | 0.1 –50 μM | 24 hours | To evaluate the cytotoxicity of nitidine chloride in rat primary-cultured proximal tubular cells and the effect of OCT2 inhibitors, results showed that nitidine chloride concentration-dependently decreased cell viability, and OCT2 inhibitors significantly attenuated its toxicity | PMC4959954 |
RAW 264.7 cells | 1 μM, 10 μM | 24 hours | To evaluate the effect of NitC on LPS-induced inflammatory response. Results showed that NitC significantly inhibited the expression of iNOS, COX2, IL-1β, and NLRP3, indicating its ability to suppress NLRP3 inflammasome activation. | PMC9353946 |
Cardiac fibroblasts (CFs) | 1.25, 2.5, 5, 10, 20, 40 μM | 24 or 48 hours | To evaluate the effect of NC on cardiac fibroblasts, it was found that low concentrations of NC (1.25, 2.5, 5 μM) increased cell viability, while high concentrations (20, 40 μM) decreased cell viability | PMC9388977 |
Li-7 hepatocellular carcinoma cells | 10, 20, 40, 80 μg/mL | 24, 48, 72 hours | Evaluate the cytotoxic effect of TPGS-FA/NC on Li-7 cells, results showed TPGS-FA/NC had better cytotoxicity than 5-Fu and NC | PMC9549606 |
HUVECs | 10 μM | 36 hours | Nitidine chloride showed no significant effect on HUVECs | PMC4310574 |
A549 cells | 10 μM | 36 hours | Nitidine chloride significantly inhibited the dispersion of A549 cancer cells, almost completely abolishing the spheroids' dispersion | PMC4310574 |
A549 | 0.5 μM | 48 hours | NC induced cell swelling and large bubbles emerging from the plasma membrane, showing typical pyroptotic features. | PMC9524076 |
NCI-H1688 | 0.5 μM | 48 hours | NC induced cell swelling and large bubbles emerging from the plasma membrane, showing typical pyroptotic features. | PMC9524076 |
MCF-7 cells | 1 or 2.5 μM | 48 hours | NC inhibited the proliferation of MCF-7 cells in a dose-dependent manner and suppressed their migratory and invasive capabilities | PMC4910241 |
MDA-MB-468 cells | 1 or 2.5 μM | 48 hours | NC inhibited the proliferation of MDA-MB-468 cells in a dose-dependent manner and suppressed their migratory and invasive capabilities | PMC4910241 |
U2OS cells | 8 μM | 48 hours | To evaluate the effect of NC on U2OS cell apoptosis, results showed that NC treatment obviously induced cell apoptosis. | PMC6389778 |
U2OS cells | 4 μM | 72 hours | To evaluate the effect of NC on U2OS cell proliferation, results showed that NC significantly inhibited cell growth in a dose-dependent manner. | PMC6389778 |
MG63 cells | 1.5 μM | 72 hours | To evaluate the effect of NC on MG63 cell proliferation, results showed that NC significantly inhibited cell growth in a dose-dependent manner. | PMC6389778 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Sprague-Dawley rats | Healthy male rats | Intravenous injection | 5 mg/kg | Once daily for 20 consecutive days | To evaluate the nephrotoxicity of nitidine chloride in rats after 20 days of successive intravenous administration, results showed that nitidine chloride caused increased levels of blood urea nitrogen (BUN) and lactate dehydrogenase (LDH), reduced levels of alkaline phosphatase (ALP), and pathological changes in the kidney | PMC4959954 |
C57BL/6 mice | Cardiac hypertrophy model | Intraperitoneal injection | 2.5, 5, 10 mg/kg | Once daily for 4 weeks | To evaluate the effect of NC on cardiac function, it was found that high-dose NC caused cardiac hypertrophy and dysfunction in mice, and cardiac autophagy levels were reduced | PMC9388977 |
BALB/c nude mice | HCC xenograft model | Intraperitoneal injection | 7 mg/kg | Every other day for 15 days | Significantly reduced tumor volume | PMC6737102 |
C57 mice | High-fat diet-induced NAFLD model | Gavage | 8 mg/kg | Once daily for 4 weeks | To evaluate the therapeutic effect of NC-CS/PT-NPs on high-fat diet-induced NAFLD. Results showed that NC-CS/PT-NPs significantly inhibited weight gain, decreased serum AST, ALT and lipid levels, improved liver and intestinal inflammation, and altered the diversity of gut microbiota in mice. | PMC10929648 |
Sprague-Dawley rats | Chronic nephrotoxicity model | Intravenous injection | 2 mg/kg and 6 mg/kg | Once daily for 21 days | To evaluate the nephrotoxicity and underlying mechanisms of nitidine chloride. Results showed accumulation of NC in the inner cortex region of the kidney, leading to renal tubule damage and metabolic disturbances. | PMC11314895 |
BALB/c mice | H1688 or A549 xenograft model | Intraperitoneal injection | 8 mg/kg/week or 16 mg/kg/week | Twice a week for 21 days | NC significantly inhibited tumor growth and induced tumor cell pyroptosis by inhibiting the PI3K/Akt pathway. | PMC9524076 |
Zebrafish | HCC xenograft model | Yolk sac injection | 3.0 ng | Every 24 hours | To validate the inhibitory effect of NC on HCC growth, metastasis, and angiogenesis in vivo, results showed that NC significantly inhibited the growth, metastasis, and angiogenesis of HCC | PMC11796242 |
BALB/c nude mice | Liver cancer xenograft model | Intraperitoneal injection | 10, 5, 2.5 mg/kg | Once daily for 14 days | To evaluate the antitumor effect of nitidine chloride on liver cancer xenograft models, results showed that nitidine chloride significantly inhibited tumor growth | PMC6192772 |
Sprague-Dawley rats | Osteoarthritis model induced by destabilization of the medial meniscus (DMM) surgery | Intra-articular injection | 10 μM | Once a week for 6 weeks | To evaluate the effect of NitC on DMM surgery-induced osteoarthritis model. Results showed that NitC significantly alleviated cartilage erosion, ECM degradation, and subchondral alterations. | PMC9353946 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.03mL 2.61mL 1.30mL |
26.05mL 5.21mL 2.61mL |
Tags: Nitidine | Parasite | Apoptosis | STAT | Topoisomerase | ERK | FAK | p38 MAPK | NF-κB | Extracellular signal regulated kinases | PTK2 protein tyrosine kinase 2 | Zanthoxylum nitidum DC | Nitidine chloride | anticancer | anti-malarial | apoptosis | STAT3 inhibition | MAPK | NF-kB | DNA topoisomerase | ERK | c-Src/FAK | Focal adhesion kinase | Nuclear factor-κB | Nuclear factor-kappaB | 13063-04-2
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