D-Fagomine (1,2-dideoxynojirimycin) is a six-membered ring iminocyclitol that was first isolated from seeds of buckwheat (Fagopyrum sculentum Moench, Polygonaceae) and is also present in other plant sources such as mulberry (Morus Alba, Moraceae) leaves and gogi (Lycium chinense) roots. D-fagomine is present in common buckwheat-based foodstuffs in amounts ranging from 1 to 25 mg/kg or mg/L, it is stable during boiling, baking, frying and fermentation, and it is biosynthesised upon sprouting. The estimated total intake of D-fagomine resulting from a diet that includes such foodstuffs would be between 3 and 17 mg per day (mean for both genders; range from P5 to P95). In animal studies D-Fagomine lowers postprandial blood glucose. D-fagomine agglutinated Enterobacteriaceae (Escherichia coli, Salmonella enterica serovar Typhimurium), while it did not show this effect on Bifidobacterium spp. or Lactobacillus spp. D-fagomine significantly inhibited the adhesion of Enterobacteriaceae and promoted the adhesion of Lactobacillus acidophilus to intestinal mucosa. D-Fagomine did not show any effect on bacterial cell viability. D-fagomine may be used as a dietary ingredient or functional food component to reduce the health risks associated with an excessive intake of fast-digestible carbohydrates, or an excess of potentially pathogenic bacteria.

AZD-7687 is a potent inhibitor of Diacylglycerol O-acyltransferase 1 (DGAT1) which was developed by AstraZeneca for the treatment obesity and type 2 diabetes mellitus. AZD-7687 reached phase I of clinical trials, but was discontinued by unknown reasons.

Cobalt protoporphyrin (CoPP) is a potent HO-1 inducer and generally known to be an antioxidant in various cell types. CoPP has been shown to downregulate various cytochrome P450 isoforms, and various mechanisms of action have been attributed to its ability to induced HO- 1. It has also been used to promote endogenous carbon dioxide (CO) generation and protect against myocardial infarction in vivo. CoPP also participated in regulating the inflammatory response in CNS which mainly suppressed inflammatory component. It has been demonstrated that CoPP reduced LPS/Interleukin 13 (IL-13)-induced microglial death.

L-Arabinose is a monosaccharide extracted from plant gums, corn fiber and beet pulps. It is a poorly-absorbed, readily-available sweet-tasting pentose. L-Arabinose is known to suppress obesity by regulating the fasting blood glucose level and the insulin resistance index. L-arabinose is a non-caloric sugar. L-arabinose may inhibit intestinal sucrase activity and thereby delay sucrose digestion.

D-Psicose (akaD-allulose) is a low energy monosaccharide found throughout nature in small quantities. t is a c-3 epimer of D-fructose and has 50% the sweetness of sucrose. Possible health benefits include improved insulin resistance, antioxidant enhancement and formation, and hypoglycemic controls. The use US-FDA lists psicose as generally recognized as safe (GRAS) and has approved its use as a food additive in a wide variety of products. Psicose is not generally metabolized and does not raise blood sugar levels above baseline after consumption. In addition, to use as a low-calorie sweetener, psicose has also been formally investigated as a dietary supplement to control obesity and pre-diabetic insulin insensitivities. Furthermore, D-psicose has shown the ability to inhibit the proliferation of ovarian cancer cells in vitro.

Lipoprotein lipase (LPL) is a rate-limiting enzyme that hydrolyzes circulating triglyceride-rich lipoproteins such as very low-density lipoproteins and chylomicrons. Otsuka Pharmaceutical Factory, Inc. synthesized the LPL activator NO-1886 (ibrolipim, [4-(4-bromo-2-cyano-phenylcarbamoyl)-benzyl]-phosphonic acid diethyl ester, CAS 133208-93-2). NO-1886 increased LPL mRNA and LPL activity in adipose tissue, myocardium and skeletal muscle, resulting in an elevation of postheparin plasma LPL activity and LPL mass. It was discovered, that this agent has a potentially beneficial for the treatment of hypertriglyceridemia, hypo-HDL cholesterolemia, and protection from atherosclerosis. In addition, this agent may be used in the treatment of obesity and obesity-linked health problems in postmenopausal women.

MK-0557, trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro [6 azaisobenzofuran-1(3H),10-cyclohexane]-40-carboxamide, is an orally available Neuropeptide Y (NPY5) receptor antagonist. MK-0557 was studied in the clinical trials for the treatment of obesity, however, MK-0557 did not significantly increase the weight loss efficacy. MK-0557 safety and effectiveness were studied in a trial for the treatment of cognitive impairment in patients with schizophrenia. It seems MK-0557 development was discontinued.

Amitifadine is a novel, serotonin-preferring triple reuptake inhibitor with a relative potency to inhibit serotonin (5-HT), norepinephrine (NE), and dopamine (DA) reuptake. Amitifadine is most potent against the 5-HT transporter. Amitifadine did not cause marked inhibition of major CYP450 isoenzymes, and had a good safety margin at the hERG ion channel. Initial clinical trial in patients with severe major depression demonstrated significant antidepressant activity with amitifadine, including attenuating symptoms of anhedonia, and a tolerability profile that was comparable to placebo. Amitifadine did not increase any sexual side effects as well as weight gain. It’s in phase III clinical trial for the treatment of Major depressive disorder.

Lapachone (aka beta-Lapachone) is an ortho naphthoquinone, originally isolated from a tree whose extract has been used medicinally for centuries. It has garnered interest as a potential therapeutic or lead compound against a number of disease conditions including cancers, and blindness due to retinopathy of prematurity. It is lethal to a number of cancer cell types at micromolar concentrations, and it is capable of enhancing the efficacy of radiation therapies against cultured cells. A number of clinical trials have been conducted.

Metamfepramone (dimethylcathinone, dimethylpropion, and dimepropion) was synthesized by various routes in the 1930s and 1940s and clinically evaluated as anorectic as well as a treatment of hypotension and symptoms of the common cold. It was widely used for the treatment of the common cold or hypotonic conditions. Due to its stimulating properties and its rapid metabolism resulting in major degradation products such as methylpseudoephedrine and methcathinone, it has been considered relevant for doping controls by the World Anti-Doping Agency (WADA). Metamfepramone was marketed as an appetite suppressant, but was made illegal in 2006.