Piperales

Aristolochic acid A is the main component of the plant extract aristolochic acids, primarily found in the herbaceous plants Aristolochia and Asarum. It significantly inhibits the activity of activator protein 1 (AP-1) and NF-κB, and downregulates the expression of the bladder cancer-associated BLCAP gene in human cells. It is commonly used to induce nephrotoxicity models.

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

Flavokawain C (FKC), a naturally occurring chalcone, which can be isolated from Kava.FKC has the potential to be developed into chemotherapeutic drug for the treatment of colon adenocarcinoma.

Piperlongumine (Piplartine) is a natural alkaloid from Piper longum L. It selectively kills cancer cells and strengthens the level of reactive oxygen species (ROS).

Methysticin is a kavalactone isolated from the kava roots. Methylsticin (Methysticin) exhibit osteoclast formation inhibitory activity. It inhibits activation of NF-χB in lung adenocarcinoma tissue, activates Nrf2 in neurons and astroglia, decreases peak amplitude of voltage-gated Na+ channels in hippocampal neurons, and suppresses growth of Fusarium, Trichoderma, and Colletotrichum.

1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS/D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK/NFκB and Jak2/STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.

Isostearic acid (Isooctadecanoic acid) is an active ingredient in imiquimod formulations that promotes the entry of imiquimod or peripherally secreted cytokines into the brain, and can be used to induce psoriasis-like disease models.

Piperlonguminine, an alkaloid amide isolated from the Piper species, exhibits anti-inflammatory, antitumor, neuroprotective, anti-platelet, anti-melanogenic, antifungal, and antibacterial activities. It inhibits Akt/mTOR signaling, promotes autophagy, and mediates cancer cell death.

Reynoutrin (Reinutrin) with antioxidant and radical-scavenging activity.

1. Sauchinone is a useful adjunctive treatment for bacterial infection. 2. Sauchinone, an active lignan found in Saururus chinensis, to regulate the activation of HSCs, to prevent liver fibrosis, and to inhibit oxidative stress in vivo and in vitro. 3. Sa

Aristolochic acid C, a derivative of Aristolochic acid, acts as a phospholipase A2 inhibitor.

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.

1.Aristolactam I (Aristololactum) has cytotoxic potency, mediated through the induction of apoptosis in a caspase 3-dependent pathway. 2. The effects of Aristololactam I may be mediated by different mechanisms except TGF-beta1 pathway. 3. Aristololactam I may be one of toxic metabolites in Chinese herbs containing AA which participate in renal damage and fibrosis.

N-Nornuciferine hydrochloride(4846-19-9 free base) (N-Nornuciferine hydrochloride) is an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).

Piperlotine A is an alkaloid that can be extracted from Piperonyssinus rolfsii and has antiplatelet aggregation activity.Piperlotine A showed inhibition of Mycobacterium tuberculosis in an in vitro assay with a MIC value of 50 ug/mL.Piperlotine A is an alkaloid that can be extracted from Piperonyssinus rolfsii and has antiplatelet aggregation activity.

Aristolone (Aristofone) has potential anti-cancer activity.

1-Linoleoyl Glycerol (Monolinolein) is fatty acid glycerol that has been isolated from Saururus Chinensis roots. The (R)-1-Linoleoyl Glycerol and (S)-1-Linoleoyl Glycerol exhibit Lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitory activities with IC50 values of 45.0 and 52.0 μM, respectively.

Yangonin (Y100550) is a novel CB receptor ligand, it exhibits affinity for the human recombinant CB receptor. Yangonin (Y100550) could be a valuable candidate for the intervention of NF-κB-dependent pathological conditions such as inflammation.

Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.

Dihydromethysticin ((+)-Dihydromethysticin) is a kavalactone found in Piper methysticum. It has marked activity on the induction of CYP3A23.

(E)-Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.

Aristolochic Acid D, a derivative of aristolochic acid isolated from the stems of Aristolochia indica, is identified as both a carcinogen and nephrotoxin.

Decanedioic acid (Sebacinsaure) is a saturated, straight-chain naturally occurring dicarboxylic acid.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.