1. Rhynchophylline and isorhynchophylline act as noncompetitive antagonists of the NMDA receptor and that this property may contribute to the neuroprotective and anticonvulsant activity of the Uncaira species plant extracts.
2. Rrhynchophylline suppresses inflammatory responses of microglia and may act as a potential therapeutic agent for various neurodegenerative diseases involving neuroinflammation.
3. Rhynchophylline and uncaria rhynchophylla have antiepileptic effects in KA-induced seizures and are associated with the regulation of the innate immune system via a reduction in the level of superoxide anions, JNK phosphorylation, and NF-kappaB activation.
4. Rhynchophylline can reduce cardiac dysfunction and improve survival via suppression of macrophage I-κBα phosphorylation in LPS-challenged mice, and suggest that it may be a potential agent for the treatment of septic cardiac dysfunction.
5. Rhynchophylline can markedly inhibit rabbit platelet aggregation induced by ADP or thrombin possibly by depressing the inflow of Ca2+ and the rise of the cytoplasmic free calcium level in platelet.
6. Rhynchophylline can reduce the systolic blood pressure (SBP) of spontaneously hypertensive rats (SHR) significantly, decrease plasma Ang II, ADMA, and AT1R levels, and promote serum NO and NOS levels, which has the protection of vascular endothelial function.
1. Resibufogenin is a cytotoxic steroid isolated from the Chinese drug ChanSu.
2. Resibufogenin can inhibit rectifier potassium current ( I K ) and transient potassium current ( I A ), it has pathological effects on central nervous system.
3. Resibufogenin corrects hypertension in a rat model of human preeclampsia, it not only prevents the advent of hypertension and proteinuria, but also the development of intrauterine growth restriction.
4. Resibufogenina's major metabolic pathway in the human liver is CYP3A4 dominantly mediated 5β-hydroxylation .
1. Pregabalin (30 and 100mg/kg) presents central spinal but not central supraspinal antinociceptive effect and Pregabalin 100mg/kg shows peripheral antinociceptive effect.
2. Postoperative administration of Pregabalin provided significant relief of postoperative shoulder pain during earlier POD after thoracic surgery for lung cancer when received multimodal analgesia in combination with NSAIDs.
3. Pregabalin, a potent anticonvulsant agent, is used in treatment-resistant epileptic patients.
4. Pregabalin may be effective for the reduction of neuropathic pain, it improves postoperative analgesia compared with placebo at the expense of increased sedation and visual disturbances.
1. Alpha-Spinasterol has anti-inflammatory activity.
2. Alpha-Spinasterol is a novel efficacious and safe antagonist of the TRPV1 receptor with antinociceptive effect.
3. Alpha-Spinasterol can prevent TP-induced prostatic hyperplasia and may be beneficial in the management of benign prostatic hyperplasia.
4. Alpha-Spinasterol is a potent inhibitor (IC(50)= 3.9 x 10 (-12) g/mL, 9.5 pmol/L) of glomerular mesangial cell proliferation caused by high-ambient glucose (5.6 mM vs. 25 mM), it has a significant therapeutic potential to modulate the development and/or progression of diabetic nephropathy.
1. Trans-Caryophyllene has a novel role in regulating GSIS in pancreatic β-cells.
2. Trans-Caryophyllene is PPAR-α agonist thus regulates cellular lipid metabolism in PPAR-α dependent manners.
3. Trans-Caryophyllene has neuroprotective effects in various neurological disorders, such as chemical induced seizure and brain damage.
4. Trans-Caryophyllene reduces both acute and chronic pain in mice, which may be mediated through the opioid and endocannabinoid systems.
5. Trans-Caryophyllene suppresses the hypoxia-induced neuroinflammatory response through inhibition of NF-κB activation in microglia, suggests be beneficial in preventing hypoxia-induced neuroinflammation.