Mocimycin (also known as kyrromycin) was isolated from Streptomyces ramocissimus and tested in vitro against wide range of bacterias. Although having showed good results, drug did not enter clinical trials. Mocimycin acts by binding tightly and specifically to bacterial EF-Tu. Upon administration the antibiotic prevents EF-Tu-GDP from leaving the ribosome and thus inhibits bacterial protein synthesis. Nowadays, the antibiotic is mainly used to study bacterial protein synthesis at the level of elongation factor EF-Tu-GDP release.

Clinafloxacin is a broad-spectrum fluoroquinolone antibiotic that was originally developed and subsequently abandoned in the late 1990s as a human health antibiotic for respiratory diseases. Clinafloxacin displays broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic pathogens by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 ug/ml) as well as topoisomerase IV (IC50 = 1.62 ug/ml).

Broquinaldol is a halogenated derivative of quinoline and a member of the class of compounds known as halogenated phenazines. Broquinaldol and related compounds have demonstrated efficacy against antibiotic-tolerant bacterial biofilms and Mycobacterium tuberculosis. Against several bacterial strains, broquinaldol had a minimum inhibitory concentration of 0.78 microM. Broquinaldol was also identified as having antiproliferative activity against thyroid cancer cells in vitro.

Eperezolid is an antibiotic agent developed for the treatment of a wide range of bacterial infections. The drug exerts its action by binding to 50 S ribosome subunit causing the inhibition of protein synthesis in bacterias. Eperezolid was tested in preclinical in vivo models of different becterial diseases in which it was shown to be active.

Streptonigrin is an antibiotic produced by Streptomyces flocculus. Streptonigrin exhibits activity as a broad spectrum antibiotic against both Gram-positive and Gram-negative bacteria. Streptonigrin shows antitumor activity against sarcomas, carcinomas, leukemias and lymphomas in vivo and in vitro. Due to its high toxicity, streptonigrin has not recieved widespread clinical use.

Barbinervic acid is a triterpene of the plant origin. Barbinervic acid inhibits Staphylococcus aureus growth with IC50 = 0.098 g/l.

3,6-DIMETHYLMANGOSTIN (Fuscaxanthone C) is a constituent of Garcinia mangostana (mangosteen). Fuscaxanthone C has shown α-glucosidase inhibitory activity.

The mixture of artemotil and alpha-arteether is used in patients with cerebral malaria. Both beta and alpha/beta arteether have comparable activity and are curative at a dose of 5 mg/kg for 3 days against blood-induced Plasmodium cynomolgi B infection in the rhesus monkey; alpha arteether alone is slightly less active, with a 50% cure rate at the above dose. Alpha-arteether is a fourth generation anti-bacterial and anti-fungal drug. Alpha-arteether was found to inhibit the growth of E-coli strains defective in DNA-gyrase enzyme. DNA gyrase mutants were sensitive to α-arteether whereas the wild type of E-coli having intact DNA gyrase genes were not sensitive to α-arteethers. In fact, the isomer of this compound, β-arteether, does not exhibit this activity. The beta-isomer of arteether was characterized by a longer elimination half-life and a relatively larger volume of distribution than the alpha-isomer, suggesting that beta-arteether may be responsible for the prolonged in vivo schizontocidal activity.

Beauvericin is a famous mycotoxin produced by many fungi, such as Beaveria bassiana and Fusarium spp. Beauvericin is a cyclic hexadepsipeptide (Figure 1) that belongs to the enniatin antibiotic family. It contains three D-hydroxyisovaleryl and three N-methylphenylalanyl residues in an alternating sequence. Beauvericin was first isolated from Beaveria bassiana, which is a common and commercial entomopathogenic mycoinsecticide. Beauvericin was one of the active constituents of B. bassiana and was confirmed to have antimicrobial and anti-tumor activities. Beauvericin has a strong antibacterial activity against human, animal and plant pathogenic bacteria with no selectively between Gram-positive and Gram-negative bacteria. The cytotoxicity of beauvericin to human tumor cells has been frequently reported.

Jatrorrhizine is an active component of the traditional Chinese herb Coptis chinensis, which has been used to prevent and treat metabolic disorders. It is also found plants such as Enantia chlorantha, Thalictrum lucidumm, Thalictrum revolutum. Jatrorrhizine possesses antifungal, antibacterial activity. It has low toxicity and was studied in mouse models of obesity and hypercholesterolemia. The mechanism of action of Jatrorrhizine is not fully elucidated. The compound blocks alpha-1 and alpha-2 adrenoreceptors, monoamine oxidase A and B.