U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 31 - 40 of 209 results

Corydaline is a pharmacologically active isoquinoline alkaloid isolated from Corydalis tubers. It exhibits the antiacetylcholinesterase, antiallergic, antinociceptive, and gastric emptying activities. Corydaline exhibited strong nematocidal activity, showed little cytotoxicity and represents a potential treatment for Strongyloidiasis. Corydaline exhibits gastrointestinal modulatory, antinociceptive, anti-allergic, and anti-parasitic activities. Corydaline is currently in clinical trials as a potential treatment for functional dyspepsia. In animal models, corydaline increases gastric emptying and small intestine transit speed and induces gastric relaxation. In other animal models, corydaline inhibits chemically-induced pain. Additionally, this compound may inhibit mast cell-dependent smooth muscle contraction of the aorta. Corydaline also exhibits nematocidal activity against species of Strongyloides.
(R)-Bambuterol is a selective β2-adrenoceptor agonist. R-Bambuterol Hydrochloride Tablets ("Laevo-Bambuterol") is categorized as a Class 1 new drug. Its preclinical studies show that it is more effective and have lower toxicity than Bambuterol, a popular asthma drug currenTLy on the market. Laevo-Bambuterol was approved by the China Food and Drug Administration for the treatment of asthma.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Wikstromol is the enantiomer of nortrachelogenin, isolated from Trachelospermum asiaticum var. intermedium and Pinus palustris. Wikstromol exhibited acetylcholinesterase (AChE) inhibitory. It has been found to be active against P-388 lymphocytic leukemia growth implanted in mice. The reason for this is at present unclear, although it is possible that wikstromol is either metabolized to an active antileukemic agent by the host or else serves as a biological response modifier.
Scutellarin is the main bioactive component of Breviscapine prepared from the traditional Chinese herb Erilgeron breviscapus (Vant) Hand-Mazz. Scutellarin demonstrated protective effect on cardiovascular and cerebrovascular ischemia. The potential cytoprotective effects of the drug against cerebrovascular ischemia were evidenced by reducing cerebral infarct sizes, ameliorating neurological deficit and inhibiting neuronal apoptosis. Scutellarin is capable of inhibiting I(Na) in neurons through predominantly affecting the inactivated state of I(Na). Scutellarin may alleviate cognitive impairment in a mouse model of hypoxia by promoting proliferation and neuronal differentiation of neural stem cells. Scutellarin might play an therapeutic role by inhibiting oxidative stress and apoptosis in Alzheimer's disease treatment.
Kalopanaxsaponin B is the main component of stem bark of Kalopanax pictus Nakai (KP, family Araliaceae), which has been used for inflammation in Chinese traditional medicine. Kalopanaxsaponin B also exhibits pro-cognitive action in mouse models of memory deficit.
Beauvericin is a famous mycotoxin produced by many fungi, such as Beaveria bassiana and Fusarium spp. Beauvericin is a cyclic hexadepsipeptide (Figure 1) that belongs to the enniatin antibiotic family. It contains three D-hydroxyisovaleryl and three N-methylphenylalanyl residues in an alternating sequence. Beauvericin was first isolated from Beaveria bassiana, which is a common and commercial entomopathogenic mycoinsecticide. Beauvericin was one of the active constituents of B. bassiana and was confirmed to have antimicrobial and anti-tumor activities. Beauvericin has a strong antibacterial activity against human, animal and plant pathogenic bacteria with no selectively between Gram-positive and Gram-negative bacteria. The cytotoxicity of beauvericin to human tumor cells has been frequently reported.
Cholesteryl hemisuccinate (CHEMS) is an acidic cholesterol ester. It self-assembles into bilayers in alkaline and neutral aqueous media. CHEMS exhibits pH sensitive polymorphism. It consists of succinic acid esterified to the beta-hydroxyl group of cholesterol. It was shown; that CHEMS was potent inhibitors of acetylcholinesterase and it alone or in combination with tetrahydroaminoacridine could be used in the treatment of organophosphate poisoning and Alzheimer's disease. It was also revealed, that CHEMS upon incorporation into the cell membrane, which presumably promotes the expression of latent tumor-associated antigens, induced a marked increase in specific immunogenicity of tumor cells.
Estragole (ES) is a natural constituent of a number of plants (e.g. tarragon, sweet basil and sweet fennel) and their essential oils have been widely used in foodstuffs as flavouring agents. Estragole ES was given GRAS Generally Recognized As Safe status by the Flavor and Extract Manufacturer’s Association FEMA, 1965 and is approved by the Food and Drug Administration for food use 21 CFR code of Federal Regulation 121.1164 . Several studies with oral, i.p. or s.c. administration to CD-1 and B6C3F1 mice have shown the carcinogenicity of ES. In vivo and in vitro experimental assays have shown that EST has sedative, anticonvulsant, antioxidant, antimicrobial, and anesthetic activity.