Arctigenin is a plant lignan extracted from Arctium lappa that has been shown to have estrogenic properties. In ER-positive MCF-7 cells, arctigenin efficiently inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cell migration and invasion. Arctigenin confers anti-metastatic effects by inhibiting MMP-9 and uPA via the Akt, NF-κB and MAPK signaling pathways on breast cancer, regardless of ER expression. Intake of arctigenin could be an effective supplement for breast cancer patients. Arctigenin is a phenylpropanoid dibenzylbutyrolactone lignan compound possessing antitumor, anti-inflammatory, anti-influenza, antioxidant, antibacterial, and hypoglycaemic activities. Arctigenin exhibited significant antiproliferative activity against CCRF-CEM cells after 72 h treatment with IC50 values of 1.21 ± 0.15 um. It arrested CCRF-CEM cells in the S phase. It induced apoptosis in CCRF-CEM cells in a concentration- and time-dependent manner. Arctigenin is a good candidate for the development of novel agents against T-cell lymphoma. Arctigenin has been found to act as an agonist of adiponectin receptor 1 (AdipoR1). Arctigenin is an antagonist of MR and effectively decreases the Na/K-ATPase 1 gene expression, thus highlighting its potential as an anti-hypertensive drug lead compound.

Zolertine is an alpha-adrenergic receptor antagonist that acts as an antihypertensive agent. Its effect was studied in animals in vivo and in vitro. Zolertine considerably decreased systemic blood pressure in mecamylamine hypertensive dogs in a dose-related fashion. Using the intravital microscopic method in rat's mesocygeus microvasculature a direct relationship between zolertine dosage and blockade was demonstrated as well as an inverse relationship between time of action of zolertine and percentage of vasoconstriction caused by noradrenaline. When only zolertine was applied, it caused a small vasoconstriction that decreased as its concentration increased which could be due to its ability to antagonize alpha receptor responses, but not beta responses. Zolertine is a more active alpha blocker than azapetin, a blocker used in medical practice. Competition binding experiments using the alpha1-adrenoceptor antagonist [3H] prazosin showed a zolertine pKi of 6.81 +/- 0.02 in rat liver (alpha1B-adrenoceptors) and 6.35 +/- 0.04 in rabbit liver (alpha1A-adrenoceptors) membranes. Zolertine showed higher affinity for alpha1D-adrenoceptors compared to alpha1A-adrenoceptors, while it had an intermediate affinity for alpha1B-adrenoceptors. The ability of the alpha1-adrenoceptor antagonist zolertine to block alpha1D-adrenoceptor-mediated constriction in different vessels of Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats may explain its antihypertensive efficacy despite its low order of potency.

Etiocholanone is an androstane neurosteroid. Etiocholanone potentiates GABA-A receptor currents and exerts anticolvunsant properties in rodents. Etiocholanolone demostrates pyrogenic properties.

Monatepil is a calcium antagonist that, as do existing calcium antagonists, inhibits the influx of extracellular Ca 2 + through voltage-dependent Ca 2 + channels. It is a new type of antihypertensive agent. Its unique chemical structure was specially designed with intrinsic calcium antagonist and a1 -adrenoceptor-blocking moieties, creating a dual mechanism of action. Positive effects on plasma lipid metabolism are derived from the a1 -adrenoceptor-blocking activity and the antiatherosclerotic effect derives from the calcium antagonist properties. The novel structure of monatepil produces a slow onset of action and a long-lasting antihypertensive effect in experimental animals.

Lemildipine is a 1,4-dihydropyridine calcium channel blocker which is under phase III development by Banyu (Merck and Co), in Japan, for its potential to treat hypertension and cerebrovascular ischemia. In one study, involving five patients with essential hypertension accompanied by cerebrovascular disorder, lemildipine, administered orally at doses of 5 to 20 mg/day, significantly lowered blood pressure and increased cerebral blood flow. Another study in 31 patients with essential hypertension demonstrated that lemildipine has significant pressure lowering effects without affecting serum lipids. Worldwide rights to market the drug have been assigned to Kowa in Japan.

Carmoxirole is a dopamine D2 receptor agonist with limited central activity that modulates sympathetic activation and subsequently reduces pre-load and afterload in animals. It was shown, that carmoxirole induced beneficial effects on hemodynamic and neurohumoral parameters in heart failure. In addition, experimental evidence showed that carmoxirole lowered blood pressure in various models of hypertension mainly or exclusively through inhibition of noradrenaline release from sympathetic nerve endings. That effect of carmoxirole was mediated by presynaptic dopamine receptors with the characteristic that release inhibition was restricted to low rates of sympathetic nerve discharge.

Teprotide, a nonapeptide isolated from the venom of a Brazilian pit viper, Bothrops jararaca, was the first angiotensin converting enzyme (ACE) inhibitor to be discovered and tested. It was found to be an effective, non-toxic antihypertensive agent as well as an afterload-reducing agent for patients with congestive heart failure (CHF). The primary activity of teprotide resulted from blockade of the angiotensin I converting enzyme--the pivotal step in the renin-angiotensin-aldosterone system (RAAS), and consequent reductions in angiotensin II levels. There was limited clinical testing for teprotide because of: its scarcity; the need for parenteral administration; and the subsequent discovery and synthesis of captopril, the first orally active angiotensin converting enzyme inhibitor.

Iganidipin is a new dihydropiridynic derivative of calcium antagonist. It is the only currently available calcium antagonist in the form of ophthalmic solution. Its topical administration increases ipsilateral optic nerve head blood flow in rabbits and monkeys and inhibits the contraction of blood vessels induced by endothelin -1. Iganidipin is also used for treat Angina pectoris and Hypertension.

Cromakalim is an ATP-sensitive potassium (KATP) channel opener, which was studied for the treatment of gastric ulcer, hypertension and preventing a cardiomyopathy. But the development of this drug was discontinued due to heart lesions found in monkey chronic toxicity studies.

Fusaric acid (J-butylpicolinic acid) is a fungal toxin with low to moderate toxicity synthesized by some Fusurium species which cause infections in cereal grains and other agricultural commodities. It may potentiate the effects of other Fusurium toxins. Fusaric acid is a potent inhibitor of DNA synthesis. Fusaric acid has potent anti-proliferative activity in vitro on various normal and cancer cell lines and suggest that it exhibits some cytotoxic specificity for growing and confluent colorectal adenocarcinoma and mammary adenocarcinoma cell lines. Fusaric acid is known as a potent dopamine-beta-hydroxylase inhibitor of high specificity. Fusaric acid calcium salt elicited the hypotensive response primarily through the reduction of total peripheral vascular resistance index.