1. Apoptosis
  2. Apoptosis
  3. Conophylline

Conophylline is a vinca alkaloid extracted from leaves of a tropical plant Ervatamia microphylla. Conophylline is a differentiation inducer of for pancreatic cells. Conophylline suppresses HSC and induces apoptosis.

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Conophylline

Conophylline Chemical Structure

CAS No. : 142741-24-0

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Based on 1 publication(s) in Google Scholar

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Description

Conophylline is a vinca alkaloid extracted from leaves of a tropical plant Ervatamia microphylla. Conophylline is a differentiation inducer of for pancreatic cells. Conophylline suppresses HSC and induces apoptosis[1][2].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.17 μM
Compound: 65
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth
[PMID: 36170798]
A549 IC50
0.21 μM
Compound: Conophylline
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 23944995]
A549 IC50
3.2 μM
Compound: 5
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 30869890]
HCT-116 IC50
0.8 μM
Compound: 5
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
[PMID: 30869890]
HL-60 IC50
0.17 μM
Compound: 65
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth
[PMID: 36170798]
HL-60 IC50
0.17 μM
Compound: Conophylline
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 23944995]
HT-29 IC50
3 μM
Compound: 5
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 30869890]
KB/VJ300 IC50
4.9 μM
Compound: 5
Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay
Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay
[PMID: 30869890]
KB/VJ300 IC50
> 10 μM
Compound: 5
Cytotoxicity against human KB/VJ300 cells after 72 hrs by MTT assay
Cytotoxicity against human KB/VJ300 cells after 72 hrs by MTT assay
[PMID: 30869890]
LNCaP IC50
> 10 μM
Compound: 5
Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay
Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay
[PMID: 30869890]
MCF7 IC50
0.17 μM
Compound: 65
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
[PMID: 36170798]
MCF7 IC50
1.02 μM
Compound: Conophylline
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 23944995]
MCF7 IC50
2.1 μM
Compound: 5
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 30869890]
MDA-MB-231 IC50
1.6 μM
Compound: 5
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 30869890]
PC-3 IC50
0.3 μM
Compound: 5
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
[PMID: 30869890]
SMMC-7721 IC50
0.17 μM
Compound: 65
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth
[PMID: 36170798]
SW480 IC50
0.17 μM
Compound: 65
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth
[PMID: 36170798]
SW480 IC50
1.49 μM
Compound: Conophylline
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
[PMID: 23944995]
In Vitro

Conophylline (100 ng/ml; 48 hours) reproduces differentiationinducing activity but not apoptosis-inducing activity of activin[1].
? Conophylline (100 ng/ml; 72 hours) exhibits the differentiation-inducing activity in AR42J cells and converts these cells to endocrine cells[1].
? Conophylline increases the expression of neurogenin-3 by activating p38 mitogen-activated protein kinase to induce differentiation of AR42J cells[1].
? Conophylline reduces the expression of α-SMA and collagen-1 in rat HSC and Lx-2 cells[2].
? Conophylline inhibits DNA synthesis induced by serum[2].
? Conophylline also promots activation of caspase-3 and induces apoptosis in Lx-2 Cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: Lx-2 Cells
Concentration: 12 hours
Incubation Time: 0.1 μg/ml
Result: Induced apoptosis

Western Blot Analysis[2]

Cell Line: Lx-2 cells
Concentration: 0.1 μg/ml
Incubation Time: 15 minutes, 30 minutes, 60 minutes, 120 minutes
Result: Increased phospho-JNK.
In Vivo

Conophylline (0.9 mg/kg; p.o.; daily; for 12 weeks) attenuates formation of the liver fibrosis induced by TAA in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (70-80 g)[2]
Dosage: 0.9 mg/kg
Administration: Oral administration; daily; for 12 weeks
Result: Attenuated formation of the liver fibrosis induced by TAA.
Molecular Weight

794.89

Formula

C44H50N4O10

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC[C@]1(C2)[C@@]3([H])[C@](C4=CC(O)=C5OC)(CCN3[C@@](C(C=C([C@]6(CCN7C[C@]8([H])[C@@]9([H])O8)[C@]7([H])[C@@]9(C%10)CC)C(NC6=C%10C(OC)=O)=C%11)=C%11O%12)([H])[C@@]%12([H])[C@H]1O)C(NC4=C5OC)=C2C(OC)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥98.0%

References
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Conophylline
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