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  1. General Info
  2. Source Info
  3. Effects Info
  4. Reference
Phytochemical Details
01. General Information
Name Berberine
PubChem CID 2353
Molecular Weight 336.4g/mol
Synonyms

Berberine, Umbellatine

Formula C₂₀H₁₈NO₄+
SMILES COC1=C(C2=C[N+]3=C(C=C2C=C1)C4=CC5=C(C=C4CC3)OCO5)OC
InChI 1S/C20H18NO4/c1-22-17-4-3-12-7-16-14-9-19-18(24-11-25-19)8-13(14)5-6-21(16)10-15(12)20(17)23-2/h3-4,7-10H,5-6,11H2,1-2H3/q+1
InChIKey YBHILYKTIRIUTE-UHFFFAOYSA-N
CAS Number 2086-83-1
ChEMBL ID CHEMBL295124
ChEBI ID CHEBI:16118
Herb ID HBIN017893
Drug Bank ID DB04115
KEGG ID C00757
Toxicity Organism Test Type Route(Dose)
rat LD50 intraperitoneal(165 mg/kg)
mouse LD50 intraperitoneal(254 mg/kg)
rat LD50 oral(322 mg/kg)
Structure 2D-img
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2D MOL 3D MOL
02. Source Information of Phytochemical
(1) Lilium longiflorum Cold
Chineses Pinyin BaiHe
Use Part Bulb
Habitat China
Flavor Sweet
Meridian Tropism Heart, Lung
Species
>Kingdom: Viridiplantae
 -->Phylum: Streptophyta
  -->Class: Equisetopsida
   -->Order: Liliales
    -->Family: Liliaceae
     -->Genus: Lilium
      -->Species: Lilium longiflorum
(2) Coptis chinensis Cold
Chineses Pinyin HuangLian
Use Part Rhizome
Habitat SiChuan, YunNan, HuBei
Flavor Bitter
Meridian Tropism Heart; Spleen; Stomach; Liver; Gallbladder; Large Intestine
Species
>Kingdom: Viridiplantae
 -->Phylum: Streptophyta
  -->Class: Equisetopsida
   -->Order: Ranunculales
    -->Family: Ranunculaceae
     -->Genus: Coptis
      -->Species: Coptis chinensis
03. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Drug(s) whose efficacy can be enhanced by this phytochemical
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Combination Pair ID: 601
Pair Name Berberine, Erlotinib
Partner Name Erlotinib
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Down-regulation Expression CCND1 hsa595
Down-regulation Phosphorylation EGFR hsa1956
Down-regulation Phosphorylation MAPK1 hsa5594
In Vitro Model A-431 Skin squamous cell carcinoma Homo sapiens (Human) CVCL_0037
NCI-H1666 Minimally invasive lung adenocarcinoma Homo sapiens (Human) CVCL_1485
NCI-H441 Lung papillary adenocarcinoma Homo sapiens (Human) CVCL_1561
NCI-H1781 Minimally invasive lung adenocarcinoma Homo sapiens (Human) CVCL_1494
In Vivo Model A431 cells (5×10⁶) were suspended in 200 µL of normal saline and subcutaneously implanted into 6-7-week-old male athymic nude mice.
Result Our data supported use of BBR in combination with erlotinib as a novel strategy for treatment of patients with EGFR positive tumors.
Combination Pair ID: 602
Pair Name Berberine, Cisplatin
Partner Name Cisplatin
Disease Info [ICD-11: 2B51] Osteosarcoma Investigative
Biological Phenomena Induction-->Blockade of cell cycle in G0/G1 phase
Gene Regulation Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Down-regulation Expression CCND1 hsa595
Down-regulation Expression CDK4 hsa1019
Down-regulation Phosphorylation MAPK1 hsa5594
Down-regulation Phosphorylation MAPK14 hsa1432
Down-regulation Phosphorylation MAPK8 hsa5599
Down-regulation Expression MMP2 hsa4313
Down-regulation Expression MMP9 hsa4318
In Vitro Model MG-63 Osteosarcoma Homo sapiens (Human) CVCL_0426
Result Berberine and Cisplatin Exhibit Synergistic Anticancer Effects on Osteosarcoma MG-63 Cells by Inhibiting the MAPK Pathway
Combination Pair ID: 756
Pair Name Berberine, Niraparib
Partner Name Niraparib
Disease Info [ICD-11: 2C73] Ovarian cancer Investigative
Biological Phenomena Induction-->DNA damage
Gene Regulation Up-regulation Phosphorylation H2AX hsa3014
Down-regulation Expression NR1H4 KEGG ID N.A.
Down-regulation Expression RAD51 hsa5888
In Vitro Model A2780 Ovarian endometrioid adenocarcinoma Homo sapiens (Human) CVCL_0134
HO-8910 Human papillomavirus-related cervical adenocarcinoma Homo sapiens (Human) CVCL_6868
In Vivo Model The animals were subcutaneously inoculated with 1 × 106 A2780 cells (suspended in 100 μl PBS) and six days later the tumor-bearing mice were randomly divided into four groups and were then treated daily by oral gavage with vehicle (sodium carboxymethycellulose, SCMC), berberine (200 mg/kg bodyweight), niraparib (40 mg/kg bodyweight) and berberine (200 mg/kg) in combination with niraparib (40 mg/kg), respectively, for 15 days.
Result The results indicate that by inducing oxidative DNA damage and downregulating HRR in cancer cells berberine is able to further sensitize cancer cells to PARP inhibition. These results demonstrate a potential therapeutic value of combined application of berberine and PARP inhibitors in ovarian cancer treatment.
Combination Pair ID: 945
Pair Name Berberine, Letrozole
Partner Name Letrozole
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Gene Regulation Up-regulation Expression ROS1 hsa6098
In Vitro Model MDA-MB-231 Breast adenocarcinoma Homo sapiens (Human) CVCL_0062
Result Our results suggest that concomitant treatment of LTZ-BBR increases the efficacy of chemotherapeutic agents with low BBR concentrations, especially in chemo-resistant malignancies.
Drug(s) whose resistance can be reversed by this phytochemical
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Combination Pair ID: 887
Pair Name Berberine, Lapatinib
Partner Name Lapatinib
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->ROS generation
Gene Regulation Down-regulation Expression MYC hsa4609
Down-regulation Expression NFE2L2 hsa4780
Up-regulation Expression ROS1 hsa6098
In Vitro Model BT-474LabR Lapatinib-resistant breast adenocarcinoma Homo sapiens (Human) N.A.
AU-565LapR Lapatinib-resistant breast adenocarcinoma Homo sapiens (Human) N.A.
Result Berberine reverses Lapatinib resistance of HER2-positive breast cancer cells by increasing the level of ROS
04. Reference
No. Title Href
1 Antitumor effects of erlotinib in combination with berberine in A431 cells. BMC Pharmacol Toxicol. 2023 May 11;24(1):29. doi: 10.1186/s40360-023-00661-2. Click
2 Berberine and Cisplatin Exhibit Synergistic Anticancer Effects on Osteosarcoma MG-63 Cells by Inhibiting the MAPK Pathway. Molecules. 2021 Mar 17;26(6):1666. doi: 10.3390/molecules26061666. Click
3 Berberine induces oxidative DNA damage and impairs homologous recombination repair in ovarian cancer cells to confer increased sensitivity to PARP inhibition. Cell Death Dis. 2017;8(10):e3070. Published 2017 Oct 5. doi:10.1038/cddis.2017.471 Click
4 Synergistic Combination of Letrozole and Berberine in Ascorbic Acid-Stabilized AuNPs: A Promising Solution for Breast Cancer. Pharmaceuticals (Basel). 2023 Aug 3;16(8):1099. doi: 10.3390/ph16081099. Click
5 Berberine reverses Lapatinib resistance of HER2-positive breast cancer cells by increasing the level of ROS. Cancer Biol Ther. 2016;17(9):925-934. doi:10.1080/15384047.2016.1210728 Click
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