antitumor activity

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

1. Hypericin (Cyclosan) has antineoplastic activity. 2. Hypericin has antibiotic and antiviral activities. 3. Hypericin has antidepressive activity through inhibiting monoamine oxidase enzyme. 4. Hypericin inhibits RANKL-mediated osteoclastogenesis via affecting ERK signalling in vitro and suppresses wear particle-induced osteolysis in vivo.

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

Digitonin is a natural product of the glycoside family and is a detergent. Digitonin has antitumor activity, binds to cholesterol molecules to increase the permeability of cell membranes, and is active in the cleavage of cell membranes in a wide range of cells.

Tunicamycin is a mixture of antibiotics that inhibit N-linked glycosylation by blocking GlcNAc phosphotransferase (GPT). Tunicamycin has antitumor activity, as well as anti-bacterial, anti-fungal, and anti-viral activity.

Doxycycline (Doxiciclina) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity. Doxycycline has antibacterial activity and antitumor activity.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Lactic acid (2-hydroxypropanoic acid) is a product of glycolysis and is widely found in nature.Lactic acid is produced in the body during hypoxia in contracted skeletal muscle and can be removed under fully aerobic conditions.Lactic acid can be used as a hemodynamic indicator in critically ill patients.Lactic acid has antitumor activity.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

2-Amino-2-dichlorobenzophenone is an aromatic natural compound that has been used to study the effects of various compounds on cell metabolism, protein synthesis and enzyme activity. It has also been used in the synthesis of drugs, such as antitumor drugs and anti-inflammatory agents.

Testosterone acetate (NSC-523836) is a hormone with in vitro antitumor activity.

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

Cephalomannine (Baccatin III) is a taxol derivative obtained from Taxus yunnanensis with antitumor activity.

2-methoxycinnamaldehyde is a natural compound of Cinnamomum cassia,has been widely studied with regard to its antitumor activity.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Annatto is a natural food coloring derived primarily from Bixa orellana L. Annatto has antitumor activity and at high doses increases the likelihood of cellular mutations.Annatto can be used in beverages, baking, and other foods.

Holomycin (N-Demethylthiolutin) is a secondary metabolite of dithiopyrrolidone. HolomycinHolomycin, an antibiotic secondary metabolite, is required for the biofilm formation of natural photogenic Bacillus galatheae S2753 and is also a broad-spectrum antibiotic. holomycin promotes biofilm formation of S2753 through its alene-disthionyl group. Holomycin has antitumor activity and is involved in RNA synthesis.

1-beta-D-Arabinofuranosylthymine (Thymine 1-β-D-arabinofuranoside) is a purine nucleoside analog. Purine nucleoside analogs have a broad spectrum of antitumor activity, targeting inert lymphoid malignancies and inducing apoptosis.1-beta-D-Arabinofuranosylthymine's anticancer mechanism is dependent on the inhibition of DNA synthesis.1-beta-D-Arabinofuranosylthymine is a purine nucleoside analog.

Torachrysone Triglucoside is a glucoside isolated from cassia seeds with potential antitumor activity.

Usenamine A is a small molecule compound derived from lichen Usnea longissima that has antitumor activity and can be used in the study of tumors.

(Z)-Butylidenephthalide ((Z)-3-Butylidenephthalide) has antitumor and hypoglycemic effects, and can effectively inhibit the tumor growth of glioma and inhibit R-glucosidase activity.

7,3′,4′-Tri-O-methyleriodictyol (7,3',4'-Tri-O-methyleriodictyol) is an isolate from the methanolic extract of Pogostemon cablin and possesses antimicrobial, antioxidant, antitumor, and antiprotozoal activities, inhibits Mycobacterium tuberculosis infections , . Inhibits SOS inducing activity.

Cedrelone is a citrulline analog and a phenazine biosynthesis-like domain protein (PBLD) activator.Cedrelone induces apoptosis in cancer cells.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone has insecticidal activity, inhibiting the growth of arrowhead venom of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus). Cedrelone has insecticidal activity, inhibiting the growth of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus).Cedrelone has antitumor effects and exhibits significant cytotoxicity against cancer cell lines such as -60, SMMC-7721, A-549, MCF-7, and SW480.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone is a very potent inducer of apoptosis, leading to cell cycle arrest.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

1. Gelsemine (Gelsemin) has antitumor activity. 2. Gelsemine has anti-oxidative activity. 3. Gelsemine has anti-hyperlipidemic activity. 4. Gelsemine has marked antinociception in inflammatory, neuropathic and bone cancer pains without inducing antinociceptive tolerance.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

Cryptotanshinone (Cryptotanshinon), a STAT3 inhibitor (IC50: 4.6 μM) in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a little effect on STAT3 Ser727, but no inhibition for STAT1 nor STAT5.

β-Elemene (Levo-β-elemene) is a natural product isolated from Curcuma wenyujin, with an antitumor activity and induce cell apoptosis.

1. Berberrubine chloride (9-Berberoline Chloride) has antitumor activity. 2. Berberrubine has antidiabetic activity. 3. Berberrubine dose-dependently inhibits IL-8 and MCP-1 protein levels in the media and mRNA expression of the cells stimulated with IL-1beta or TNF-alpha.

5-Azacytidine (Ladakamycin) is a cytidine nucleoside analog, a DNA methylation inhibitor with specificity. 5-Azacytidine regulates gene expression by decreasing the level of DNA methylation. 5-Azacytidine induces autophagy and has antitumor activity.

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg/kg, i.v., 50-200 J/cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg/m2, IV, 100 J/cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

Psoralenoside is a natural product isolated from the fruits of Psoralea corylifolia, shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

Formosanin C (Polyphyllin B) is a compound isolated from Rhizoma Paridis, showed pro-apoptosis and immunoregulation with antitumor activity in cultured cells and animal systems.

Jasplakinolide(Jaspamide), a naturally occurring cyclic peptide from marine sponges, is a potent inducer of actin polymerization.Jasplakinolide exhibits antifungal and antitumor activity and stabilizes pre-existing actin filaments. Jasplakinolide competitively binds to F-actin with the ghost pen cyclic peptide and has a Kd value of 15 nM for F-actin.

SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.

Homoharringtonine (HHT) is a natural alkaloid that inhibits the translation of proteins and is cytotoxic. Homoharringtonine acts on the ribosomes of tumor cells to inhibit the elongation step of protein translation, thereby inhibiting protein synthesis, and has antitumor activity.

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

Palmitic acid (Cetylic acid) is a natural product, a common saturated fatty acid found in animals, plants and microorganisms. Palmitic acid has antitumor activity.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

Sodium Demethylcantharidate (Sodium norcantharidin) is extracted from Mylabris phqlarata pallas and has potent antitumor activity.

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

Berbamine dihydrochloride (Berbamine), a natural compound derived from the Berberis amurensis plant, has been shown to exhibit antitumor activity in several Ys.

4,6-Benzilidine-D-Glucose is a clinical antitumor compound showing antitumor activity in rats with chemically induced hepatocellular carcinoma.

Shishijimicin A, a novel antitumor agent isolated from the ascidian Didemnum proliferum, exhibits highly potent cytotoxicities and demonstrates considerable anti-tumor activity [1] [2]. This compound also serves as a click chemistry reagent due to its alkyne group, enabling it to partake in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

Marsdenoside B (compound 8), an isolate from the Alocasia genus, exhibits antitumor activity by inhibiting the proliferation of MGC-803 and HT-29 tumor cell lines with IC50 values of 25.6 μg/mL and 32.4 μg/mL, respectively.

Danshenol A has strong aldose reductase (AR) inhibitory activity, has IC50 of 0.10 microM which is comparable to that of epalrestat in clinical use. Danshenol A also has antitumor activity in T-24, QGY, K562, Me180 and BIU87 cell lines, shows inhibited growth of K562 (IC50 = 0.53 μg/mL), T-24 (IC50 = 7.94 μg/mL), QGY (IC50 = 4.65 μg/mL) and Me180 (IC50 = 6.89 μg/mL) cell lines.

Psammaplin A, a marine metabolite, functions as a robust inhibitor of HDAC and DNA methyltransferases, displaying notable potency and selectivity as a DAC1 inhibitor, with an IC50 value of 0.9 nM. It exhibits antimicrobial effects against Gram-positive bacteria and inhibits both DNA synthesis and DNA gyrase activity, also demonstrating antitumor activity[1][2].

12-Oleanene-3,6-diol has antitumor activity, it can induce apoptosis and has inhibition effect on the proliferation in RKO cell line.