rapamycin

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Demethoxyrapamycin is a new antifungal antibiotic agent which is co-produced with rapamycin by Streptomyces hygroscopicus.

Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1 Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

L-Leucine ((S)-Leucine) is one of nine essential amino acids in humans (provided by food), L-Leucine is important for protein synthesis and many metabolic functions. L-Leucine contributes to regulation of blood-sugar levels; growth and repair of muscle and bone tissue; growth hormone production; and wound healing. L-Leucine also prevents breakdown of muscle proteins after trauma or severe stress and may be beneficial for individuals with phenylketonuria. L-Leucine is available in many foods and deficiency is rare.

(+)-Usnic acid (D-Usnic Acid) is a naturally occurring dibenzofuran derivative found in several lichen species.

Cyclovirobuxine D (Bebuxine) is extracted from Buxus microphylla.

Dihydromyricetin (Ampelopsin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyricetin can activate autophagy by inhibiting mTOR signaling.

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.

Hederacolchiside A1 (Raddeanoside R13) shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential. Hederacolchiside A1 shows antiproliferation activities in three cancer cell lines with the IC50 value of 2.4 uM, it exhibits a preferential cytotoxicity on a pigmented melanoma cell line. It suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K Akt mTOR signaling pathway.

Trehalose 6-phosphate potassium salt hydrate (α,α-Trehalose 6-phosphate potassium salt hydrate) is a Trehalose derivative, an intermediate in trehalose biosynthesis, and an important signaling metabolite in plants. It can regulate root branching through the master kinase SNF1-related kinase-1 (SnRK1) and rapamycin target (TOR).

25(R,S)-Ruscogenin is a natual product.

Glucosylsphingosine (Lyso-Gb1) is a naturally occurring glycosyl ceramide, a metabolite of GBA (acid β-glucosidase), involved in cellular recognition, signaling, and intercellular interactions.Glucopsychosine accumulates in certain neurodegenerative diseases (e.g., Gaucher disease), disrupts lysosomal function through activation of mammalian target of rapamycin complex 1 (mTORC1), and is a noncompetitive inhibitor of glucocerebrosidase.

WDB002, a natural product belonging to the FK506 rapamycin family, targets CEP250 and may be employed in COVID-19 research [1].

Arnicolide D is a sesquiterpene lactone. Arnicolide D isolates from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K AKT mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner. Arnicolide D exerts strong cytotoxic activity on the human colon carcinoma HT-29 cell line.