Fangchinoline

Fangchinoline, a bisbenzylisoquinoline alkaloid, is a novel HIV-1 inhibitor with pain-relieving, blood pressure-depressing, and antibiotic activities.

Fangchinoline Chemical Structure

Fangchinoline Chemical Structure

CAS No. 33889-68-8

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Biological Activity

Description Fangchinoline, a bisbenzylisoquinoline alkaloid, is a novel HIV-1 inhibitor with pain-relieving, blood pressure-depressing, and antibiotic activities.
Targets
HIV-1 [1]
In vitro
In vitro Fangchinoline (FCL) exhibits antiviral activity against HIV-1 laboratory strains NL4-3, LAI and BaL in MT-4 and PM1 cells with a 50% effective concentration ranging from 0.8 to 1.7 µM. The compound targets a late event in infection cycle. Fangchinoline inhibits HIV-1 replication by interfering with gp160 proteolytic processing[1]. FCL inhibits autophagosomes-lysosomes fusion, decreases the activities of cathepsin B and cathepsin D and affects the cellular acidification. FCL also increases the nuclear translocation of transcription factor EB (TFEB), a master regulator of autophagic and lysosomal genes, and the mRNA expressions of TFEB-targeted genes, such as SQSTM1, MAP1LC3B, and UVRAG. Knockdown of TFEB by using small inference RNA decreases the FCL-induced expression of LC3-II and the formation of GFP-LC3 puncta[2]. Fangchinoline effectively suppresses proliferation and invasion of SGC7901 cell lines, but not MKN45 cell lines by inhibiting the expression of PI3K and its downstream pathway. fangchinoline targets PI3K in tumor cells that express PI3K abundantly and inhibits the growth and invasive ability of the tumor cells[3]. Fangchinoline is also a non-specific calcium antagonist[4].
Cell Research Cell lines MT-4 cells
Concentrations 2.5 μM
Incubation Time 24 h
Method

MT-4 cells are infected with HIV-1 NL4-3 at a high MOI of 1. After incubating for 24 hours, the cells are washed and incubated with 1 µM indinavir (IDV) alone or with 1 µM IDV plus 2.5 µM fangchinoline for an additional 24 hours. Thereafter, MT-4 cells are cultured with an equal number of the C8166 cells in a culture plate in the presence of the same compounds in duplicate. After 24 hours of cocultivation, syncytium formation is examined using light microscopy.

In Vivo
In vivo Fangchinoline attenuates morphine (SC)-induced antinociception in a dose-dependent manner with significant effect at doses of 30 and 60mg/kg body wt. (IP) in the tail-flick test but not the tail-pinch tests, carried out in mice[4].
Animal Research Animal Models ICR male mice
Dosages 5, 30 and 60mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 608.72 Formula

C37H40N2O6

CAS No. 33889-68-8 SDF Download Fangchinoline SDF
Smiles CN1CCC2=CC(=C3C=C2C1CC4=CC=C(C=C4)OC5=C(C=CC(=C5)CC6C7=C(O3)C(=C(C=C7CCN6C)OC)O)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (164.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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