A common flavonol, which inhibits lipoxygenase and ornithine decarboxylase induction.

Nakadate T, Aizu E, Yamamoto S, Kato R. Prostaglandins. 30:357-368 (1985).

A phospholipase A2 inhibitor. Showed synergistic inhibition of of prostate
cancer cells when used in combination with paclitaxel or lovastatin.

de Souza PL, Castillo M, Myers CE. Br J Cancer. 75:1593-600 (1997).

A firmly established and well tolerated angiotensin-converting enzyme inhibitor. It attenuates the myocardial infarction induced rise in cardiac cytokine expression. Clinical trials show that quinapril prevents restenosis after coronary stenting in patients with angiotensin-coverting enzyme D allele.

Warnica JW, Gilst WV, Baillot R, Johnstone D, Block P et al. Can J Cardiol. 18:1191-200 (2002).
We GC, Siroi MG, QuR, Liu P, Roulea JL. Cardiovasc Drugs Ther. 16:29-36 (2002).
Culy CR, Jarvis B. Drugs. 62:339-85 (2002).

Eston, Estrovis, Plestrovis
C25H32O2            Mol. Wt.: 364.52             [152-43-2]
It is used in estrogen replacement therapy.

Mann V, Huber C, Kogianni G, Collins F, Noble B Bone. 40:674-684 (2006).

Rabeprazole

A proton pump/ATP-ase inhibitor.

Furuta T, Shirai N, Sugimoto M et al. Pharmacogenomics. 5:181-202 (2004).

A potent enkephalinase inhibitor exhibits selective antisecretory activity.

Primi MP, Bueno L, Baumer P et al. Ali. Pharm Ther. 13 suppl6:3-7 (1999).

Racemethorphan

See Dextromethorphan Hydrobromide

C18H23NO3                      Mol.: 301.38             [90274-24-1]
An adrenergic β-Agonistsagonist with effects of increasing muscle mass and decreasing body fat in rodents and lifestock.

Page et. al. Domest Anim Endocrinol. 26:23-31 (2004).

Monorden
Macrolactone antibiotic from several fungi. It has antifungal activity. It is a tyrosine kinase inhibitor, cell differentiation modulator, and has antiangiogenic activity.

Shimada et al. J. Antibiot. 48:824 (1995).
Pillay et al. Cell Growth Differ. 7:1487 (1996).
Oikawa et al. Eur J Pharmacol. 241:221 (1993).

A selective estrogen receptor modulator (SERM. It is effective for the prevention of postmenopausal osteoporosis. It has been found to have caner chemopreventive activity in laboratory animals and antiproliferative effecs in human breast cancer.

Anzano MA, Peer CW, Smith JM et al. J Natl Cancer Inst. 88:123-5 (1996).
Dowsett M, Bundred NJ, Decensi A et al. Cancer Epidemiol Biomarkers Prev. 10:961-6 (2001).
Seeman E. J Bone Miner Metab. 19:65-75 (2001).

An angiotensin-converting enzyme (ACE) inhibitor. Ramipril is a prodrug of the active metabolite ramiprilat which is formed upon absorption.

Warner GT, Perry CM. Am J Cardiovasc Drugs. 3:113-6 (2003).

A frog skin peptide that interferes with nociception by action on the D2 receptor.

Zhu HZ, Ji XQ, Wu SX et al. Chung Kuo Yao Li Hseuh Pao. 12(4):291-293 (1991).

A histamine H2-receptor antagonist used in the treatment of gastrointestinal lesions due to excessive gastric acid secretion.

Grant SM, Langtry HD, Brogden RN. Drugs. 37:801-70 (1989).
Boyd EJ, Wilson JA, Wormsley KG. J Clin Gastroenterol. 5 Suppl 1:133-41 (1983).

A novel metabolic modulator and membrane stabilizer. It is an antiischaemic and antianginal agent. Shifts myocardial energy metabolism away from free fatty acids and toward glucose as the substrate for production of adenosine triphosphate.

Schofielf RS, Hill JA. Expert Opin Investig Drugs. 11:117-23 (2002).
McCormack JG, Barr RL, Wolff AA et al. Circulation. 93:135-42 (1996).
Lodge JP, Lam FT, Perry SL et al. Transplantation. 50:755-9 (1990).

An antifungal antibiotic that has immunosuppressive activity. It blocks cytokine-mediated signal transduction pathways.

Singh K, Sun S. Vezina C. J Antibiot (Tokyo). 32:630-45 (1979).
Sehgal SN. Ther Drug Monit. 17:660-5 (1995).

An antiulcer agent that enhances mucosal resistance. It increases endogenous prostaglandin in gastric mucosa, and also scavenges oxygen-derived free radicals and inhibits their production.

Otsubo K. Morita S. Uchida M et al. Chem Pharm Bull. 39:2906-9 (1991).
Iinuma S. Naito Y. Yoshikawa T et al. Dig Dis Sci. 43:35S-39S (1998).

(Core, NS3, NS4, NS5)

(gp41, "O"IDR, gp36)

(TpN15, TpN17, TpN44.5, TpN47)

Natrual product isolated from Euphorbia poisonii. RTX is an irritant to skin and mucous membranes, but not a tumor promoter. It is an extremely potent capsaicin analog that stimulates, with subsequent desensitization of specific subpopulations, sensory receptors.

Hergenhahn M, Kusumoto S, Hecker EJ. Cancer Res. Clin.Oncol. 108:98-109 (1984).
Szallasi A, Blumber PM, Life Sci. 47:1399-1408 (1990).
Dray A, Biochem. Pharm. 44:611-615 (1992).

ROPA is a hydrolysis product of resiniferatoxin. ROPA retains its strong skin irritant property. It is used to reconstitute either resiniferatoxin or tinyatoxin.

Jang M, Cai L, Udeani GO et al. Science, 275:218-220 (1997).
Carbo N, Costelli P, Baccino FM, Lopez-Soriano FJ. Biochem Ciophys Res Commun. 254:739-43 (1999).
Gautam SC, Xu YX, Dumaguin M et al. Bone Marrow Transplant. 25:639-45 (2000).

An antioxidant found in grapes, shown to have significant chemopreventive activity.

Jang M, Cai L, Udeani GO et al. Science. 275:218-220 (1997).
Carbo N, Costelli P, Baccino FM, Lopez-Soriano FJ. Biochem Ciophys Res Commun. 254:739-43 (1999).
Gautam SC, Xu YX, Dumaguin M et al. Bone Marrow Transplant. 25:639-45 (2000).

A vitamin A analog that inhibits cell proliferation and induces cell differentiation.

Kelloff GJ, Crowell JA, Hawk ET et al. J. Cell. Biochem Suppl. 26:54-71 (1996).
Zheng Y, Kramer PM, Olson G et al. Carcinogenesis. 18:2119-2125 (1997).

A vitamin A analog that inhibits cell proliferation and induces cell differentiation.

Kelloff GJ, Crowell JA, Hawk ET et al. J. Cell. Biochem Suppl. 26:54-71 (1996).

The active metabolite of vitamin A. A potential chemopreventive against skin, colon, and mammary tumors.

M Leid, Kastner P, Chambon P. Trends Biochem. Sci. 17:427-33 (1992).
Athar M, Agarwal R, Wang ZY et al. Carcinogenesis. 12:2325-9 (1991).
Stopera SA, Bird RP. Int. J. Cancer. 53:798-803 (1993).
Toma S, Isnardi L, Raffo P et al. Int. J. Cancer. 70:619-27 (1997).

Inhibits cell proliferation and induces cell differentiation.

Kelloff GJ, Boone CW, Crowell JA et al. Cancer Epidemiol. Biomarkers Prev. 3:85-98 (1994).

A vitamin A analog that inhibits cell proliferation and induces cell differentiation. A chemopreventive against rat mammary tumors.

Grubbs CJ, Eto I, Juliana MM et al. Anticancer Res. 10:661-666 (1990).

A vitamin A analog that inhibits cell proliferation and induces cell differentiation. Effective in lung cancer chemoprevention.

Pastorino U, Soresi E, Clerici, M et al. Acta Oncol. 27:773-782 (1988).

An inhibitor of eukaryotic cell growth. Shown to have a strong antitumor effect against human ovarian carcinoma BG-1.

Takahashi H, Yamashita Y, Takaoka H. Oncol Res. 9:7-11 (1997).
Osada H. Curr Med Chem. 10:727-732, (2003).

Antineoplastic agent.

Platelet aggregation inhibitor.

The 4-residue sequence found at the cell-adhesive region of the peptide vitronectin.

Lin HB, Garcia-Echeverria C, Asakura S et al. Biomaterials. 13:905-914 (1992).

A tetrapeptide structurally similar to RGDS. RGDS is a synthetic peptide that represents the fibroblast binding site of fibronectin. RGES is often used in fibroblast binding experiments.

Pasula R, Wisniowski P, Martin WJ 2nd. Infect Immun. 70:1287-92 (2002).

A synthetic peptide that represents the active site of a protein kinase.

Pattanaik A, Gowda DC, Urry DW. Biochem Biophys Res Commun. 178:539-45 (1991).

Induces apoptosis in cancer cell lines and inhibits transforming growth factor beta1 induced plasminogen activator inhibitor-1 in endothelial cells.

Zhu J, Liu Z, Huang H, Chen Z, Li L. Chin Med J (Engl).116:354-9 (2003).
Huang YH, Zhen YS. Yao Xue Xue Bao. 36:334-8 (2001).

Synthetic broad-spectrum antiviral nucleoside found to have antitumor activity on L1210 leukemia in mice. It regulates signal transduction in human ovarian cancer cells.

Li W, Shen F, Weber G. Oncol Res. 11:243-7 (1999).
Jolley WB, Chu WT, Salter JM. Ann N Y Acad Sci. 284:585-90 (1977).

Riboflavin deficiency causes formation of single strand breaks in nuclear DNA, increases carcinogen-DNA binding and decreases hepatic glutathione content.All of this can be reversed by riboflavin supplementation.

Webster RP, Gawde MD, Bhattacharya RK. Cancer Lett. 98:129-35 (1996).
Pangrekar J, Krishnaswamy K, Jagadeesan V. Food Chem Toxicol. 31:745-50 (1993).
Chiao CH, Chung Hua Chung Liu Tsa Chih.11:92-4 (1989).

Albendazole sulfoxide
Active metabolite of albendazole, an anthelmintic.

Castillo JA, Palomo-Canales J, Garcia JJ et al. Drug Dev Ind Pharm. 25:1241-8 (1999).

Rifampicin
An antibacterial from 3-formyl rifamycin SV.

Maggi et al. Chemotherapia. 11:285 (1966).

A derivative of rifamycins found to interact with biological membranes. It causes a change in permeability to K+ and H+ in the mitochondrial membrane.

Inouye B, Uchinomi Y, Wachi T, Utsumi K. J Antibiot (Tokyo). 30:494-9 (1977).

An antimicrobial agent, inhibits DNA polymerase.

Furesz S, Arioli V, Pallanza R. Antimicrob Agents Chemother. 5:770-7 (1965).
Frolova LY, Meldrays YA, Kochkina LL et al. Nucleic Acids Res. 4:523-38 (1977).

A rifamycin derivative. It is a non-absorbable broad-spectrum antibiotic that possesses in vitro activity against a wide range of bacteria. It acts by inhibiting bacterial ribonucleic (RNA) synthesis.

Prasad ES, Wenman WM. Diagn Microbiol Infect Dis. 16:135-6 (1993).
Gillis JC, Brogden RN. Drugs. 49:467-84 (1995).

Tuftsin-like tetrapeptide that stimulates phagocytosis activity. Rigin demonstrates high stress-protective activity in neuroendocrine and immune systems in rats. It stimulates release of interleukin-1 and tumor necrosis factor from mouse peritoneal macrophages and from human monocytes.

Rocchi R, Biondi L, Filira F, Tzehoval E, Dagan S, Fridkin M.Int J Pept Protein Res. 37:161-6 (1991).
Klusha VE, Mutsenietse RK, Svirskis ShV, Zalitis GM, Liepa IR. Biull Eksp Biol Med. 104:186-7 (1987).

Used for influenza A treatment and prevention.

Tominack RL, Hayden FG. Infect Dis Clin North Am. 1:459-78 (1987).

Rilutek
C8H5F3N2OS                    Mol. Wt.: 234.1983             [1744-22-5]
Has anticonvulsant activity and inhibits glutamate release. Has been used to treat amyotrophic lateral sclerosis.

Mantz, et al Anesthesiology 76:844 (1992).
van Kan HJ, Groeneveld GJ, Kalmijn S, Spieksma M, van den Berg LH, Guchelaar HJ Br. J. Clin. Pharmacol. 59:310-3 (2005).

A pyridinyl biphosphonate. It inhibits osteoclast-mediated bone resorption.

Boiser S, Ferreras M, Peyruchaud O, Magnetto S. Cancer Res. 60:2949-54 (2000).
Goa KL, Balfour JA. Drugs Aging. 13:83-91 (1998).

A biophosphonate that displays potent inhibition of bone resorption. Shown to prevent bone metastases in rats.

Muhlbauer RC, Bauss F, Schenk R. J Bone Miner Res. 6:1003-1011 (1994).

Ritodrina, Ritodrinium
C17H21NO3.HCl                    Mol. Wt.: 323.81             [23239-51-2]
Adrenergic b2-agonist that relaxes uterine muscle. It is used to stop premature labor.

Bassett JM, Symonds ME Am. J. Physiol. 275:R112-R119 (1998).

A dopamine receptor agonist commonly used to treat Parkinson disease and restless legs sydrome.

Gallagher G Jr, Lavanchy PG, Webster CA et al. J Med Chem. 28:1533-1536 (1985).
Anonymous, Health News. 10:2 (2004).

Natural product isolated from rosemary, sweet basal and perilla. It has anti-inflammatory activity and inhibits the proliferation of murine mesangial cells.

Makino T, Ono T, Muso E et al. Nephrol Dial Transplant. 15:1140-5 (2000).
Englberger W, Hadding U, Etschenberg E et al. Int J Immunopharmacol. 10:729-37 (1988).

A histamine H2-receptor antagonist used in ulcer treatment. Found to inhibit platelet function in vitro.

Brandstatter G, Marks IN, Lanza F et al. Clin Ther. 17:467-478 (1995).
Nakamura K, Kariyazono H, Shinkawa, T et al. Human Exptal Tox. 18: 487-492 (1999).

An antibiotic with a wide antibacterial spectrum against oral pathogens and an immunomodulatory effect. It has also been shown to increase neutrophil apoptosis, reduce tumor size of B16BL6 melanoma, and inhibit pulmonary metastasis of B16BL6 cells.

Yatsunami J, Tsuruta N, Fukuno Y et al. Clin Exp Metastasis. 17:119-24 (1999).
Oyama T, Sakuta T, Matsushita K et al. J Periodontal. 71:1546-53 (2000).

A tyrosine kinase-specific substrate often used in experiments to determine Tyr kinase activity.

Shen SS, Kinsey WH, Lee SJ. Dev Growth Differ. 41: 345-55 (1999).

Oridonin
A diterpene isolated from the leaves of Rabdosia rubescens Hora. It appears to have antitumor activity in cell culture studies.

Li XT, Lin C, Li PY. Chinese J Oncology. 8:184-186 (1986).
Fuji K, Node M, Sai M et al. Chem Pharmaceut Bull. 37:1472-1476 (1989).

A quinone antibiotic agent. Found to inhibit reverse transcrisptase from HIV-1 to a greater degree than it inhibits cellular DNA polymerase alpha.

Goldman ME, Salituro GS, Bowen JA et al. Mol. Pharmacol. 38:20-25 (1990).

A fluoroquinolone antibacterial that shows photosensitizing properties toward biological substrates. It inhibits B-cell differentiation in human mononuclear cells.

Gollapudi S, Perumal V, Thadepalli H, J Antimicrob Chemother. 29:669-76 (1992).
Condorelli G. De Guidi G, Giuffrida S et al. Photochem Photobiol. 70:280-6 (1999).

Rutecarpine
An alkaloid isolated from the chinese herb Evodia rutaecarpa. It has vasorelaxing effect and inhibits platelet aggregation and COX-2. It is a selective inhibitor of cytochrome P450 1A.

Chiou WF, Chou CJ, Liao JF et al. Europ J Pharm. 257:59-66 (1994).
Sheu JR, Hung WC, Lee YM, Yen MH. Europ J Pharm. 318:469-475 (1996).
Moon TC, Murakami M, Kudo I et al. Inflam Res. 48:621-625 (1999).
Ueng, YF., Jan, WC., Lin, LC. et al Drug Metab. Disp. 30:349-353 (2002).

A glycoside of quercetin. Inhibits the initiation and promotion stages of carcinogenesis, and enhances detoxification. An effective inhibitor of carcinogen-induced aberrant crypt foci in the rat colon.

Elangovan V, Sekar N, Govindasamy S. Cancer Lett. 87:107-113 (1994).
Wargovich MJ, Chen CD, Jimenez A et al. Cancer Epidimiol. Biomarkers Prev. 5:355-360 (1996).