SlideShare a Scribd company logo
1 of 1
Evodiamine isolated from Evodia rutaecarpa as human
topoisomerase catalytic inhibitor
Xiaobei Pan1
, Janet M. Hartley2
, John A. Hartley2
, Kenneth N White1
,
Zhengtao Wang1,3
, S. W. Annie Bligh1
1
Institute for Health Research and Policy, London Metropolitan University, 166-220 Holloway Road, London N7 8DB, UK
2
Cancer Research UK Drug-DNA Interactions Research Group, UCL Cancer Institute, University College London, Paul O’Gorman Building, London, UK
3
The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese
Materia Medica, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Zhangjiang Hi-tech Park, Shanghai 201210, China
Introduction
 Topoisomerase (Fig. 1) is an enzyme, which
can relieve torsional stress in DNA.
 Topoisomerase I and II cleave the single
and double stranded DNA, respectively.
 Since camptothecin was found as a
topoisomerase inhibitor, a number of semi-
synthetic compounds were successfully
developed and used to treat cancer.
 Evodia rutaecarpa (Fig. 2) is a Chinese
herbal medicinal plant that has been used to
treat gastrointestinal disorders, bacterial
infection & inflammation-related disorders.
 Evodiamine isolated from Evodia rutaecarpa
is cytotoxic to several cancer cell lines.
Aims and Objectives
 To isolate quinoline alkaloids from the Evodia and structure elucidation
 To study their potential cytotoxicity, inhibitory activity of topoisomerase I and
II, and catalytic mechanisms.
Methods
 Alkaloids were isolated using reverse-phase HPLC and the structures were
elucidated by 1-D, 2-D NMR spectroscopy and mass spectrometry.
 Their cytotoxicities were determined using MTT-based assay.
 Topoisomerase (Topo) inhibitory activities were studied using Topo I relaxation
and Topo II decatanation assay.
 Comet assay and cell cycle distribution study were carried out by flow
cytometry.
Results and Discussion
 Eight alkaloids were isolated from Evodia, of which evodiamine (Fig. 3)
showed the most potent activity against human leukemia K562 and THP-1
cell lines (IC50 34.35 µM and 90.87 µM respectively.)
 Evodiamine is an inhibitor for both human Topo I and Topo II (Fig. 4).
 It did not induce DNA strand breaks at the cellular level (Fig. 5) and
arrested cell growth at the G2/M phase in the cell cycle.
N
H
N
N
O2
3
5
6
78
9
10
11
12
13
15
16
17
18
19
20
21
H
H3C
Conclusion
Evodiamine was found to be a dual inhibitor for both topoisomerase I and II
with potent cytotoxicity against human leukemia cell lines.
Figure 1. Structure of topoisomerase
Figure 2. Evodia rutaecarpa
Figure 3. Structure of Evodiamine
Figure 4. IC50 of evodiamine against human Topo I
(A, C) using relaxation assay and Topo II (B, D)
using decatanation assayFigure 5. The comet assay did not detect DNA
strand breaks induced by evodiamine
Acknowledgement
X.Pan thanks the Department of Human Science at London Metropolitan University for a student bursary.

More Related Content

What's hot

Effects of hypoxia on human cancer cell line chemosensitivity
Effects of hypoxia on human cancer cell line chemosensitivityEffects of hypoxia on human cancer cell line chemosensitivity
Effects of hypoxia on human cancer cell line chemosensitivityEnrique Moreno Gonzalez
 
Murdannia loriformis(hassk) - Yapakking
Murdannia loriformis(hassk) - Yapakking Murdannia loriformis(hassk) - Yapakking
Murdannia loriformis(hassk) - Yapakking Suphalada C.
 
Protective role of co q10 or l carnitine on the integrity of the myocardium i...
Protective role of co q10 or l carnitine on the integrity of the myocardium i...Protective role of co q10 or l carnitine on the integrity of the myocardium i...
Protective role of co q10 or l carnitine on the integrity of the myocardium i...Prof. Hesham N. Mustafa
 
Environmental exposure and health risks of the insecticide monocrotophos - a ...
Environmental exposure and health risks of the insecticide monocrotophos - a ...Environmental exposure and health risks of the insecticide monocrotophos - a ...
Environmental exposure and health risks of the insecticide monocrotophos - a ...Innspub Net
 
Comprehensive assessment of chamber-specific and transmural heterogeneity in ...
Comprehensive assessment of chamber-specific and transmural heterogeneity in ...Comprehensive assessment of chamber-specific and transmural heterogeneity in ...
Comprehensive assessment of chamber-specific and transmural heterogeneity in ...Justin Doop
 
Non biopsy diagnosis of acute rejection of Renal allograft
  Non biopsy diagnosis of acute rejection of Renal allograft  Non biopsy diagnosis of acute rejection of Renal allograft
Non biopsy diagnosis of acute rejection of Renal allograftBakshish Singh
 
Pharmacogenetics - Pharmacokinetics
Pharmacogenetics  - Pharmacokinetics Pharmacogenetics  - Pharmacokinetics
Pharmacogenetics - Pharmacokinetics Areej Abu Hanieh
 
M. Celeste Simón-Homenaje al bioquímico español Alberto Sols
M. Celeste Simón-Homenaje al bioquímico español Alberto SolsM. Celeste Simón-Homenaje al bioquímico español Alberto Sols
M. Celeste Simón-Homenaje al bioquímico español Alberto SolsFundación Ramón Areces
 
Genetic polymorphism in drug transport
Genetic polymorphism in drug transportGenetic polymorphism in drug transport
Genetic polymorphism in drug transportVineetha Menon
 
In vitro metabolite profiling
In vitro metabolite profilingIn vitro metabolite profiling
In vitro metabolite profilingTejaswini Jadhav
 
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...Mark Lipstein
 
Pharmacology bao jiaolin
Pharmacology bao jiaolinPharmacology bao jiaolin
Pharmacology bao jiaolinJiaolin Bao
 

What's hot (19)

Effects of hypoxia on human cancer cell line chemosensitivity
Effects of hypoxia on human cancer cell line chemosensitivityEffects of hypoxia on human cancer cell line chemosensitivity
Effects of hypoxia on human cancer cell line chemosensitivity
 
Murdannia loriformis(hassk) - Yapakking
Murdannia loriformis(hassk) - Yapakking Murdannia loriformis(hassk) - Yapakking
Murdannia loriformis(hassk) - Yapakking
 
Protective role of co q10 or l carnitine on the integrity of the myocardium i...
Protective role of co q10 or l carnitine on the integrity of the myocardium i...Protective role of co q10 or l carnitine on the integrity of the myocardium i...
Protective role of co q10 or l carnitine on the integrity of the myocardium i...
 
Environmental exposure and health risks of the insecticide monocrotophos - a ...
Environmental exposure and health risks of the insecticide monocrotophos - a ...Environmental exposure and health risks of the insecticide monocrotophos - a ...
Environmental exposure and health risks of the insecticide monocrotophos - a ...
 
Amiji poster
Amiji posterAmiji poster
Amiji poster
 
CHROMB17026[1]
CHROMB17026[1]CHROMB17026[1]
CHROMB17026[1]
 
2
22
2
 
Comprehensive assessment of chamber-specific and transmural heterogeneity in ...
Comprehensive assessment of chamber-specific and transmural heterogeneity in ...Comprehensive assessment of chamber-specific and transmural heterogeneity in ...
Comprehensive assessment of chamber-specific and transmural heterogeneity in ...
 
Axl inhibitor (1)
Axl inhibitor (1)Axl inhibitor (1)
Axl inhibitor (1)
 
Non biopsy diagnosis of acute rejection of Renal allograft
  Non biopsy diagnosis of acute rejection of Renal allograft  Non biopsy diagnosis of acute rejection of Renal allograft
Non biopsy diagnosis of acute rejection of Renal allograft
 
Pharmacogenetics - Pharmacokinetics
Pharmacogenetics  - Pharmacokinetics Pharmacogenetics  - Pharmacokinetics
Pharmacogenetics - Pharmacokinetics
 
Synthesis, Docking Studies and Anticancer Activity of New Substituted Pyrimid...
Synthesis, Docking Studies and Anticancer Activity of New Substituted Pyrimid...Synthesis, Docking Studies and Anticancer Activity of New Substituted Pyrimid...
Synthesis, Docking Studies and Anticancer Activity of New Substituted Pyrimid...
 
M. Celeste Simón-Homenaje al bioquímico español Alberto Sols
M. Celeste Simón-Homenaje al bioquímico español Alberto SolsM. Celeste Simón-Homenaje al bioquímico español Alberto Sols
M. Celeste Simón-Homenaje al bioquímico español Alberto Sols
 
Genetic polymorphism in drug transport
Genetic polymorphism in drug transportGenetic polymorphism in drug transport
Genetic polymorphism in drug transport
 
In vitro metabolite profiling
In vitro metabolite profilingIn vitro metabolite profiling
In vitro metabolite profiling
 
2012-JCI
2012-JCI2012-JCI
2012-JCI
 
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kd...
 
ASMSPoster_2015
ASMSPoster_2015ASMSPoster_2015
ASMSPoster_2015
 
Pharmacology bao jiaolin
Pharmacology bao jiaolinPharmacology bao jiaolin
Pharmacology bao jiaolin
 

Similar to Pan xiao

Molecular Mechanisms of Radiation Damage.
Molecular Mechanisms of Radiation Damage. Molecular Mechanisms of Radiation Damage.
Molecular Mechanisms of Radiation Damage. Dmitri Popov
 
Medical review of medolife’s escozine tm technology in pre clinical & cli...
Medical review of medolife’s escozine tm technology in pre clinical & cli...Medical review of medolife’s escozine tm technology in pre clinical & cli...
Medical review of medolife’s escozine tm technology in pre clinical & cli...PetLife Pharmaceuticals Inc
 
Thesis defense - QUANG ONG - FINAL
Thesis defense - QUANG ONG - FINALThesis defense - QUANG ONG - FINAL
Thesis defense - QUANG ONG - FINALQuang Ong
 
mitochondria poster
mitochondria postermitochondria poster
mitochondria posterAbhinav Suri
 
ZechSG16-acs-jmedchem-5b01552
ZechSG16-acs-jmedchem-5b01552ZechSG16-acs-jmedchem-5b01552
ZechSG16-acs-jmedchem-5b01552Stephan G. Zech
 
HepG2 cell model for genotoxicity and steatosis assessment
HepG2 cell model for genotoxicity and steatosis assessmentHepG2 cell model for genotoxicity and steatosis assessment
HepG2 cell model for genotoxicity and steatosis assessmentHCS Pharma
 
Drug induced hepatotoxicity and its regulatory implications
Drug induced hepatotoxicity and its regulatory implicationsDrug induced hepatotoxicity and its regulatory implications
Drug induced hepatotoxicity and its regulatory implicationsChander K Negi
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...daranisaha
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...semualkaira
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...semualkaira
 
Assignment on Toxicology
Assignment on ToxicologyAssignment on Toxicology
Assignment on ToxicologyDeepak Kumar
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...AnonIshanvi
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...NainaAnon
 
Metallothionein 2A expression and its relation to different clinical stages
Metallothionein 2A expression and its relation to different clinical stagesMetallothionein 2A expression and its relation to different clinical stages
Metallothionein 2A expression and its relation to different clinical stageswael mansy
 
Effects Of Oxygen On Radiation Therapy
Effects Of  Oxygen On  Radiation  TherapyEffects Of  Oxygen On  Radiation  Therapy
Effects Of Oxygen On Radiation Therapyfondas vakalis
 
Omics technology: an important tool in mechanism studies of Chinese herbal fo...
Omics technology: an important tool in mechanism studies of Chinese herbal fo...Omics technology: an important tool in mechanism studies of Chinese herbal fo...
Omics technology: an important tool in mechanism studies of Chinese herbal fo...LucyPi1
 

Similar to Pan xiao (20)

Cm ecs2016
Cm ecs2016Cm ecs2016
Cm ecs2016
 
Molecular Mechanisms of Radiation Damage.
Molecular Mechanisms of Radiation Damage. Molecular Mechanisms of Radiation Damage.
Molecular Mechanisms of Radiation Damage.
 
NMT_JMedChem2
NMT_JMedChem2NMT_JMedChem2
NMT_JMedChem2
 
Medical review of medolife’s escozine tm technology in pre clinical & cli...
Medical review of medolife’s escozine tm technology in pre clinical & cli...Medical review of medolife’s escozine tm technology in pre clinical & cli...
Medical review of medolife’s escozine tm technology in pre clinical & cli...
 
Thesis defense - QUANG ONG - FINAL
Thesis defense - QUANG ONG - FINALThesis defense - QUANG ONG - FINAL
Thesis defense - QUANG ONG - FINAL
 
mitochondria poster
mitochondria postermitochondria poster
mitochondria poster
 
ZechSG16-acs-jmedchem-5b01552
ZechSG16-acs-jmedchem-5b01552ZechSG16-acs-jmedchem-5b01552
ZechSG16-acs-jmedchem-5b01552
 
HepG2 cell model for genotoxicity and steatosis assessment
HepG2 cell model for genotoxicity and steatosis assessmentHepG2 cell model for genotoxicity and steatosis assessment
HepG2 cell model for genotoxicity and steatosis assessment
 
Drug induced hepatotoxicity and its regulatory implications
Drug induced hepatotoxicity and its regulatory implicationsDrug induced hepatotoxicity and its regulatory implications
Drug induced hepatotoxicity and its regulatory implications
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
 
Assignment on Toxicology
Assignment on ToxicologyAssignment on Toxicology
Assignment on Toxicology
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
 
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
A 43-Year-Old Male with PCM1-JAK2 Gene Fusion Experienced T-Lymphoblastic Lym...
 
UROP poster
UROP posterUROP poster
UROP poster
 
NMT_Nature
NMT_NatureNMT_Nature
NMT_Nature
 
Metallothionein 2A expression and its relation to different clinical stages
Metallothionein 2A expression and its relation to different clinical stagesMetallothionein 2A expression and its relation to different clinical stages
Metallothionein 2A expression and its relation to different clinical stages
 
Effects Of Oxygen On Radiation Therapy
Effects Of  Oxygen On  Radiation  TherapyEffects Of  Oxygen On  Radiation  Therapy
Effects Of Oxygen On Radiation Therapy
 
Omics technology: an important tool in mechanism studies of Chinese herbal fo...
Omics technology: an important tool in mechanism studies of Chinese herbal fo...Omics technology: an important tool in mechanism studies of Chinese herbal fo...
Omics technology: an important tool in mechanism studies of Chinese herbal fo...
 

More from LondonMet PGR Students (20)

Sara cannizzaro
Sara cannizzaroSara cannizzaro
Sara cannizzaro
 
Inflation targeting misfiring on development of housing market bubble
Inflation targeting misfiring on development of housing market bubbleInflation targeting misfiring on development of housing market bubble
Inflation targeting misfiring on development of housing market bubble
 
Md kanu
Md kanuMd kanu
Md kanu
 
Jabeen shah
Jabeen shahJabeen shah
Jabeen shah
 
Glyn robbins
Glyn robbinsGlyn robbins
Glyn robbins
 
Robert gonouya
Robert gonouyaRobert gonouya
Robert gonouya
 
Janet bowstead poster
Janet bowstead posterJanet bowstead poster
Janet bowstead poster
 
Veronica azolukwam
Veronica azolukwamVeronica azolukwam
Veronica azolukwam
 
Deepthi ratnayake
Deepthi ratnayakeDeepthi ratnayake
Deepthi ratnayake
 
Veronica azolukwam
Veronica azolukwamVeronica azolukwam
Veronica azolukwam
 
Marta kaleta
Marta kaletaMarta kaleta
Marta kaleta
 
Tracy part
Tracy partTracy part
Tracy part
 
Shazaib butt
Shazaib buttShazaib butt
Shazaib butt
 
Ozlem edizel
Ozlem edizelOzlem edizel
Ozlem edizel
 
Thao nguyen
Thao nguyenThao nguyen
Thao nguyen
 
Qicheng yu
Qicheng yuQicheng yu
Qicheng yu
 
Mohammad khaleq newaz
Mohammad khaleq newazMohammad khaleq newaz
Mohammad khaleq newaz
 
Joycelyn adinkrah
Joycelyn adinkrahJoycelyn adinkrah
Joycelyn adinkrah
 
Janet bowstead
Janet bowsteadJanet bowstead
Janet bowstead
 
Syahnaz mohdmokhter
Syahnaz mohdmokhterSyahnaz mohdmokhter
Syahnaz mohdmokhter
 

Recently uploaded

Corporate and higher education May webinar.pptx
Corporate and higher education May webinar.pptxCorporate and higher education May webinar.pptx
Corporate and higher education May webinar.pptxRustici Software
 
Manulife - Insurer Transformation Award 2024
Manulife - Insurer Transformation Award 2024Manulife - Insurer Transformation Award 2024
Manulife - Insurer Transformation Award 2024The Digital Insurer
 
FWD Group - Insurer Innovation Award 2024
FWD Group - Insurer Innovation Award 2024FWD Group - Insurer Innovation Award 2024
FWD Group - Insurer Innovation Award 2024The Digital Insurer
 
Automating Google Workspace (GWS) & more with Apps Script
Automating Google Workspace (GWS) & more with Apps ScriptAutomating Google Workspace (GWS) & more with Apps Script
Automating Google Workspace (GWS) & more with Apps Scriptwesley chun
 
Real Time Object Detection Using Open CV
Real Time Object Detection Using Open CVReal Time Object Detection Using Open CV
Real Time Object Detection Using Open CVKhem
 
presentation ICT roal in 21st century education
presentation ICT roal in 21st century educationpresentation ICT roal in 21st century education
presentation ICT roal in 21st century educationjfdjdjcjdnsjd
 
TrustArc Webinar - Unlock the Power of AI-Driven Data Discovery
TrustArc Webinar - Unlock the Power of AI-Driven Data DiscoveryTrustArc Webinar - Unlock the Power of AI-Driven Data Discovery
TrustArc Webinar - Unlock the Power of AI-Driven Data DiscoveryTrustArc
 
MS Copilot expands with MS Graph connectors
MS Copilot expands with MS Graph connectorsMS Copilot expands with MS Graph connectors
MS Copilot expands with MS Graph connectorsNanddeep Nachan
 
Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...
Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...
Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...Drew Madelung
 
ICT role in 21st century education and its challenges
ICT role in 21st century education and its challengesICT role in 21st century education and its challenges
ICT role in 21st century education and its challengesrafiqahmad00786416
 
Strategize a Smooth Tenant-to-tenant Migration and Copilot Takeoff
Strategize a Smooth Tenant-to-tenant Migration and Copilot TakeoffStrategize a Smooth Tenant-to-tenant Migration and Copilot Takeoff
Strategize a Smooth Tenant-to-tenant Migration and Copilot Takeoffsammart93
 
Connector Corner: Accelerate revenue generation using UiPath API-centric busi...
Connector Corner: Accelerate revenue generation using UiPath API-centric busi...Connector Corner: Accelerate revenue generation using UiPath API-centric busi...
Connector Corner: Accelerate revenue generation using UiPath API-centric busi...DianaGray10
 
Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...
Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...
Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...apidays
 
Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...
Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...
Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...Miguel Araújo
 
Apidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, Adobe
Apidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, AdobeApidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, Adobe
Apidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, Adobeapidays
 
Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...
Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...
Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...apidays
 
A Beginners Guide to Building a RAG App Using Open Source Milvus
A Beginners Guide to Building a RAG App Using Open Source MilvusA Beginners Guide to Building a RAG App Using Open Source Milvus
A Beginners Guide to Building a RAG App Using Open Source MilvusZilliz
 
Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...
Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...
Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...apidays
 
Powerful Google developer tools for immediate impact! (2023-24 C)
Powerful Google developer tools for immediate impact! (2023-24 C)Powerful Google developer tools for immediate impact! (2023-24 C)
Powerful Google developer tools for immediate impact! (2023-24 C)wesley chun
 

Recently uploaded (20)

Corporate and higher education May webinar.pptx
Corporate and higher education May webinar.pptxCorporate and higher education May webinar.pptx
Corporate and higher education May webinar.pptx
 
+971581248768>> SAFE AND ORIGINAL ABORTION PILLS FOR SALE IN DUBAI AND ABUDHA...
+971581248768>> SAFE AND ORIGINAL ABORTION PILLS FOR SALE IN DUBAI AND ABUDHA...+971581248768>> SAFE AND ORIGINAL ABORTION PILLS FOR SALE IN DUBAI AND ABUDHA...
+971581248768>> SAFE AND ORIGINAL ABORTION PILLS FOR SALE IN DUBAI AND ABUDHA...
 
Manulife - Insurer Transformation Award 2024
Manulife - Insurer Transformation Award 2024Manulife - Insurer Transformation Award 2024
Manulife - Insurer Transformation Award 2024
 
FWD Group - Insurer Innovation Award 2024
FWD Group - Insurer Innovation Award 2024FWD Group - Insurer Innovation Award 2024
FWD Group - Insurer Innovation Award 2024
 
Automating Google Workspace (GWS) & more with Apps Script
Automating Google Workspace (GWS) & more with Apps ScriptAutomating Google Workspace (GWS) & more with Apps Script
Automating Google Workspace (GWS) & more with Apps Script
 
Real Time Object Detection Using Open CV
Real Time Object Detection Using Open CVReal Time Object Detection Using Open CV
Real Time Object Detection Using Open CV
 
presentation ICT roal in 21st century education
presentation ICT roal in 21st century educationpresentation ICT roal in 21st century education
presentation ICT roal in 21st century education
 
TrustArc Webinar - Unlock the Power of AI-Driven Data Discovery
TrustArc Webinar - Unlock the Power of AI-Driven Data DiscoveryTrustArc Webinar - Unlock the Power of AI-Driven Data Discovery
TrustArc Webinar - Unlock the Power of AI-Driven Data Discovery
 
MS Copilot expands with MS Graph connectors
MS Copilot expands with MS Graph connectorsMS Copilot expands with MS Graph connectors
MS Copilot expands with MS Graph connectors
 
Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...
Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...
Strategies for Unlocking Knowledge Management in Microsoft 365 in the Copilot...
 
ICT role in 21st century education and its challenges
ICT role in 21st century education and its challengesICT role in 21st century education and its challenges
ICT role in 21st century education and its challenges
 
Strategize a Smooth Tenant-to-tenant Migration and Copilot Takeoff
Strategize a Smooth Tenant-to-tenant Migration and Copilot TakeoffStrategize a Smooth Tenant-to-tenant Migration and Copilot Takeoff
Strategize a Smooth Tenant-to-tenant Migration and Copilot Takeoff
 
Connector Corner: Accelerate revenue generation using UiPath API-centric busi...
Connector Corner: Accelerate revenue generation using UiPath API-centric busi...Connector Corner: Accelerate revenue generation using UiPath API-centric busi...
Connector Corner: Accelerate revenue generation using UiPath API-centric busi...
 
Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...
Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...
Apidays Singapore 2024 - Scalable LLM APIs for AI and Generative AI Applicati...
 
Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...
Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...
Mastering MySQL Database Architecture: Deep Dive into MySQL Shell and MySQL R...
 
Apidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, Adobe
Apidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, AdobeApidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, Adobe
Apidays New York 2024 - Scaling API-first by Ian Reasor and Radu Cotescu, Adobe
 
Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...
Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...
Apidays New York 2024 - Accelerating FinTech Innovation by Vasa Krishnan, Fin...
 
A Beginners Guide to Building a RAG App Using Open Source Milvus
A Beginners Guide to Building a RAG App Using Open Source MilvusA Beginners Guide to Building a RAG App Using Open Source Milvus
A Beginners Guide to Building a RAG App Using Open Source Milvus
 
Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...
Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...
Apidays New York 2024 - The Good, the Bad and the Governed by David O'Neill, ...
 
Powerful Google developer tools for immediate impact! (2023-24 C)
Powerful Google developer tools for immediate impact! (2023-24 C)Powerful Google developer tools for immediate impact! (2023-24 C)
Powerful Google developer tools for immediate impact! (2023-24 C)
 

Pan xiao

  • 1. Evodiamine isolated from Evodia rutaecarpa as human topoisomerase catalytic inhibitor Xiaobei Pan1 , Janet M. Hartley2 , John A. Hartley2 , Kenneth N White1 , Zhengtao Wang1,3 , S. W. Annie Bligh1 1 Institute for Health Research and Policy, London Metropolitan University, 166-220 Holloway Road, London N7 8DB, UK 2 Cancer Research UK Drug-DNA Interactions Research Group, UCL Cancer Institute, University College London, Paul O’Gorman Building, London, UK 3 The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Zhangjiang Hi-tech Park, Shanghai 201210, China Introduction  Topoisomerase (Fig. 1) is an enzyme, which can relieve torsional stress in DNA.  Topoisomerase I and II cleave the single and double stranded DNA, respectively.  Since camptothecin was found as a topoisomerase inhibitor, a number of semi- synthetic compounds were successfully developed and used to treat cancer.  Evodia rutaecarpa (Fig. 2) is a Chinese herbal medicinal plant that has been used to treat gastrointestinal disorders, bacterial infection & inflammation-related disorders.  Evodiamine isolated from Evodia rutaecarpa is cytotoxic to several cancer cell lines. Aims and Objectives  To isolate quinoline alkaloids from the Evodia and structure elucidation  To study their potential cytotoxicity, inhibitory activity of topoisomerase I and II, and catalytic mechanisms. Methods  Alkaloids were isolated using reverse-phase HPLC and the structures were elucidated by 1-D, 2-D NMR spectroscopy and mass spectrometry.  Their cytotoxicities were determined using MTT-based assay.  Topoisomerase (Topo) inhibitory activities were studied using Topo I relaxation and Topo II decatanation assay.  Comet assay and cell cycle distribution study were carried out by flow cytometry. Results and Discussion  Eight alkaloids were isolated from Evodia, of which evodiamine (Fig. 3) showed the most potent activity against human leukemia K562 and THP-1 cell lines (IC50 34.35 µM and 90.87 µM respectively.)  Evodiamine is an inhibitor for both human Topo I and Topo II (Fig. 4).  It did not induce DNA strand breaks at the cellular level (Fig. 5) and arrested cell growth at the G2/M phase in the cell cycle. N H N N O2 3 5 6 78 9 10 11 12 13 15 16 17 18 19 20 21 H H3C Conclusion Evodiamine was found to be a dual inhibitor for both topoisomerase I and II with potent cytotoxicity against human leukemia cell lines. Figure 1. Structure of topoisomerase Figure 2. Evodia rutaecarpa Figure 3. Structure of Evodiamine Figure 4. IC50 of evodiamine against human Topo I (A, C) using relaxation assay and Topo II (B, D) using decatanation assayFigure 5. The comet assay did not detect DNA strand breaks induced by evodiamine Acknowledgement X.Pan thanks the Department of Human Science at London Metropolitan University for a student bursary.