Biological activities of bombolitins from Bombus ardens, B. consobrinus, B. terrestris and B. ussurensis (bombolitinsA, C, T and U, respectively) were examined using hemolytic, anti-microbial, anti-fungal and anti-tumor activity assays.Among the four bombolitins tested, bombolitin T showed the highest hemolytic and anti-tumor activities. All bombolitinsexhibited strong anti-microbial and anti-fungal activities, and bombolitin A specifically possessed the highest anti-microbialactivity against the Gram-negative bacteria Escherichia coli. Circular dichroism spectrometry analysis revealed that allfour bombolitins had over 61.7% and 45.5% of α-helicity in 30 mM sodium dodecyl sulfate and 50% trifluoroethanolbuffers, respectively, which form lipid-membrane-mimicking environments. Bombolitin T showed the lowest IC50 valuesof 8.5 μM and 8.8 μM against SK-OV-3 and NIH-OVCAR-3 cell lines, respectively, after 72 h of treatment, but itsrelative hemolytic activity at a concentration of 200 μM was 2.3-fold higher than that of 0.1% Triton X-100. Thisstudy provides new information on the biological and molecular properties of venom peptides of bumblebees. However,further studies on reducing cytotoxicity of bombolitins are needed for designing selective anti-tumor peptides.
Bombolitin is a venom peptide originally isolated from bumblebees and possesses various biological activities, including hemolytic activity. Bombolitins exhibit amphipathic α-helical structure in lipid-membrane-mimicking environments. To investigate their pharmacological and toxicological properties, anti-tumor, anti-microbial and cytotoxic activities of bombolitins from Bombus ardens and Bombus ussurensis were evaluated. Bombolitins of the two species exhibited extremely high anti-tumor activity against ovarian tumor cells SK-OV-3 and NIH; OVCAR-3 at 25-50 μM, which is 2-fold more potent than other wasp venom peptides studied to date (Yoon et al., 2015; Yoon et al., 2016). The two bombolitins showed significantly high antimicrobial activity. However, bombolotin of B. ussurensis showed no antimicrobial activity against Escherichia coli. In addition to their high levels of anti-tumor activity, bombolitins showed considerable levels of hemolytic activity. Thus, to utilize bombolitins as a potential candidate for anti-tumor peptide drugs, further studies for reducing cytotoxic properties of bombolitns is essential.
The lesser paper wasp, Parapolybia varia, belongs to large subfamily Polistinae and is distributed in Middle East, the Indo-Papuan region and East Asia. P. varia is known to become aggressive when disturbed for defending their colonies, resulting in fatal envenomation. Vespid chemotactic peptide (VCP) and vespakinin have recently been determined to be the top two genes most abundantly transcribed in venom glands of P. varia. To investigate the pharmacological and toxicological properties of VCP and vespakinin, their antitumor, antimicrobial, and cytotoxic activities were evaluated. VCP exhibited a significantly high antitumor activity against ovarian tumor cell SK-OV-3 at 100 M. VCP also showed higher hemolytic activity than vespakinin. Antimicrobial activity was only observed with VCP against yeast Candida albicans at 1 mM. Since VCP showed a relatively low hemolytic activity but a considerable level of antitumor activity, it has further merits to be exploited as a potential antitumor agent with reduced side effects on normal cells.
Anthocyanins are very important constituent of human diet. In recent years, they have gained much attention due to their antioxidative properties. As the radish (Raphanus sativus L) has rich content of anthocyanins, the study is aimed to develop increased functional radish from selected radish varieties. ‘Bordeux’ is a hybrid variety of breeding between one accession derived from ‘Oharu’ as a maternal variety and ‘Chungpihongsim’ as a paternal variety. In this study, we investigated the new varieties of radish commonly consumed in Republic of Korea for their total phenolic content (TPC) and antioxidant activities using three (DDPH, FRAP and CUPRAC) different assays. The selected radish varieties like ‘Bordeux’, ‘Chungbok’, ‘3209’, ‘Chungwoon’, ‘Oharu’, and ‘Chungpihongsim’ were procured from the company Syngenta Korea. Among the selected radish varieties, ‘Bordeux’ (289 μg/g FW) and ‘Chungpihongsim’ (276 μg/g FW) revealed maximum amount of phenolics; whereas ‘3209’ (103 μg/g FW) and ‘Chungwoon’ (166 μg/g FW) showed the lower amount of phenolics content, respectively. Extracts from these studied radishes showed good to moderate antioxidant activities. The varieties ‘Chungpihongsim’ and ‘Bordeux’ revealed maximum antioxidant activity for all assays as demonstrated. However, some varieties like ‘3209’ and ‘Oharu’ exhibited the lowest antioxidant activity in all the tested assays, viz; DPH, FRAP and CUPRAC in μg TE/g FW, respectively. The antioxidant activities may be attributed to the higher phenolic acid contents as a linear relation was observed between the two components and the antioxidant parameters.