Hypaphorine is the alkaloid isolated from the seeds of Brazilian medicinal plant Erythrina spp. This compound was investigated for sleep-promoting effects in mice, and the results showed that it significantly increased non-rapid eye movement (NREM) sleep time during the first hour after its administration. Hypaphorine prevented the differentiation of 3T3-L1 preadipocytes into adipocytes by down-regulating hormone-stimulated protein expression of peroxisome proliferator activated receptor γ (PPARγ) and CCAAT/enhancer binding protein (C/EBPα), and their downstream targets, sterol regulatory element binding protein 1 c (SREBP1c) and fatty acid synthase (FAS). Hypaphorine may exert anti-inflammatory actions through the regulation of TLR4 and PPAR-γ dependent on PI3K/Akt/mTOR signal pathways. It is considered as a therapeutic agent that can potentially relieve or ameliorate endothelial inflammation-associated diseases. Hypaphorine was also a key component of Vaccaria segetalis. Vaccaria hypaphorine might be considered as a potential therapeutic agent for treating osteoclast-based bone loss.

2-methyl-4,6-dinitrophenol (4,6-Dinitro-ortho-cresol, DNOC) is a yellow crystalline solid. DNOC is used agriculturally as a larvicide, ovicide and insecticide (against locusts and other insects) as well as a potato haulm desiccant. It is also used as a polymerization inhibitor and as an intermediate in the chemical industry. For agricultural uses, DNOC is mainly formulated as emulsifiable concentrate, either aqueous or oily. 4,6-Dinitro-o-cresol is an uncoupler of the mitochondrial respiratory system. It causes an increase in basal metabolic rate with raised temperature and weight loss in man and animals. After metabolic activation, 4,6-dinitro-o-cresol has mutagenic potential in vitro. In vivo, evidence of clastogenic effects was obtained with a herbicide containing 4,6-dinitro-o-cresol but not with the pure substance. A long-term study with rats yielded no evidence of carcinogenic effects. During the 1930s, DNOC, along with dinitrophenol, was used therapeutically as a weight-loss agent after animal experiments had demonstrated that dinitrophenols increased the basal metabolic rate (BMR). The earliest mention of the use of these compounds for weight loss is a publication by Cutting and Tainter (1933) in which the authors reported clinical studies of dinitrophenol for this purpose. Dodds and Robertson (1933) reported that the related compound, DNOC, exhibited a greater effect on metabolism than dinitrophenol, leading to the marketing of DNOC for weight loss. Following the publication of these reports, dinitrophenol, and to a lesser extent, DNOC, began selling in drug stores and was prescribed by physicians for weight loss. DNOC acts mainly as an inhibitor of oxidative phosphorylation at the mitochondrial level, inducing a significant increase in basal metabolism and hyperthermy. The oxidation of carbohydrate forms the main source of energy of the body and the energy is “stored” in the form of compounds containing phosphate (high energy phosphate bonds of adenosine triphosphate or ATP). This compound is then a source of energy to the body. DNOC inhibits the formation of ATP. In the presence of DNOC the oxidative process continues and is even increased, but the energy cannot be converted to a useable form and it is therefore dissipated as heat. In muscle ATP cannot be re-synthesized and is progressively broken down to adenylic acid. The shortage of ATP may lead to muscular paralysis which for critical organs, such as heart and respiratory muscles, includes a blocking of their vital functions and in the case of death by DNOC poisoning, to early rigor mortis.

ASARININ, (+)- ((+)-episesamin), an abundant lignan in sesame seed, has been identified as an active principle in an aqueous extract of Lindera obtusiloba (Japanese Spicebush) with a strong anti-inflammatory potential. (+)-episesamin (ES) is known to block the TNF-α-induced mitogenic VSMC response. Protective effect of (+)-episesamin against PDGF-BB-induced activation of vascular smooth muscle cells is mediated by induction of haem oxygenase-1 and inhibition of mitogenic signalling. ES interferes with inflammation-associated VSMC activation and subsequent decreased proliferation and migration due to anti-oxidative properties and impaired activation of NF-ĸB, known contributors to atherogenesis. These results suggest ES as a complemental treatment of VSMC specific vascular diseases such as atherosclerosis. (+)-Episesamin inhibits adipogenesis and exerts anti-inflammatory effects in 3T3-L1 (pre)adipocytes by sustained Wnt signaling, down-regulation of PPARγ and induction of iNOS. (+)-episesamin seems to be the active drug in the L. obtusiloba extract being responsible for the inhibition of adipogenesis and, thus, should be evaluated as a novel potential complementary treatment for obesity.

Dehydroabietic acid (DHA or DAA), a diterpene, is obtained from Commiphora oppbalsamum. DHA has potential as treatment for obesity and metabolic syndrome, obese diabetic KK-Ay mice treated with DHA showed decreased plasma glucose, insulin, and triglyceride levels. It has been reported that DHA inhibits the production of proinfammatory mediators such as TNF-α in macrophages and adipocytes and causes endothelium-dependent relaxation of pulmonary artery via PI3K/Akt-eNOS signaling pathway. Also was shown, that DHA could reverse several cell responses stimulated by TNF-α, including the activation of FOXO1 and the TGF-β1/Smad3 signaling pathway. Thus, DAA could be useful in improving the diabetic wound healing.

(+)-DDMS (R-Didesmethylsibutramine , (R)-DDMS) is one of sibutramine active metabolites. Sibutramine is widely used in the treatment of obesity. Sibutramine acts by inhibiting the reuptake of serotonin and noradrenaline in synapses, thereby enhancing both satiety and energy expenditure. In preclinical models (R)-enantiomer of Didesmethylsibutramine was clearly more potent than the (S)-enantiomers and (R)-didesmethylsibutramine shows some activity in all tests. (S)-didesmethylsibutramine affected locomotor behavior and the Porsolt test but appeared to be completely inactive on food intake. R-Didesmethylsibutramine is more potent than sibutramine in depressing food intake and decreasing body weight, suggest that these enantioselective metabolites might be safer and more effective than sibutramine as potential therapies for obesity.

Lorcaserin, currently marketed under the trade name Belviq and previously Lorqess during development, is a weight-loss drug developed by Arena Pharmaceuticals. Lorcaserin is a selective 5-HT2C receptor agonist, and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets. 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion, the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor

Lorcaserin, currently marketed under the trade name Belviq and previously Lorqess during development, is a weight-loss drug developed by Arena Pharmaceuticals. Lorcaserin is a selective 5-HT2C receptor agonist, and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets. 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion, the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor

Lorcaserin, currently marketed under the trade name Belviq and previously Lorqess during development, is a weight-loss drug developed by Arena Pharmaceuticals. Lorcaserin is a selective 5-HT2C receptor agonist, and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets. 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion, the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor

Subitramine is a potent inhibitor of monoamines (serotonin, dopamine, noradrenaline) reuptake that was approved by FDA for the treatmen of obesity. Sibutramine is metabolized to metabolites M1 and M2 which are more active toward the monoamine transporters.The drug was withdrawn from the market because of clinical trial data indicating an increased risk of heart attack and stroke. It was sold under a variety of brand names including Reductil, Meridia and Sibutrex.

Subitramine is a potent inhibitor of monoamines (serotonin, dopamine, noradrenaline) reuptake that was approved by FDA for the treatmen of obesity. Sibutramine is metabolized to metabolites M1 and M2 which are more active toward the monoamine transporters.The drug was withdrawn from the market because of clinical trial data indicating an increased risk of heart attack and stroke. It was sold under a variety of brand names including Reductil, Meridia and Sibutrex.