reversal

1. Pristimerin (Celastrol methyl ester) has anticancer activity , treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. 2. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS IKK NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.

Compound 13, also known as Anti-inflammatory agent 57 and classified as a pyranocoumarin, is a natural product extracted from the roots of Peucedanum praeruptorum. This compound possesses both multidrug-resistance (MDR) reversal properties and anti-inflammatory effects [1].

Astragaloside II (Astrasieversianin VIII) is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteogenic activities, differentiation, proliferation, and mineralization, through the bone morphogenetic protein-2/MAPK and Smad1/5/8 pathways.

Protosappanin A (PTA) has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Acerinol is an active ingredient from traditional Chinese medicinal herbs. It could be used as a cancer multidrug resistance reversal agent. Acerinol can significantly stimulate the activity of ABCB1 ATPase without affecting the expression of ABCB1 on nei

1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.

1. Coptisine (Coptisin) treatment increases cell viability based on its reversal effect on the enhanced activity of Indoleamine 2, 3-dioxygenase . 2. Coptisine treats myocardial I/R likely through suppressing myocardial apoptosis and inflammation by inhibiting the Rho/ROCK pathway. 3. Coptisine is a potential anti-osteosarcoma drug candidate, via exerting a strong anti-osteosarcoma effect with very low toxicity . 4. Coptisine with a high dosage could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. 5. Coptisine suppresses adhesion, migration and invasion of MDA-MB-231 breast cancer cells in vitro, the down-regulation of MMP-9 in combination with the increase of TIMP-1 possibly contributing to the anti-metastatic function for breast cancer.

Due to the multi-drug resistance reversal activity of the less polar ecdysteroids, several new products( including 20-hydroxyecdysone,20-hydroxyecdysone 2,3;20,22-diacetonide) are promising for being tested against various cancer cell lines.

Wallichinine shows inhibitory activity on platelet aggregation caused by platelet activating factor (PAF). Wallichinine with ABCB1 presents valuable clues for the development of novel MDR reversal reagents from natural products, wallichinine can significa

1. Tectochrysin (Techtochrysine) has antioxidant effect. 2. Tectochrysin is promising inhibitors for the reversal of ABCG2-mediated drug transport. 3. Tectochrysin leads to apoptotic cell death in NSC-LC cells through activation of DR3 and Fas expression via inhibition of STAT3 phosphorylation.

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tu

trans-Trimethoxyresveratrol (MR-3), a natural methoxylated analog of resveratrol, inhibits breast Y cell invasiveness by downregulation of PI3K/Akt and Wnt/β-catenin signaling cascades and reversal of epithelial-mesenchymal transition.