Berberine chloride (NSC 646666)

Catalog No.S2271 Synonyms: Natural Yellow 18 chloride

For research use only.

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

Berberine chloride (NSC 646666) Chemical Structure

CAS No. 633-65-8

Selleck's Berberine chloride (NSC 646666) has been cited by 7 Publications

Purity & Quality Control

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Biological Activity

Description Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Targets
Caspase-3 [1] Caspase-8 [1] PARP [1] cytochrome c [1] cIAP1 [1] Click to View More Targets
In vitro

Compared with regorafenib alone, the combined treatment of Berberine (BBR) and regorafenib significantly inhibits the proliferation of hepatocellular carcinoma (HCC) cells and induces cellular apoptosis.[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MRC5 cells NUPNd41pTnWwY4Tpc44h[XO|YYm= M4jTUWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEVVZiaX6gUXJEPSClZXzsd{BjgSCybHHxeYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuOlgh|ryP NWflWpRyOTd{M{m1PVQ>
MRC5 cells NX\BVZN{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUn1SottOTBizszN M{DpV|U1KGi{cx?= NUHMe3pjUW6qaXLpeIlwdiCxZjDIR21XKHC{b3zp[oVz[XSrb36gbY4hVVKFNTDj[YxteyCjZoTldkA2PCCqcoOgdI9{fC2rbn\lZ5Rqd25iYYSgNVAhfU1iYomgdIxieXWnIHHzd4F6 MojtNVczOzl3OUS=
MRC5 cells NW\hOFJJWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWfvdlVuOTBizszN NG\Q[nYzPCCq M{nZb2lvcGmkaYTpc44hd2ZiSFPNWkBxem:uaX\ldoF1cW:wIHnuJG1TSzViY3XscJMh[W[2ZYKgNlQhcHK|IIDvd5QucW6oZXP0bY9vKGG2IEGwJJVOKGK7IIDsZZF2\SCjc4PhfS=> MmHtNVczOzl3OUS=
Bel7402 cells MWrGeY5kfGmxbjDhd5NigQ>? MlT1NVIhcA>? NITycoFKdmS3Y4Tpc44hd2ZiTFTMVkBxem:2ZXnuJIlvKGi3bXHuJGJmdDd2MEKgZ4VtdHNiYX\0[ZIhOTJiaILzJIJ6KFKWLWDDVkBie3OjeTDy[YxifGm4ZTD0c{Bkd262cn;s MV6xPVA6ODd4Nx?=
HepG2 cells M{[5fWZ2dmO2aX;uJIF{e2G7 MXyxNEB2\y:vTB?= MorRNVIhcA>? MX\JcoR2[3Srb36gc4YhVESOUjDwdo91\WmwIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiMUCgeYcwdUxiYX\0[ZIhOTJiaILzJIJ6KG[ub4egZ5l1d22ndIL5 NVi2[G51OTlyOUC3Olc>
KB cells MkXSR5l1d3SxeHnjbZR6KGG|c3H5 MX63NkBp MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDh[pRmeiB5MjDodpMtKEmFNUC9O{4{OiEQvF2= MVixNVE1OTFyNR?=
HL60 cells NYXoVpZiSXCxcITvd4l{KGG|c3H5 NVrNU2FjPDhiaILz MnnJTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDR6IHjyd{B2e2mwZzDhco5mgGmwIG[tdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDifUBHSUOVIHHuZYx6e2m| M1TJXVIxOjJ5MUS0
A549 cells NYnyOXdyS3m2b4TvfIlkcXS7IHHzd4F6 NVTqco9PS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCkeTDTVmIh[XO|YYmsJGlEPTB;Nj6yO{DPxE1? MUWyNFU6PDh2OB?=
SKOV3 cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= NF;KU3pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCkeTDTVmIh[XO|YYmsJGlEPTB;MU[uOFQh|ryP Mm\aNlA2QTR6NEi=
SK-MEL-2 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= M2rGSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD2yJINmdGy|IHL5JHNTSiCjc4PhfUwhUUN3ME2xN{44PiEQvF2= M3\Ge|IxPTl2OES4
HCT15 cells MlTCR5l1d3SxeHnjbZR6KGG|c3H5 MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFnDOVA:OTZwNUmg{txO NV\SU4JmOjB3OUS4OFg>
CEM cells NEC4SZlEgXSxdH;4bYNqfHliYYPzZZk> NXLXeoZsPDhiaILz M1\xTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNGVSClZXzsd{BmgHC{ZYPzbY5oKGe{ZXXuJIZtfW:{ZYPj[Y51KHC{b4TlbY4h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhS0N3ME2yMlA6KM7:TR?= M4PJTVIyOjl3OEmx
human CEM cells NYnKenR2TnWwY4Tpc44h[XO|YYm= MV63JIRigXN? NI\3fWdCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEAxNjB3IF3PTUBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KDFiTly0MlMhcW6oZXP0[YQhcW5iaIXtZY4hS0WPIHPlcIx{KGW6cILld5NqdmdiZ4Ll[Y4h\my3b4Lld4NmdnRicILveIVqdiCjc4Pld5Nm\CCjczDwNlQh[W62aXflckBxem:mdXP0bY9vKG2nYYP1doVlKDdiZHH5d{Bxd3O2IHnu[oVkfGmxbjDifUBGVEmVQTygSWM2OD1yLkGzJO69VQ>? MUOyNVI6PTh7MR?=
SKN cells NVjId3d7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4fle|czKGh? NGfIXI9Iem:5dHigbY5pcWKrdHnvckBi\2GrboP0JIh2dWGwIGPLUkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTF3Lki4JO69VQ>? MVyyNVQxOTFzNB?=
RKN cells MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MknyOFghcHK| MkfSS5Jwf3SqIHnubIljcXSrb36gZYdicW6|dDDoeY1idiCUS16gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NF01QS54IN88US=> M1;IVlIyPDBzMUG0
G402 cells MorMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPkVWI1QCCqcoO= NWi5Tml5T3Kxd4ToJIlvcGmkaYTpc44h[WejaX7zeEBpfW2jbjDHOFAzKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGdKPTB;MUGuPFch|ryP NUT0e|dFOjF2MEGxNVQ>
A10 cells M2K1OGZ2dmO2aX;uJIF{e2G7 NIrIN2Y{OCEQvF2= M4rVPFI1KGi{cx?= MV;Ec5dvemWpdXzheIlwdiCxZjDTZ4QzKG2UTlGg[ZhxemW|c3nvckBqdiC{YYSgRVExKGOnbHzzJIF1KDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDxeYFvfGm2YYTpeoUhWlRvUFPSJIFv[Wy7c3nz M1\JXFIyPDBzMUG0
A10 cells NGPzcVdHfW6ldHnvckBie3OjeR?= MYmzNEDPxE1? MXeyOEBpenN? NXjvb4U1TG:5bjDy[Yd2dGG2aX;uJI9nKFC{aX2yJI1TVkFiZYjwdoV{e2mxbjDpckBz[XRiQUGwJINmdGy|IHH0JFMxKHWPIHHmeIVzKDJ2IHjyd{BjgSCzdXHueIl1[XSrdnWgVnQuWEOUIHHuZYx6e2m| MXGyNVQxOTFzNB?=
A10 cells MUDGeY5kfGmxbjDhd5NigQ>? NWLDOZdrOzBizszN M4fpbFI1KGi{cx?= M176SmRwf26{ZXf1cIF1cW:wIH;mJGlueGtibWLORUBmgHC{ZYPzbY9vKGmwIILheEBCOTBiY3XscJMh[XRiM{CgeW0h[W[2ZYKgNlQhcHK|IHL5JJF2[W62aYTheIl3\SCUVD3QR3Ih[W6jbInzbZM> M{noN|IyPDBzMUG0
HepG2-A16-CD81 cells Mk\iSpVv[3Srb36gZZN{[Xl? NEXr[IkyOCEQvF2= MmKyUm9XSVKWSWO6JGFvfGmvYXzhdolidCCuaY\ldkB{fGGpZTDhZ5Rqfmm2eTDt[YF{fXKnZDDhd{BiKGe{ZXH0[ZIhfGijbjC1NEUhemWmdXP0bY9vKGmwIGDsZZNud2SrdX2gfY9mdGmrIIPjbIl7d262IHHy[YEhcW5iSHXwS|IuSTF4LVPEPFEh[2WubIOgZZQhOTC3TTDjc41xd3WwZDDjc45k\W62cnH0bY9vNCCmZYTldo1qdmWmIHL5JIludXWwbz3mcJVwemW|Y3XuZ4Uv NYDDeHlbOjJyOU[xNFE>
HepG2-A16-CD81 cells NELLNGxHfW6ldHnvckBie3OjeR?= NHPFfIUyOCEQvF2= NWiwXYl3Vk:YQWLUTXM7KEGwdHntZYxiemmjbDDsbZZmeiC|dHHn[UBi[3Srdnn0fUBu\WG|dYLl[EBieyC{ZXT1Z5Rqd25iaX6gVIxie22xZHn1cUB6d2WuaXmgd4NpcXqxboSgZZJm[SCrbjDI[ZBIOi2DMU[tR2Q5OSClZXzsd{BjgSCrbX31co8u\my3b4Lld4NmdmOnLDDhcoQhdWWmaXHuJJNkcGm8b370JJNqgmViYYSgNVB2VSClb33wc5Vv\CClb37j[Y51emG2aX;uMEBKSzVyPUCuOVQ5KM7:TR?= NGi3[HozOjB7NkGwNS=>
HepG2 cells M{L5NmZ2dmO2aX;uJIF{e2G7 NGO0Z5cyOCEQvF2= NIPvfmo1KGh? NHmzPXJKdmO{ZXHz[UBqdiCDTWDLZYxxcGFicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEincFeyJINmdGy|IHH0JFExKHWPIHHmeIVzKDRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczDy[YxifGm4ZTD0c{B2dnS{ZXH0[YQh[2:wdILvcC=> NF61TVAzOzB3OEGwOy=>
HepG2 cells MYPGeY5kfGmxbjDhd5NigQ>? NUizOlFPOTBizszN MYe0JIg> NH\TXZpKdmO{ZXHz[UBqdiC2b4ThcEBCVVCNYXzwbIEhdGW4ZXygbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiMUCgeW0h[W[2ZYKgOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{KHKnbHH0bZZmKHSxIIXueJJm[XSnZDDjc451em:u M3Lic|I{ODV6MUC3
HepG2 cells MWDGeY5kfGmxbjDhd5NigQ>? MUeyNEDPxE1? MYmyOEBpenN? M{DnUWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhdW:{cHjvcI9ocWOjbDDjbIFv\2W|IHH0JFIxKHWPIHHmeIVzKDJ2IHjyd{B2e2mwZzDIc4VkcHO2IEOzNlU5KHO2YXnubY5oKGK7IH\seY9z\XOlZX7j[UBucWO{b4Pjc5Bq[yCjbnHsfZNqew>? M1HzNlI{OTh{MEi4
HT-29 cells NV[3fFFtS3m2b4TvfIlkcXS7IHHzd4F6 NYfWc|lYPDhiaILz NWruV4U3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF05NjR3IN88US=> MVeyN|E5OjB6OB?=
HepG2 cells Ml;JR5l1d3SxeHnjbZR6KGG|c3H5 MYSyOEBpenN? MlLjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNU4zOiEQvF2= NEDOTG4zOzF6MkC4PC=>
HepG2 cells NWLr[VJOS3m2b4TvfIlkcXS7IHHzd4F6 NY\LVHVTPDhiaILz NEf3PY1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVgvOzJizszN MYOyN|E5OjB6OB?=
In vivo

The combined treatment group with Berberine (BBR) and regorafenib has a dramatic inhibitory effect on the growth of hepatocellular carcinoma (HCC) xenograft tumors in nude mice. The increased apoptosis of xenograft tumors is seen in the combined treatment group.[3]

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: hepatocellular carcinoma (HCC) cells
  • Concentrations: 5, 10, 20, 40, 80, 160, 320, 640 and 1280 μM
  • Incubation Time: 48 h
  • Method:

    HCC cells are seeded into a 96-well plate with 5,000 cells per well. After overnight incubation, HCC cells are treated with the indicated concentrations of regorafenib, Berberine (BBR) or their combination for 24h or 48h. The viability of HCC is examined by MTS Assay and Synergy H1/Epoch microplate reader.The interaction between regorafenib and BBR is quantified by Com-puSyn software. The Cell-LightTM EdU ApolloR567 In Vitro Imaging Kit is used to detect the level of cell proliferation. The Annexin V-FITC/PI Apoptosis Detection Kit and DeadEndTM Fluorometric Tunel System assay are used to measure cellular apoptotic level.

Animal Research:

[3]

  • Animal Models: Male BALB/c nude mice
  • Dosages: 10mg/kg/day
  • Administration: i.p.

    (Data sourced from selleck products)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 371.81
Formula

C20H18NO4.Cl

CAS No. 633-65-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C2=C[N+]3=C(C=C2C=C1)C4=CC5=C(C=C4CC3)OCO5)OC.[Cl-]

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05463003 Not yet recruiting Dietary Supplement: Berberine Pharmacokinetic Study in Healthy Volunteers University Medicine Greifswald July 2022 Not Applicable
NCT03281096 Completed Drug: Berberine hydrochloride|Drug: Placebo Colorectal Adenomas Xijing Hospital of Digestive Diseases August 29 2017 Phase 2|Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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