Botanical Source

Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator. Icariin has been reported to have anti-hypoxic, phytoestrogenic, anti-osteoporotic, anti-inflammatory, neuroprotective, and anti-depressant-like activities. Icariin is effective in the attenuation of AHR and chronic airway inflammatory changes in OVA-induced murine asthma model, and this effect is associated with regulation of Th17/Treg responses. Icariin inhibited NF-κB signaling activation and the NLRP3-inflammasome/caspase-1/IL-1β axis.

Momordicoside K is a triterpenoid saponin, which is derived from the bitter melon plant, scientifically known as *Momordica charantia*. This compound predominantly occurs in the fruit and leaves of the plant. As a phytochemical, Momordicoside K contributes to the plant’s defense mechanisms against pests and environmental stress. The mode of action of Momordicoside K involves modulating various biochemical pathways. It is known to exert potential anti-inflammatory and antidiabetic effects by influencing cellular pathways and enzyme activities associated with glucose metabolism and inflammation. These modulatory effects make it a compound of interest in the development of therapeutic strategies for metabolic disorders. Momordicoside K is primarily studied for its uses in the management and treatment of diabetes, given its ability to improve glucose uptake and insulin sensitivity. Additionally, its anti-inflammatory properties hold promise for treating inflammatory-related conditions. Research continues to explore its full potential, including any synergistic effects with other phytochemicals and its overall efficacy in clinical applications.

In vitro, procyanidin C1 (PC1) dose-dependently decreased Fc epsilon RI-mediated degranulation and cytokine production of mast cells, inhibited tyrosine phosphorylation of Syk and linker for activation of T cells, and the ROS generation in stimulated mast cells.PC1 suppresses Fc epsilon RI-mediated mast cell activation by inhibiting intracellular signaling pathways, These observations provide evidence for the anti-allergenic effects of the procyanidin-enriched apple extract.

Berberine hydrochloride (berberine), a natural plant alkaloid derived from Chinese herbal medicine, is characterized by diverse pharmacological effects, such as anticancer and lower elevated blood glucose, it can prevent adhesion by downregulating ICAM-1 and reduce inflammation by inhibiting the TAK1/JNK and TAK1/NF-κB signaling after abdominal surgery, which brings out a good therapeutic approach for the development of clinical application for postoperative abdominal adhesion and inflammation.

Matrine, an alkaloid purified from the chinese herb Sophora flavescens Ait, is well known to possess activities including anti-inflammation, anti-fibrotic and anticancer, it could inhibit cell proliferation and induce apoptosis of SGC-7901 cells in vitro by up-regulating Fas/FasL expression and activating caspase-3 enzyme.

Qingyangshengenin is a a glycoside from the roots of Cynanchum otophyllum.

Aescin monosodium salt is a semisynthetic, anti-inflammatory product derived from escin, which is a mixture of saponins extracted from horse chestnut seeds (Aesculus hippocastanum). It functions primarily by enhancing the integrity of venous walls and decreasing vascular permeability. This is achieved through the stabilization of lysosomal membranes and the inhibition of enzymes that contribute to the breakdown of the vascular endothelium, as well as promoting the release of prostaglandins with vasoprotective properties. Aescin monosodium salt is utilized in scientific research and medicinal applications for its efficacy in treating conditions associated with impaired venous circulation and edema. It is often applied in studies focusing on chronic venous insufficiency, varicose veins, and in reducing postoperative or traumatic swelling. Its roles in modulating inflammatory responses and improving capillary resistance make it a valuable compound in exploring cardiovascular and anti-inflammatory therapeutics.

Forsythoside B inhibits inflammatory response, has antioxidant, antisepsis properties, and also has potent neuroprotective effects with a favorable therapeutic time-window, reduce of cerebral ischemia and reperfusion injury degree, attenuating blood-brain barrier (BBB) breakdown. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.

Camelliaside B is a bioactive compound, which is a glycosylated flavonoid derived from the leaves of *Camellia sinensis*, the tea plant. It functions through its antioxidant properties, scavenging free radicals and reducing oxidative stress in biological systems. The molecular structure of Camelliaside B allows it to interact with cellular components, providing protective effects against reactive oxygen species. The compound is of significant interest in pharmaceutical and nutraceutical research due to its potential health benefits. Its applications span a range of uses, including the development of supplements for improving cardiovascular health, enhancing neuroprotection, and reducing inflammation. Additionally, it is explored for its ability to synergize with other natural compounds, enhancing the overall efficacy of complex formulations. Scientists are continuing to investigate its molecular interactions and potential therapeutic roles in various chronic conditions.

Ziziphin is a triterpene glycoside which exhibits taste-modifying properties and derives from the leaves of Ziziphus jujuba (Rhamnaceae). In a study, Ziziphin was up to 4 times more active in suppressing the sweet taste of sucrose than other anti-sweet constituents (Suttisri, 1995). Ziziphin suppressed the sweetness induced by D-glucose, D-fructose, stevioside, glycine, sodium saccharin, aspartame and naringin dihydrochalcone. Ziziphin however showed no uppressive effect on the sour taste of hydrochloric acid and the bitter taste of quinine, indicating that ziziphin is highly specific to the sweet taste (Kurihara, 1992). Ziziphin was found to inhibit the sweet taste receptors in humans (Smith, 1983) by a mechanism known as taste modification. In comparison with known gymnemic acids, effects suggest that net dissociation of ziziphins from taste receptor membranes and/or inactivation in the membrane may be much faster than with gymnemic acids (Mahajan, 2009).

Dehydrotrametenolic acid is a promising candidate for a new type of insulin-sensitizing drug; it can be a potential anticancer agent against H-ras transformed tumor.

Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.

Hydroxy-alpha-sanshool exerts antiobesity and hypolipidemic activities in HFD rats by reducing liver oxidative stress and thus could be considered as a potential candidate drug to cure or prevent obesity and hyperlipidemia. It also has analgesic properties, it activates TRPV1 and TRPA1 in sensory neurons.

Baicalin methyl ester shows inhibitory effects on the Avian Myeloblastosis Virus reverse transcriptase (AMV-RT).

Wilforine has anti-inflammatory effect, which might be mediated by down-regulation of the expression of inflammatory factors TNF-α, IL-6 and NO. It also has insecticidal activity by inhibiting the Na+-K+-ATPase in the central nervous system.

Alisol B, a novel inhibitor of the sarcoplasmic/endoplasmic reticulum Ca(2+) ATPase pump, induces autophagy, endoplasmic reticulum stress, and apoptosis.Alisol B may be a potential novel therapeutic molecule for bone disorders through targeting the differentiation of osteoclasts as well as their functions. Alisol B also inhibited RANKL-induced expression of NFATc1 and c-Fos, which are key transcription factors for osteoclastogenesis.

Isoliensinine has anti-cancer, anti-fibrosis, anti-proliferative, antioxidant, and anti-inflammatory activities, it inhibited TNF-alpha and TGF-beta 1; decreased the overexpression of growth factors Platelet-derived growth factor (PDGF)-beta, basic fibroblast growth factor (bFGF), proto-oncogene c-fos, c-myc and hsp70; and activated ROS and p38 MAPK/JNK .

Glycyrrhizic acid has immunoregulatory function,it(up to 100 mg/ml) can inhibit interleukin-6 and elevate interleukin-10 production in lipopolysaccharide-activated macrophages, and significantly inhibit proliferation of spleen lymphocytes; rectally administered glycyrrhizic acid has significant protective effects against TNBS-induced colitis in rats.

Genkwanin has antitumor, and anti-inflammatory activities, it enhances host immunity, decreases the inflammatory cytokine levels, and regulates the miR-101/MKP-1/MAPK pathway.Genkwanin may have anti-skin ageing activity, it can up-regulate the transcriptional activation of human type vii collagen gene promoter, stimulating the formation of anchoring fibrils at the basement membrane zone in skin contributed to preventing skin ageing; it also induces a decrease of melanin synthesis by inhibiting tyrosinase activity, it could as skin whitening agent in cosmetic preparations.

Eupatilinthe has anti-proliferative effect in MCF10A- ras cells, is associated with its blockade of cell cycle progression which appears to be attributable in part to inhibition of ERK1/2 activation.

Calycosin-7-O-β-d-glucoside(CG) treatment can significantly reduce infarct volume, histological damage and BBB permeability in the in vivo MCAO ischemia-reperfusion rat model; inhibit the expression and activities of MMPs, and secure the expression of cav-1 and tight junction proteins in the microvessels isolated from ischemic rat cortex; scavenge NO, inhibit the activities of MMP-2 and MMP-9, and attenuate cell death in the in vitro cultured brain microvascular endothelial cells under OGD condition; thus CG could protect BBB integrity in experimental cerebral ischemia-reperfusion injury via regulating NO/cav-1/MMPs pathway.

Epimedin A,epimendin B, epimendin C, icariin and baohuoside are flavonoids, main active ingredient in Epimedium, have clear anti-osteoporosis effect, the accumulation of epimedins A, B, C, and icariin in a traditional medicinal plant could be suppressed by light stress.

Lithospermic acid (LSA) was originally isolated from the roots of Salvia mitiorrhiza ,

Periplogenin plays protective roles against thyrotoxicosis and associated cardiovascular problems, are mediated through its direct antithyroidal and/or LPO inhibiting properties. Periplogenin induces necroptotic cell death through oxidative stress in HaCaT cells and ameliorates skin lesions in the TPA- and IMQ-induced psoriasis-like mouse models.

Anemoside B4(AB4) and tetrandrine(Tet) have some reversal effect on resistant to L-OHP in Lo Vo/L-OHP cells, the molecular mechanism of the resistance reverse effect was related to down-regulation of P-gp for AB4 and down-regulation of z DHHC9 for Tet.

Isoescin IB is a natural product from Aesculus hippocastanum L.

Chicoric acid, a new compound able to enhance insulin release and glucose uptake, it is a new potential antidiabetic agent carrying both insulin sensitizing and insulin-secreting properties. Chicoric acid has antiobesity effects, it can induce apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. L-Chicoric acid has antiviral activity against HIV-1, which has been attributed to the inhibition of HIV-1 integration.

Epimedin A is a naturally occurring flavonoid glycoside, which is a type of compound found in certain plants, specifically within the Berberidaceae family. The primary source of this compound is the plant genus Epimedium, commonly known as Horny Goat Weed. Epimedin A acts by influencing various biological pathways, primarily modulating nitric oxide levels and influencing the signaling pathways associated with cellular proliferation and differentiation. Epimedin A has garnered scientific interest due to its potential uses and applications in the fields of pharmacology and biochemistry. It has been studied for its possible roles in enhancing bone density, which may be beneficial in the treatment of osteoporosis. Additionally, its effects on modulating cardiovascular function and its possible antioxidant properties have been explored. While research is still ongoing to fully elucidate its mechanisms and therapeutic potential, Epimedin A presents an intriguing candidate for further study in the development of novel therapeutic agents targeting age-related and degenerative conditions.

Phellodendrine chloride has anti-nephritic activity, may be due to its ability to inhibit the proliferation or the migration of macrophages and cytotoxic T lymphocytes in the glomeruli.

Afzelin, isolated from Cornus macrophylla, has antibacterial effects on Pseudomonas aeruginosa, its minimum inhibitory concentration (MIC) is 31 μg/mL.