天然药（产）物化学一 天然药物化学的魅力 一个充满魅力的领域？ u find them? 史清文教授 Nature is friendly?What can you do with them ature is healthy?Why do we care so much? http://202.206.48.73/tryw1/default.asp Where Chemistry and Biology Meet? The Chemistry Universe 天然产物化学 C.H.O.N.PF.Cl and MW500? Chemistry 片益 天然产物在药物发现中的作用 How are drugs discovered and developed Nature is one big medicine cabinet by Source ( SM:NP 药物研发一多学科系统工程
1 天然药物化学的魅力 史 清 文 教授 药学院天然药物化学教研室405室 QQ: 46897262 Mobile: 13643389897 http://202.206.48.73/tryw1/default.asp What are they? Where can you find them? What can you do with them? Why do we care so much? 天然药(产)物化学— 一个充满魅力的领域？ Nature is good? Nature is green? Nature is friendly? Nature is healthy? Where Chemistry and Biology Meet ? Chemistry Biology 天然产物化学 All Life Is Chemistry and Biology 天然产物作为化学和生物学之间一个天然的通道，是大自然经过漫长 的筛选和进化选择出来的，天然产物的结构与功能研究将对新药发现、对 于生命科学的认识、探索药物作用机制具有重要科学意义。 The Chemistry Universe Nature has compounds at hand that have the potential to treat and possibly also prevent the prominent diseases of modern societies. 天然产物在药物发现中的作用 n All small molecule new chemical entities by Source ( 01/1981- 06/2006) N: Natural product ND: Semi-synthetic NP S*: Made by total synthesis, but the pharmacophore from NP NM: NP mimic J Nat Prod 2007,70,461 Nature is one big medicine cabinet Newman D. J. 药物研发—多学科系统工程 How are drugs discovered and developed?
1970-2000间新药投入与产出比较 More investments Fewer dru Chemistry Everyday for Everyone 大蒜：生长在土地上的天然抗生素 天然产物在哪？ Natural Produets-The Chemicals That Shaped The World? Surrounding us? Falcarinol Lycopene番茄红素 Credited with Preventing Colon Cancer An antioxidant compound 人人 nteC Natural Food is Medicine:Medicine is Natural Food
2 1970-2000 间新药投入与产出比较 The costs of drug discovery and drug development continue to increase at astronomical rates, yet despite these expenditures, there is a decrease in the number of new medicines introduced into the world market. More investments Fewer drugs 天然产物在哪？ Natural Products—The Chemicals That Shaped The World? Chemistry Everyday for Everyone Chemistry Everyday for Everyone 大蒜Allium sativum L.不仅具有防癌、抗癌、降低血糖，预防糖尿 病、抗菌效果，在控制肥胖方面也具有意想不到的效果。大蒜自古就被 当作天然杀菌剂，有“天然抗生素”之称，是人体循环及神经系统的天然 强健剂--可降血压护心脑 。 “The doctor of the further will no longer treat the human frame with drugs, but rather will cure and prevent disease with Nutrition” 大蒜：生长在土地上的天然抗生素 大蒜:犹太人的“盘尼西林” Falcarinol Credited with Preventing Colon Cancer Carrots (Daucus carota) Red Gonseng 2 mg/kg Falcarinol 镰叶芹醇 又称 人参炔醇 panaxynol Chasing Molecules from Nature: Healthy Molecules Come from Healthy Food Lycopene Lycopene 番茄红素 An antioxidant compound Natural Food is Medicine; Medicine is Natural Food
Sea Thin in the 21th Century 姜黄素Curcumin From Molecules to Medicines Fucoxanthin 岩蒸黄质，曼角藤黄素 ◆ Promoting Weight Loss-Lifestyle Drugs 大豆Isoflavones in Soybean 分子美食学(Molecular Gastronomy) Flavonoids are our friends:Are ueating enough? 三 意菜止你成肌肉男豆装会世你更美 來自植物的抗凝血化合物 THE CHEMISTRY OF COFFEE THE CHEMISTRY OF HONEY 5 3
3 Fucoxanthin Promoting Weight Loss—Lifestyle Drugs 岩藻黄质，墨角藻黄素 Sea Thin in the 21th Century HO O O C HO O O 姜黄素 Curcumin— 2007 年，美国NIH批准姜黄素用于对付四个病的临床实验：直肠癌， 胰腺癌，老年痴呆和多发性骨髓瘤。随后，乳腺癌和骨关节炎等多种疾病的 临床实验也被陆续批准实施。 From Molecules to Medicines O HO O O OH O O HO O OH OH O 大豆 Isoflavones Isoflavones in Soybean O O OH HO Daidzein O O OH O Daidzin O OH HO HO OH O O OH O Genistin O OH HO HO OH OH O O OH HO Genistein OH Flavonoids are our friends: Are u eating enough? 吃菠菜让你成为肌肉男 喝豆浆会让你更美丽 Flavonoids alter the way our cells function-in a good way Menthol is included in many different consumer products including (A) chocolate, (B) chewing gum and (C) toothpaste. Menthol Phytochemistry 2013, 96: 15-25 薄荷 HO 分子美食学(Molecular Gastronomy) Flavonoids— Lowering cardiovascular disease 分子美食学(Molecular Gastronomy) 來自植物的抗凝血化合物 “It’s amazing：After the atomic bomb in Hiroshima, the ginkgo was the first tree that came up.” 銀杏(Ginkgo biloba) 达纳康(Tanakan®)
健康钥匙一白藜芦醇Resveratrol Hypericin:Cancer Treatment 'Mmiracle Molecules'in red wine Red Wine Myth 1939 4
4 白藜芦醇—— “法兰西奇迹” ：法国人冠心病发病率 和死亡率的比例在发达国家最低，仅是美国的60％。 健康钥匙—白藜芦醇Resveratrol The 'Mmiracle Molecules' in red wine OH HO OH 1992 1939 Resveratrol is "Nature's Medicine" for Cancer, Heart Disease and Much More Hypericin : Cancer Treatment Cancer Treatment Hypericin 金丝桃素 Hypericum monogynum L. Antidepressive, antineoplastic, antitumor and antiviral activities OH CH3 O OH HO HO OH O OH CH3 贯叶金丝桃, 连翘 O O O O OH 胡桐 Calanolide A Anti-HIV (Calophyllum lanigerum) FDA 三期临床艾滋病 抗抑郁症、抗病毒