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.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Sennoside A (NSC-112929), a kind of irritant laxative isolated from rhei rhizome, causes purgative actions in the intestine.

Oleanolic Acid (Caryophyllin) is a natural compound with anti-tumor activities, which are widely distributed in plants.

Aloperine exhibits anti-inflammatory, antibacterial, antiviral, and anti-tumor properties.

Cholic acid sodium (SodiumCholate) exhibits a strong spermicidal and antiviral [anti-human immunodeficiency virus (HIV)-1] activity.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Doxorubicin (Adriamycin) is a Topoisomerase II (Top2) inhibitor with antineoplastic activity.

Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.

Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.

Psoralen (Ficusin) is a furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division.

Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3/Girdin/Akt signaling in HCC cells.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

Ganolucidic acid A exhibits cytotoxicity, has inhibitory activities against human HeLa cervical cancer cell lines. It shows significant anti-human immunodeficiency virus (anti-HIV)-1 protease activity with IC50 values of 20-90 microM.

Oxindole (Indolin-2-one) is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.Oxindole structure has been used in receptor tyrosine kinases (RTKs) inhibitors such as SU4984 and intedanib, the RTK family represents an important therapeutic target for anti-cancer drug development.

Bellidifolin (Bellidifoline) has anti-oxidation, hepatoprotective, anti-inflammatory and antitumor actions, it may contribute to the protective effects associated with nerve injury initiated by hypoxia by mechanisms related to inhibition of cell apoptosis independent of the ERK pathway. Bellidifolin shows interesting inhibitory activity of monoamine oxidases (MAO) A, it could be useful for treating type-2 diabetes, likely via the improvement of insulin resistance (IR). Bellidifolin also shows an antifungal effect (MIC values of 50 microg/mL).

Fumagillin (Amebacilin) is a selective and potent irreversible inhibitor of Methionine aminopeptidase 2 (MetAP2), used as an antibiotic to treat microsporidiosis.

Ivermectin (MK-933) is a glutamate-gated chloride channel (GluCls) activator, with antiparasitic activity.

Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.

Limonin (Citrolimonin) is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability.

Trilobatin (P-Phlorizin) has anti-oxidant effect, can increase superoxide dismutase (SOD) activity.Trilobatin has anti-inflammatory effect, it potentially inhibits the lipopolysaccharide (LPS)-induced inflammatory response by suppressing the NF-κB signaling pathway.Trilobatin shows a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase for management of postprandial hyperglycemia with less side effect.

Tripterifordin shows anti-HIV replication activity in H9 lymphocyte cells with an EC50 of 1 microgram/ml.

Zingibroside R1 (Ginsenoside Z-R1) has anti-HIV-1 activity.

Oleanonic acid (3-Ketooleanolic Acid) is relatively non-toxic, hepatoprotective, and exhibits antitumor and andantiviral properties.

2-Hydroxycinnamic acid is a natural product isolated from Angraecum fragrans, has photooxidant activity.

Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt/β-catenin signaling.

α-mannosidase I inhibitor

Methyl gallate (Gallincin) is a reverse transcriptase inhibitor with antioxidant, anti-HIV-1 and HIV-1 enzyme inhibition activities.

Erythromycin ethylsuccinate (EES) is a macrolide antibiotic, produced by Streptomyces erythreus.

Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

Maslinic acid (Crategolic acid) is a DNA polymerase B inhibitor.

Azulene (Bicyclo[5.3.0]Decapentaene) is a natural product.

L-Chicoric Acid (trans-Caffeoyltartaric acid) has been shown to inhibit hyaluronidase and HIV-1 integrase, and to possess phagoeytosis stimulatory activity in vitro and in vivo and antiviral acitivy. L-Chicoric acid may reduce acute alcohol-induced steatosis in mice through interfering with the induction of iNOS and iNOS-dependent signaling cascades in the liver. 3. L-Chicoric acid inhibited cell viability and induced apoptosis in 3T3-L1 preadipocytes which was characterized by chromatin condensation and poly ADP-ribose-polymerase (PARP) cleavage.

Soyasaponin II has antiviral effects, it can inhibit the replication of human cytomegalovirus, influenza virus, and human immunodeficiency virus type 1.

Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.

Theaflavin 3,3'-digallate (8-Gingerol) , a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.

Bevirimat (PA-457) is a first-in-class inhibitor of HIV-1 maturation, blocking the cleavage of the Gag capsid (CA) precursor, CA-SPI, to mature CA protein during virion maturation.

Pentoxifylline (PTX) modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It also inhibits platelet aggregation and improves blood flow by increasing erythrocyte and leukocyte flexibility.

α-Lipoic Acid (DL-α-Lipoic acid) an octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.

Ganoderic acid GS-2 inhibits the activity of the human immunodeficiency virus-1 (HIV-1) protease.

Gomisin G is a natural compound and exhibits potent anti-HIV activity (EC50: 0.006 μg/mL; therapeutic index: 300). It is a good substrate of CYP2C9.

Rosamultin has antioxidant, antiinflammatory/antinociceptive properties,and has anti-human immunodeficiency virus (HIV) activity.

Cichoric Acid (Dicaffeoyltartaric acid) is a potent inhibitor of human immunodeficiency virus type-1 (HIV-1) integrase and the replication in tissues. It also a class of cannabinomimetics with CB2 receptor-dependent and independent.

Ganoderiol F has anti-inflammatory, cytotoxic and anti-HIV activity, it inhibits activity of topoisomerases in vitro, and it inhibits human immunodeficiency virus-1 protease with IC(50) values of 20-40 microM. It induced HO-1 expression, activation of the mitogen-activated protein kinase EKR and up-regulation of cyclin-dependent kinase inhibitor p16 and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production.

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

Fangchinoline (Tetrandrine B) is extracted from Stephania tetrandra S. Moore.