Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.

Deltamethrin (DLM) is a pyrethroid insecticide and veterinary treatment that is approved for use in the EU, Australia and the USA. It has a low aqueous solubility, is semi-volatile and has a low potential to leach to groundwater. It is not persistent in soil and is non-mobile. Deltamethrin is highly toxic to humans and other mammals and is a neurotoxin. It is relatively non-toxic to birds and earthworms although it presents a high risk to most aquatic organisms and honeybees. Recent in vitro and in vivo studies have shown that the deltamethrin have the potential to induce apoptogenic signaling pathways which plays an important role in the mechanism of anticancer action. Thus, deltamethrin thereof could have the potential to develop as an anticancer agent.

Bergenin, isolated from Bergenia ligulata is a potent antioxidant and antilithiatic agent. Bergenin is an effective and broad-spectrum antifungal and antiviral Chinese medicine. Bergenin was reported to possess anti-microbial properties against filamentous fungi, yeast and HIV, but not against bacteria. Bergenin also exhibits anti-inflammatory activity through the inhibition of cyclo-oxygenase-2 or by means of affecting the Th1- or Th2-skewed cytokine production. Bergenin also exerts an anti-oxidant effect by scavenging free radicals, such as H, OH and CH3. In addition, bergenin was reported to possess hepatoprotective, neuroprotective and gastroprotective properties. R. aesculifolia Batal containing bergenin was used to treat protozoal infection and fever in rural China. Also was evaluated the antimalarial activity of bergenin in vitro and in vivo trials. Bergenin effectively inhibited Plasmodium falciparum growth in vitro (IC50, 14.1 µg̸ml, with ~100% inhibition at 50 µg/ml), without apparent cytotoxicity to erythrocytes or to mammalian HeLa and HepG2 cells. Bergenin exhibited less cytotoxic activity and the selectivity index (SI) was 887 and 1,355 for HeLa and HepG2 cells, respectively. The administration of bergenin to Plasmodium berghei infected mice for 6 days significantly inhibited the growth of the parasites. These findings provide evidence that bergenin may be a promising novel drug for antimalarial treatment. Antioxidant potential of bergenin was shown based on decreasing in lipid peroxides and increasing in superoxide dismutase (SOD) and catalase (CAT). Histopathological studies demonstrated the regenerative effect of bergenin on pancreatic β cells. Was shown, that bergenin isolated from C. digyna possesses significant antidiabetic, hypolipidemic and antioxidant activity in Type 2 diabetic rats.

Cinchonidine is an alkaloid found in Cinchona officinalis and Gongronema latifolium. Cinchonidine is an antimalarial drug which has been used clinically in malaria caused by Plasmodium falciparum. Cinchonidine is reported as an ingredient of Quinimax in a number of countries. Quinimax is a combination of four alkaloids (quinine, quinidine, cinchoine and cinchonidine).

Cepharanthine (CEP) is a naturally occurring alkaloid extracted from the plant Stephania cepharantha Hayata. It has been widely used in Japan for more than 40 years to treat a wide variety of acute and chronic diseases. CEP inhibits tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppresses cytokine production. It has also been shown to scavenge free radicals and to have a protective effect against some of the responses mediated by pro-inflammatory cytokines such as TNF-α, interleukin (IL)-1β and IL6. CEP has successfully been used to treat a diverse range of medical conditions, including radiation-induced leukopenia, idiopathic thrombocytopenic purpura, alopecia areata, alopecia pityrodes, venomous snakebites, xerostomia, sarcoidosis, refractory anemia and various cancer-related conditions. No safety issues have been observed with CEP, and side effects are very rarely reported. Recently was described a transcriptomic approach confirmed that cepharanthine might have a potential innovative antiplasmodial mechanism of action. Cepharanthine could interfere with several important functions for Plasmodium survival and virulence as the mitochondrion, apicoplast, cytoadherence antigenic variation and Maurer’s clefts. Thus, cepharanthine might play an ongoing role in the progress on anti-malarial drug discovery efforts. Also using intravenous and oral administration of CEP was shown its protective effect for acute or late toxicity to the bladder/urethra and rectum. It was discovered, that acute urinary toxicity was significantly milder for the intravenous group than for the oral and non-administration groups. The protective efficacy of CEP was not approved for acute rectal toxicity, but late rectal toxicity was significantly milder for the intravenous group than for the oral group. Intravenous Cepharanthin administration may prevent acute or late toxicity by radiotherapy for prostate cancer.

Piromidic acid, a quinolone antibiotic has an inhibitory effect against hepatic stages of P. falciparum and P. yoelii yoelii, and has a potential for treatment or prevention of malaria through their unique antiparasitic effect against erythrocytic and hepatic stages of Plasmodium.

Piperaquine is a bisquinoline antimalarial drug that was first synthesized in the 1960s and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. Piperaquine is characterized by slow absorption and a long biological half-life, making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.

Sulfalene (INN, USAN) or Sulfametopyrazine (BAN) is a long-acting sulfonamide antibiotic used for the treatment of chronic bronchitis, urinary tract infections, and malaria. Sulfametopyrazine, by virtue of a long half-life, achieves peak blood levels of 120 mkg/ml or more which fall to around 30-50 mkg/ml one week after a single oral dose of 2 g. Long-term administration of this drug in the treatment of leprosy for up to 3 years has been accomplished without serious unwanted effects

Tyrothricin is a mixture of non-ribosomal peptides produced by Brevibacillus brevis, now known as Aneurinibacillus migulanus, a gram positive aerobic bacteria. The compound mixture shows activity against bacteria, fungi and some viruses. A very interesting feature of AMPs is the fact, that even in vitro it is almost impossible to induce resistances. It is a locally effective antibiotic effective against gram-positive bacteria. It is sometimes combined with benzocaine 5 mg (Tyrozets) to provide relief from sore throats. Recommended for short-term relief of symptoms of oral and throat inflammation. Prevention of infections before/during mouth and throat operations (tooth extractions, gum surgical treatment). Tyrothricin inhibits protein biosynthesis of gram-positive organisms, but is completely ineffective against gram-negative.

Acriflavine (ACF) is a topical antiseptic. The hydrochloride form is more irritating than the neutral form. It is derived from acridine. Commercial preparations are often mixtures with proflavine. Acriflavine was developed in 1912 by Paul Ehrlich, a German medical researcher, and was used during the First World War against sleeping sickness. ACF has known trypanocidal, antibacterial, and antiviral activities. Effects of ACF on cancer cells were first reported 50 years ago. By present time was demonstrated that ACF a drug, that binds directly to HIF-1 alpha and HIF-2 alpha and inhibits HIF-1 dimerization and transcriptional activity and thus has potent inhibitory effects on tumor growth and vascularization. Also Acriflavine in combination with 3,6-diaminoacridine (proflavine) could prove to be a potential antimalarial drug and its pharmacological action can be due to inhibition of gyrase activity. This is achieved through interaction of the ACF with the DNA substrate. This interaction may lead to conformation change in DNA unsuitable for binding of gyrase with DNA.