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(R)-Fangchinoline Sale

(Synonyms: 汉防己乙素,Thalrugosine; Thaligine) 目录号 : GC64179

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

(R)-Fangchinoline Chemical Structure

Cas No.:33889-68-8

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产品描述

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

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 ?M. 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].

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].

[1] Wan Z, et al. PLoS One. 2012, 7(6):e39225. [2] Zheng-Hai Tang, et al. RSC Adv. 2017,7:42597-42605. [3] Tian F, et al. Int J Oncol. 2015, 46(6):2355-63.

Chemical Properties

Cas No. 33889-68-8 SDF Download SDF
别名 汉防己乙素,Thalrugosine; Thaligine
分子式 C37H40N2O6 分子量 608.72
溶解度 DMSO : 50 mg/mL (82.14 mM; Need ultrasonic) 储存条件 4°C, protect from light
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1 mg 5 mg 10 mg
1 mM 1.6428 mL 8.214 mL 16.4279 mL
5 mM 0.3286 mL 1.6428 mL 3.2856 mL
10 mM 0.1643 mL 0.8214 mL 1.6428 mL
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Research Update

[Study on the interaction between fangchinoline and bovine serum albumin]

Guang Pu Xue Yu Guang Pu Fen Xi 2007 Dec;27(12):2498-501.PMID:18330294doi

The binding reaction of fangchinoline with bovine serum albumin was studied at different temperatures by fluorescence quenching spectra, synchronous fluorescence spectra and ultra-violet spectra. It was shown that fangchinoline has a strong ability of quenching the fluorescence of BSA. The Stern-Volmer curve of the fluorescence quenching of BSA by fangchinoline indicated that the quenching mechanism of fangchinoline to BSA was a static quenching. According to the Förster theory of non-radiation energy transfer, the binding distances (R) at different temperature were 2.51 nm (27 degrees C), 2.72 nm (37 degrees C) and 2.89 nm (47 degrees C), respectively, while the binding constants (KA) were 1.05 x 10(5) L x mol(-1) (27 degrees C), 3.31x 10(5) L x mol(-1) (37 degrees C), and 7.24 x 10(5) L x mol(-1) (47 degrees C), respectively. The thermodynamic parameters showed that the interaction of fangchinoline and BSA was mainly driven by hydrophobic force. Synchronous spectrum was used to investigate the conformational changes of BSA.

Ionic liquid-based ultrasound-assisted extraction of fangchinoline and tetrandrine from Stephaniae tetrandrae

J Sep Sci 2009 Oct;32(20):3550-4.PMID:19764054DOI:10.1002/jssc.200900413.

An ionic liquid-based ultrasound-assisted extraction method has been developed for the effective extraction of fangchinoline and tetrandrine from Stephaniae tetrandrae. The effects of some ultrasound-assisted extraction parameters including the concentration of [BMIM][BF(4)], pH, ultrasonic power and time were investigated to optimize the ultrasound-assisted extraction conditions. Compared to the regular ultrasound-assisted extraction and traditional refluent extraction, the proposed [BMIM][BF(4)]-based ultrasound-assisted extraction offered shorter extraction times (from 6 h to 40 min) and remarkable higher efficiencies (approximately 30% improved), which supported the suitability of the proposed approach. In addition, the proposed approach was confirmed by the good correlation coefficient (R(2)), recovery and reproducibility (RSD, n = 5), which were in the range of 0.9992-0.9995, 85.5-101.1%, and 1.87-4.33%, respectively.

Simultaneous Determination of Fangchinoline and Tetrandrine in Qi-Fang-Xi-Bi-Granules by RP-HPLC

J Chromatogr Sci 2015 Sep;53(8):1328-32.PMID:25754692DOI:10.1093/chromsci/bmv016.

Knee Osteoarthritis is one of the most common diseases of elder worldwide. Qi-Fang-Xi-Bi-Granules (QFXBG) is a new Chinese medicine granules employed for the treatment of Knee Osteoarthritis. Fangchinoline (FAN) and tetrandrine (TET) are used as targets of quality control of QFXBG. A simple, practical high-performance liquid chromatographic method was developed for the simultaneous quantitation of FAN and TET in Stephaniae tetrandrae radix and QFXBG. The analysis was performed on a Athena C18 column (250 × 4.6 mm, 5 µm) with mobile phase of methanol-water (65 : 35, v/v, pH 3.0, adjusted by glacial acetic acid) containing 1.0 g/L sodium 1-octanesulfonate. This method was validated in terms of linearity, precision, accuracy and recovery. Results showed that this method had good linearity with R(2) at >0.999. The limit of detection and limit of quantification for FAN were 0.13 and 0.35 mg/L, while for TET were 0.28 and 0.76 mg/L, respectively. The relative standard deviations of precision were 0.1-1.3% for intraday and 0.5-2.4% for interday. The recovery was 94.56-98.81% of FAN and 94.07-99.12% of TET, respectively. The chromatographic analytical time was 14 min. This method was successfully applied for the quantitative analysis of FAN and TET in Stephaniae tetrandrae radix and QFXBG, so that it could be extended to quality control of QFXGB in commercial.

Determination of tetrandrine and fangchinoline in plasma samples using hollow fiber liquid-phase microextraction combined with high-performance liquid chromatography

J Chromatogr A 2007 Sep 14;1164(1-2):56-64.PMID:17675049DOI:10.1016/j.chroma.2007.07.019.

Tetrandrine (TET) and fangchinoline (FAN) are basic and highly hydrophobic drugs with logP>5.7. In this work, a simple, inexpensive and efficient liquid-phase microextraction (LPME) technology combined with high-performance liquid chromatography (HPLC) was developed for the simultaneous analysis of tetrandrine and fangchinoline in plasma samples. Tetrahydropalmatine was used as internal standard. Several parameters influencing the efficiency of LPME were investigated and optimized including organic solvent, stirring rate, extraction time, salt concentration, organic modifier and pH. Under the optimal conditions, extraction recoveries from plasma samples were 46% for tetrandrine and 50% for fangchinoline, corresponding to the drugs enriched by a factor of 23 and 25 by LPME, respectively. Excellent sample clean-up was observed and good linearities with correlation coefficients (R) of 0.9979 (FAN) and 0.9995 (TET) were obtained in the range of 15-1000 ngmL(-1). The limits of detection (LOD, S/N=3) were 3.0 ngmL(-1) for FAN and 2.0 ngmL(-1) for TET.

Protective effects of fangchinoline and tetrandrine on hydrogen peroxide-induced oxidative neuronal cell damage in cultured rat cerebellar granule cells

Planta Med 2003 Jun;69(6):506-12.PMID:12865967DOI:10.1055/s-2003-40647.

The present study was performed to examine the neuroprotective effects of fangchinoline (FAN) and tetrandrine (TET), bis-benzylisoquinoline alkaloids, which exhibit the characteristics of Ca 2+ channel blockers, on H2O2 -induced neurotoxicity using cultured rat cerebellar granule neurons. H2O2 produced a concentration-dependent reduction of cell viability, which was blocked by (5 R,10 S)-(+)-5-methyl-10,11-dihydro-5 H-dibenzo[ a,d]cyclohepten-5,10-imine (MK-801), an N-methyl- D-aspartate (NMDA) receptor antagonist, verapamil, an L-type Ca 2+ channel blocker, and NG-nitro- L-arginine methyl ester (L-NAME), a nitric oxide synthase (NOS) inhibitor. Pretreatment with FAN and TET over a concentration range of 0.1 to 10 microM significantly decreased the H2O2 -induced neuronal cell death as assessed by a trypan blue exclusion test, a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) assay and the number of apoptotic nuclei. In addition, FAN and TET inhibited the H2O2 -induced elevation of glutamate release into the medium, elevation of the cytosolic free Ca 2+ concentration ([Ca 2+] c ), and generation of reactive oxygen species (ROS). These results suggest that FAN and TET may mitigate the harmful effects of H2O2 -induced neuronal cell death by interfering with the increase of [Ca 2+] c, and then by inhibiting glutamate release and generation of ROS. Abbreviations. AP5:D(-)-2-amino-5-phosphonopentanoic acid DMSO:dimethyl sulfoxide FAN:fangchinoline H 2 DCF-DA:2',7'-dichlorodihydrofluorescin diacetate MK-801:(5 R,10 S)-(+)-5-methyl-10,11-dihydro-5 H-dibenzo[ a,d]cyclohepten-5,20-imine MTT:3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide L-NAME: NG-Nitro- L-arginine methyl ester NMDA: N-methyl- D-aspartate TET:tetrandrine