Phytochemical can prevent Cancer!

Phytochemical can prevent

Cancer!

Developing Agents from Phytochmical

 Molecular Docking : Protein – Ligand 간의 결 합력 측정

=> 결합력이 높다고 무조건 좋은 것은 아니나 우선적 실 험 대상에 들어감

 Molecular Docking (Docking Simulation)

Phytochemicals for Cancer Cure

 Polyphenols

 Phenolic Acids, Flavonoids, Stilbenes, Curcuminoids

 Terpenoids

 Carotenoids, Non-Carotenoid Terpenoids

 Organosulfur Compounds

 Glucosinolate-derived, Allyl Sulfur Compounds

 Phytosterols

Polyphenols

 One or more Hydroxyl Groups(-OH) attached to a Benzene Ring

 >= 8000 Different Polyphenols

 Diabetes, Osterporosis, Neurodegenerative Disease, Cancer…

 Phenolic Acids, Flavonids, Stilbenes, Curcuminoids

Polyphenols

 Phenolic Acids

 30% of Dietary Polyphenols

 Phenol Ring + Carboxylic Acid

 Ex) Ellagic Acid : NF-kB & IGF-2 Inhibition, P53/P21

Induction, Modulation of Pro- and Anti-apoptotic Proteins

=> Antioxidant, Cell Cycle Arrest, Antiproliferation, Apoptosis

Polyphenols

 Ellagic Acid

Polyphenols

 Flavonoids

 60% of Dietary Polyphenols

 Two Benzene Rings Linked by Three Carbon Atoms

 Ex) (-)-Epigallocatechin-3-gallate(EGCG) : VEGF Inhibition(Anti-angiogenic), HGF/c-Met Signaling Inhibition(Invade & Metastasis Inhibition)

 Combination of EGCG with Antitumor Drug or Other

Phytochemicals => IDO Inhibition(Immune Evasion Inhibition -> Antiproliferation, Apotosis)

Polyphenols

 EGCG

Polyphenols

 Flavonoids

Ex) Genistein : Estrogen-like Effects -> Hormone-Related Cancer(Prostate, Breast) Inhibition

 Other Anti-Cancer Effects : Apoptosis, Cell Cycle Arrest, NF-kB signaling Inhibition, p53 signaling Activation,

telomerase Inhibition, VEGF signaling Inhibition, PPAR Signaling Activation…

Polyphenols

 Genistein

Polyphenols

 Flavonoids

Ex) Luteolin : Lower risk of Breast Cancer, Traditional Chinese Medicine

 Other Anti-Cancer Effects : Akt & NF-kB & COX-2 Signaling Inhibition, Apoptosis, Antioxidant

Polyphenols

 Luteolin

Polyphenols

 Flavonoids

Ex) Quercetin : Antioxidant, Anti-Proliferation, Regulation of Cell Cycle & Apoptosis, PI3k/Akt Signaling Pathway

Inhibition, COX-2 and PGE2 Production Inhibition, CD74 Expression Inhibition

Synergistic Effect with EGCG

Polyphenols

 Quercetin

Polyphenols

 Stilbenes

 Stress Metabolites(Response to Fungi Infection)

 Core of 1,2-diphenylethylene(cis-, trans-)

 Ex) Resveratrol : Suppress Carcinogenesis, Inflammation Inhibition, Apoptosis, Cell Cycle Regulation, Genomic

Stability, Anti-Proliferation

 Antitumor Activity of Other Drugs : Rapamycin, Gemcitabine

Polyphenols

 Resveratrol

Polyphenols

 Curcuminoids

 Yellow Crystalline Powder

 Two Ortho-methoxylated Phenols and a beta-diketone with conjugated double Bonds

 Ex) Curcumin : Most of Cancer Characterics Inhibition! : Cell Growth Inhibition, Apoptosis, Anti-Inflammatory, Cell Cycle Inhibition, Anti-Proliferation, Up-regulation of P53, Increase the capacity of T Effector Cells to Kill Cancer…

Polyphenols

 Curcumin

Terpenoids

 Synthesized from two Five-Carbon Isoprene units

 Secondary Metabolites : Defense against insects &

Environmental Stress, Repair of Damage & Wounding

 Antitumor Drugs : Taxane, Vincristine, Vinblastine…

 Carotenoids, Non-Carotenoid Terpenoids

Terpenoids

 Carotenoids

 Fat-Soluble Pigments

 Provitamine A Group VS Non-Provitamine A Group

 Ex) Lycopene : Akt signaling, Antioxidant/Detoxification enzymes, cell cycle Regulation, IGF signaling, Ras

signaling(Metastasis)…

=> Lower Prostate Cancer

Terpenoids

 Lycopene

Terpenoids

 Non-Carotenoid Terpenoids

 Ex) Carnosol : Antioxidant, Anti-Inflammatory, Regulation of NF-kB, AMPK, ER, And AR Pathways, Apoptotic Proteins, Proto-Oncogenes(c-jun), Invasion Inhibition by Suppressing MMP-9

=> Leukemia, Colon, Prostate Cancer Down

Terpenoids

 Carnosol

Organosulfur Compounds

 At least one atom of Sulfur in their Structure

 Glucosinolate-Derived Organosulfur Compounds, Allyl Sulfur Compounds

Organosulfur Compounds

 Glucosinolate-Derived Organosulfur Compounds

 Ex) Sulforaphane : Regulation of the JNK-, HIF-1 alpha(Metabolism), ER/AR, Fas Signaling pathway, Apoptosis/Autophagy

Organosulfur Compounds

 Sulforaphane

Organosulfur Compounds

 Allyl Sulfur Compounds

 Ex) Diallyl Disulfide : G2/M Arrest, Apoptosis

=> Colon/Gastric Cancer, Leukemia Prevention

Phytosterol

 Classified as 4-desmethylsterols

 Similar to Cholesterol, Lower Absorption

 Ex) Beta-Sistosterol : Cancer Proliferation Inhibition,

Induce Apoptosis(Caspase Activation, Fas Level Up, Increase MAPK Activity, Bcl-2 Expression Modulation)

=> Colon, Breast Cancer, Leukemia, Fibrosarcoma, Stomach, Prostate Cancer Down