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Phytochemicals HO O OH CH OC(CH3)3 3 CH3 CH3 H H O NH O CH3 O O O O OH O CH3 CH3 OH CH3 N N O O O N N CH3 OH HO OH HO Alkaloids Steroids Terpenoids Phenylpropanoids Polyphenols Others Phytochemicals Phytochemical is a general term for natural botanical chemicals Asiatic Acid [A2475] is a pentacyclic triterpene extracted from found in, for example, fruits and vegetables. Phytochemicals are Centella asiatica which is a tropical medicinal plant. Asiatic Acid not necessary for human metabolism, in contrast to proteins, possess wide pharmacological activities. sugars and other essential nutrients, but it is believed that CH3 phytochemicals affect human health. Phytochemicals are CH3 components of herbs and crude drugs used since antiquity by humans, and significant research into phytochemicals continues today. H C CH H C OH HO 3 3 O Atropine [A0754], a tropane alkaloid, was first extracted from H CH3 the root of belladonna (Atropa belladonna) in 1830s. Atropine is a HO competitive antagonist of muscarine-like actions of acetylcholine CH3 H and is therefore classified as an antimuscarinic agent. OH [A2475] O NCH3 O C CHCH2OH Curcumin [C0434] [C2302], a dietary constituent of turmeric, has chemopreventive and chemotherapeutic potentials against various types of cancers. OO CH3O OCH3 [A0754] HO OH Galantamine Hydrobromide [G0293] is a tertiary alkaloid [C0434] [C2302] found in the bulbs of Galanthus woronowi. Galantamine has shown potential for the treatment of Alzheimer's disease. TCI provides many phytochemicals such as alkaloids, steroids, terpenoids, phenylpropanoids, polyphenols and etc. OH References O . HBr Phytochemistry of Medicinal Plants, ed. by J. T. Arnason, R. Mata, J. T. CH3O Romeo, Springer US, New York, 1995. N Phytochemicals as Bioactive Agents, ed. by W. R. Bidlack, S. T. Omaye, M. CH 3 S. Meskin, D. K. W. Topham, CRC Press, Boca Raton, 2000. [G0293] Phytochemical Techniques, ed. by N. Raaman, New India Publishing, New Delhi, 2006. (+)-Bicuculline [B1890] is a phthalide isoquinoline alkaloid isolated from a variety of plants, Dicentra, Corydalis, and Adlumia, genera of the Fumariaceae family. Bicuculline blocks GABAA receptors selectively. O N O CH3 H H O O O O [B1890] 2 Please inquire for pricing and availability of listed products to our local sales representatives. Please inquire for pricing and availability of listed products to our local sales representatives. Phytochemicals A0754 5g 25g A0550 5g 25g C3584 25mg 100mg O O OCH3 CH3 OCH3 NCH3 O C CHCH2OH NCH3 OCCHCH2OH N Alkaloids O 2 Cl . O H2SO4 H2O Atropine Atropine Sulfate Monohydrate Chelerythrine Chloride CAS RN: 51-55-8 CAS RN: 5908-99-6 CAS RN: 3895-92-9 B0450 5g 25g B0451 5g 25g L0319 25mg 100mg B0397 25g 100g B1890 25mg 100mg O OH O O O HO N O O CH3 H H H 2 SO4 O . HCl O N Cl N H . CH3O . H2O CH3O xH2O N O O OCH O . 3 2 OCH3 xH2O Lycorine Hydrochloride Betanin (Red Beet extract O Berberine Chloride Hydrate Berberine Sulfate Hydrate Monohydrate diluted with Dextrin) (+)-Bicuculline CAS RN: 141433-60-5 CAS RN: 316-41-6 CAS RN: 6150-58-9 CAS RN: 7659-95-2 CAS RN: 485-49-4 B0670 25g B0946 25g B0671 5g D5696 25mg 100mg C2042 25g 500g H H H CH3O N O O CH O N CH3 CH3O N 3 H CH3 CH3 CH3 H H CH3O N N H H N N N CH3O N CH3O N O O H H H H H O N N O NN . HCl . H O O O O O 2 H H H Brucine Hydrochloride CH3 . xH2O Brucine Anhydrous Monohydrate 1,7-Dimethylxanthine Caffeine Brucine Hydrate CAS RN: 357-57-3 CAS RN: 5786-96-9 CAS RN: 611-59-6 CAS RN: 58-08-2 C1495 100mg 1g M1149 1g C0380 500mg 5g F1173 20mg 100mg C0433 100mg 1g CH3O O OCH3 OH OCH OH 3 OCH O NH CCH3 3 H3CCH3 O O CH O N 3 O CH3 N CH3O CH3 H NO N H Cl H CH3O N CH H HO 3 H O CH3 N O N OCH O CH CH3CH2 OH 3 3 . CH3O HO O . HCl 5H2O Colchicine (contains 5% OCH3 (S)-(+)-Camptothecin Capsaicin (Natural) Ethyl Acetate at maximum) Fangchinoline Curare Pentahydrate CAS RN: 7689-03-4 CAS RN: 404-86-4 CAS RN: 64-86-8 CAS RN: 436-77-1 CAS RN: 6989-98-6 C2609 100mg 1g D0600 5g 25g 100g E1012 1g G0293 100mg 1g D0653 25g 250g OH O NH N O CH3 HO N O CH2N OH H . HBr CH3 N N NH2 CH CH3O HO 3 N O N H CH3 (-)-Cytisine L-DOPA (±)-Evodiamine Galantamine Hydrobromide Gramine CAS RN: 485-35-8 CAS RN: 59-92-7 CAS RN: 518-18-3 CAS RN: 1953-04-4 CAS RN: 87-52-5 H0001 1g H0450 5g I1012 200mg 1g I0868 25mg I0714 100mg O O N N C O OH CH2CH3 O HO O O HO O N N N HO H . HCl N NCH3 O C CH O N N O . HO CH3O N 3H2O O H CH2OH H H CH3CH2 CH3 Irinotecan Hydrochloride Harmine (-)-Hyoscyamine Indican (Plant Indican) Indirubin Trihydrate CAS RN: 442-51-3 CAS RN: 101-31-5 CAS RN: 487-60-5 CAS RN: 479-41-4 CAS RN: 136572-09-3 J0009 10mg P2609 10mg 50mg P2610 5mg 25mg P2651 25mg 100mg L0272 200mg 1g CH3 CH3 OH OCH3 H OCH3 OH H3C CH3 H HO H CH3 H H H H H CH3CH2 H3C N N OH N N CH3 O H H OH H H OH OCH3 H3C CH3 H H3C H O CH3 CH3 CH3 H H3C H H H3C H H O H H H CH3 H H H H HO HO O HN CH3 HO HO H H H CH CH .HBr O OH 3 3 O Jervine Peiminine Peimine (20S)-Protopanaxadiol Lappaconitine Hydrobromide CAS RN: 469-59-0 CAS RN: 18059-10-4 CAS RN: 23496-41-5 CAS RN: 30636-90-9 CAS RN: 97792-45-5 M2120 200mg 1g M3093 50mg 250mg N0079 25mL 100mL 500mL N0963 5g 25g P0016 25g O O O OCH3 N H H CH3 O N N H H OCH3 O OCH3 H H N CH3O CH3O O N CH3 . HCl xH2O HH H H N OCH3 N N Noscapine Hydrochloride CH3O . HCl Matrine Sophoridine Nicotine Hydrate Papaverine Hydrochloride CAS RN: 519-02-8 CAS RN: 6882-68-4 CAS RN: 54-11-5 CAS RN: 912-60-7 CAS RN: 61-25-6 Please inquire for pricing and availability of listed products to our local sales representatives. Please inquire for pricing and availability of listed products to our local sales representatives. 3 Phytochemicals P0434 1g 5g P0399 5g P0460 1g 5g P2361 25mg 100mg Q0006 5g 25g H CH2 CH N N O O O N OCH3 CH3 CH3 N O N HO N N H O CH3O CH3 O O CH3 O O OCH3 . HNO OCH HCl 3 3 N Pilocarpine Hydrochloride Pilocarpine Nitrate Piperine Piperlongumine Quinidine CAS RN: 54-71-7 CAS RN: 148-72-1 CAS RN: 94-62-2 CAS RN: 20069-09-4 CAS RN: 56-54-2 Q0010 5g 25g Q0028 25g 100g Q0030 25g R0007 1g 5g R0102 1g 200mg H CH2 CH H CH2 CH H CH2 CH N H N CH3O N H N O N H N HO H H HO O N HO H H H CH O OCH CH3O . HCl 3 O 3 N CH3O CH3O . O . 2H2O OCH3 H2SO4 OCH3 . N OCH 2H2O 3 N 2 N Quinine Hydrochloride Quinidine Sulfate Dihydrate Quinine Dihydrate Reserpine Rutaecarpine CAS RN: 6591-63-5 CAS RN: 130-95-0 CAS RN: 6119-47-7 CAS RN: 50-55-5 CAS RN: 84-26-4 S0021 1g 10g O0505 25mg 100mg S0461 1g 5g 10g S0884 1g S0358 10mg O H N H H N N O O CH2OH H . OONCH3 CCH HBr . N C O H2O N . N CH CH 3H2O H H H H 3 3. Scopolamine N HCl Hydrobromide Trihydrate Sophocarpine Monohydrate (-)-Sparteine (+)-Sparteine Stachydrine Hydrochloride CAS RN: 6533-68-2 CAS RN: 145572-44-7 CAS RN: 90-39-1 CAS RN: 492-08-0 CAS RN: 4136-37-2 S0249 25g S0257 25g S0093 25g S0094 25g S0232 5g 25g N HO N N NHCH3 N H . HCl . xH2O N . N N HNO3 H H N O O O O 2 O O O O . H Strychnine Hydrochloride H2SO4 5H2O OH Strychnine Hydrate Strychnine Nitrate Strychnine Sulfate Pentahydrate Synephrine CAS RN: 57-24-9 CAS RN: 1421-86-9 CAS RN: 66-32-0 CAS RN: 60491-10-3 CAS RN: 94-07-5 Y0012 1g 5g S0233 25g T3650 1g 5g T3311 250mg T3321 200mg 1g OCH OCH3 HO OH 3 OCH3 CH3O NHCH3 OCH3 OCH3 CHCH2NHCH3 N HOOC COOH H CH3 OCH3 N CH3 . O HO OH N N OCH3 CH O CH3O OH 2 3 O OH OCH3 OCH3 (-)-Synephrine Synephrine Tartrate Tetrahydropalmatine L-Tetrahydropalmatine Tetrandrine CAS RN: 614-35-7 CAS RN: 16589-24-5 CAS RN: 2934-97-6 CAS RN: 483-14-7 CAS RN: 518-34-3 T0178 25g 100g 500g T0179 25g 100g 500g T0180 25g T3636 100mg T1429 5g CH3 CH3 CH O O 3 O H3C N O H O N CH3 CH3 H C H H H C O N N N NN. 3 CH3COONa H H HN O N N O . HCl N O NN H N H Na Gal Glc Xyl CH3 O CH3 CH3 Glc CH3 Theobromine Theophylline Theophyllol Tomatine from Tomato Trigonelline Hydrochloride CAS RN: 83-67-0 CAS RN: 58-55-9 CAS RN: 8002-89-9 CAS RN: 17406-45-0 CAS RN: 6138-41-6 V0148 10mg 50mg V0061 1g 5g Y0002 5g 25g H N CH3 CH3 OH N H N H3C H N H HH HO HN HO H CH3 H CH3O .
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  • Structural Requirements of Flavonoids and Related Compounds for Aldose Reductase Inhibitory Activity

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    788 Chem. Pharm. Bull. 50(6) 788—795 (2002) Vol. 50, No. 6 Structural Requirements of Flavonoids and Related Compounds for Aldose Reductase Inhibitory Activity Hisashi MATSUDA, Toshio MORIKAWA, Iwao TOGUCHIDA, and Masayuki YOSHIKAWA* Kyoto Pharmaceutical University; Misasagi, Yamashina-ku, Kyoto 607–8412, Japan. Received January 15, 2002; accepted February 13, 2002 The methanolic extracts of several natural medicines and medicinal foodstuffs were found to show an in- hibitory effect on rat lens aldose reductase. In most cases, flavonoids were isolated as the active constituents by 5 bioassay-guided separation, and among them, quercitrin (IC50 0.15 mM), guaijaverin (0.18 mM), and desmanthin- 1 (0.082 mM) exhibited potent inhibitory activity. Desmanthin-1 showed the most potent activity, which was equiv- alent to that of a commercial synthetic aldose reductase inhibitor, epalrestat (0.072 mM). In order to clarify the structural requirements of flavonoids for aldose reductase inhibitory activity, various flavonoids and related com- pounds were examined. The results suggested the following structural requirements of flavonoid: 1) the flavones and flavonols having the 7-hydroxyl and/or catechol moiety at the B ring (the 39,49-dihydroxyl moiety) exhibit the strong activity; 2) the 5-hydroxyl moiety does not affect the activity; 3) the 3-hydroxyl and 7-O-glucosyl moieties reduce the activity; 4) the 2–3 double bond enhances the activity; 5) the flavones and flavonols having the cate- chol moiety at the B ring exhibit stronger activity than those having the pyrogallol moiety (the 39,49,59-trihy- droxyl moiety). Key words aldose reductase inhibitor; flavonoid; structural requirement; desmanthin-1; quercitrin; guaijaverin Aldose reductase as a key enzyme in the polyol pathway is aerial parts of Centella asiatica (Umbelliferae),11) and the reported to catalyze the reduction of glucose to sorbitol.
  • (12) Patent Application Publication (10) Pub. No.: US 2009/0269772 A1 Califano Et Al

    (12) Patent Application Publication (10) Pub. No.: US 2009/0269772 A1 Califano Et Al

    US 20090269772A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0269772 A1 Califano et al. (43) Pub. Date: Oct. 29, 2009 (54) SYSTEMS AND METHODS FOR Publication Classification IDENTIFYING COMBINATIONS OF (51) Int. Cl. COMPOUNDS OF THERAPEUTIC INTEREST CI2O I/68 (2006.01) CI2O 1/02 (2006.01) (76) Inventors: Andrea Califano, New York, NY G06N 5/02 (2006.01) (US); Riccardo Dalla-Favera, New (52) U.S. Cl. ........... 435/6: 435/29: 706/54; 707/E17.014 York, NY (US); Owen A. (57) ABSTRACT O'Connor, New York, NY (US) Systems, methods, and apparatus for searching for a combi nation of compounds of therapeutic interest are provided. Correspondence Address: Cell-based assays are performed, each cell-based assay JONES DAY exposing a different sample of cells to a different compound 222 EAST 41ST ST in a plurality of compounds. From the cell-based assays, a NEW YORK, NY 10017 (US) Subset of the tested compounds is selected. For each respec tive compound in the Subset, a molecular abundance profile from cells exposed to the respective compound is measured. (21) Appl. No.: 12/432,579 Targets of transcription factors and post-translational modu lators of transcription factor activity are inferred from the (22) Filed: Apr. 29, 2009 molecular abundance profile data using information theoretic measures. This data is used to construct an interaction net Related U.S. Application Data work. Variances in edges in the interaction network are used to determine the drug activity profile of compounds in the (60) Provisional application No. 61/048.875, filed on Apr.