Phenylpropanoids

Isopimpinellin, an orally active compound isolated from Glomerella cingulata. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect.

Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC₅₀s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication. Isoscopoletin exhibits anti-inflammatory activity through inhibition of MAPK/NF-κB/STAT/AKT signaling pathway.

Caftaric acid (trans-Caftaric acid) is a polyphenolic antidiuretic, antioxidant and anti-apoptotic agent that can be hydrolyzed by intestinal microbial esterases. Caftaric acid exerts its antioxidant and potential anti-inflammatory effects mainly through intestinal microbial metabolism. Caftaric acid can reduce renal damage, restore electrolyte balance, renal function indicators and antioxidant enzyme activities in a rat albinism model, and further exert anti-oxidative stress and anti-inflammatory activities.

Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC₅₀ = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.

Purpureaside C, phenolic glycoside, is a minichromosome maintenance complex component 6 (MCM6) inhibitor. Purpureaside C binds to the ATP-pocket of MCM6, suppresses MCM6 protein expression in gastric cancer cells. Purpureaside C suppresses gastric cancer cell growth and induces apoptosis. Purpureaside C exerts antibacterial activity and proinflammatory activity. Purpureaside C can be used for the researches of gastric cancer, bacterial infection and inflammation.

3,4-Dichloroisocoumarin is a potent serine-protease and SrLip inhibitor (K_i for SrLip: 26.6 μM). 3,4-Dichloroisocoumarin is opened by serine proteases and then undergoes acylation with the enzyme, thereby inhibiting protease activity. 3,4-Dichloroisocoumarin can induce DNA fragmentation and Apoptosis. 3,4-Dichloroisocoumarin can be used in the research of multiple fields such as tumors, cardiovascular disease and enzyme catalytic mechanisms.

Calceolarioside B is a phenylethanoid glycoside. Calceolarioside B can be isolated from the leaves of Akebia quinata. Calceolarioside B inhibits RLAR activity with an IC₅₀ value of 23.99 μM. Calceolarioside B inhibits the entry of Omicron BA.2 into host cells. Calceolarioside B reduces IL-6 levels. Calceolarioside B has immunomodulatory activity. Calceolarioside B has anticancer activity against human hormone-independent prostate cancer.

2-hydroxy-4-methoxybenzaldehyde is a potent tyrosinase inhibitor. 2-Hydroxy-4-methoxybenzaldehyde, an isomer of Vanillin, could be used to synthesis Urolithin M7

Anethole is a type of orally active aromatic compound that is widely found in nature and used as a flavoring agent. Anethole possesses anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, anesthetic, estrogenic, central nervous system depressant, hypnotic, insecticidal, and gastroprotective effects. Anethole can be used in the study of oxidative stress-related skin diseases and prostate cancer.

Schisandrin C (Schizandrin-C) is a phytochemical lignan isolated from Schizandra chinensis. Schisandrin C has diverse biological activities, including anticancer, anti-inflammatory and antioxidant effects. Schisandrin C can be used for cancer, alzheimer’s disease, and liver diseases research. Schisandrin C induces cell apoptosis.

Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.

Auraptene is an orally active geranyloxycoumarin that can be isolated from plants in the Brassicaceae family, antibacterial, anti-pathogen, antioxidant, anti-tumor, and neuroprotective effects. Auraptene plays an important role in the treatment of various chronic diseases such as hypertension and cystic fibrosis.

1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative that exhibits antioxidant activity and radical scavenging activity.

2-Hydroxycinnamic acid is a phenolic acid with antimicrobial and antioxidant properties. 2-Hydroxycinnamic acid has antimicrobial activity against Staphylococcus aureus and is not susceptible to drug resistance. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC₅₀ of 0.3 mM. In addition, 2-Hydroxycinnamic acid has neuroprotective and antitumor activity.

5-O-Methylembelin is a natural isocoumarin that inhibits PCSK9, inducible degrader of the low-density lipoprotein receptor (IDLR), and sterol regulatory element binding protein 2 (SREBP2) mRNA expression.

Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC₅₀ values of 0.30 mM and 0.38 mM in rat aorta.

Isoeugenol is an essential oil constituent of nutmeg, clove, and cinnamon. Isoeugenol inhibits growth of Escherichia coli and Listeria innocua with MICs of 0.6 mg/mL and 1 mg/mL, respectively.

Coniferyl alcohol is an orally active lignin biosynthesis intermediate and antifungal agent. Coniferyl alcohol specifically inhibits the growth of fungi (Verticillium longisporum). Coniferyl alcohol inhibits the growth of Nicotiana benthamiana seedlings. Coniferyl alcohol improves cardiac dysfunction in renovascular hypertension and cardiac inflammation.

Macelignan ((+)-Anwulignan; Anwuligan)?is an orally active lignan isolated from Myristica fragrans. Macelignan possesses many pharmacological activities, including anti-inflammatory, anti-cancer, anti-diabetes, and neuroprotective activities.

Diphyllin is an orally active V-ATPase inhibitor (IC₅₀=17 nM) and HIV-1 inhibitor (IC₅₀=0.38 μM). Diphyllin blocks the acidification of osteoclast lysosomes and bone resorption lacunas (IC₅₀=0.6 nM for acid influx inhibition)， thereby inhibiting bone resorption. Diphyllin can effectively inhibit osteoclast-mediated bone resorption and has no effect on osteoblastic bone formation. Diphyllin can be used in the research of bone metabolism-related diseases and has the potential to inhibit diseases related to excessive bone resorption.