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Sittiruk Roytrakul - One of the best experts on this subject based on the ideXlab platform.
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a Scorpion Venom Peptide derivative bmkn 22 with potent antibiofilm activity against pseudomonas aeruginosa
PLOS ONE, 2019Co-Authors: Kittitat Teerapo, Anchalee Sistayanarain, Sittiruk Roytrakul, Duangkamol KunthalertAbstract:Pseudomonas aeruginosa is a leading cause of nosocomial and serious life-threatening infections and infections caused by this bacterium continue to pose a major medical challenge worldwide. The ability of P. aeruginosa to produce multiple virulence factors and in particular to form biofilms makes this bacterium resistant to all known antibiotics. As a consequence, standard antibiotic therapy are increasingly become ineffective to clear such infections associated with biofilms. In search for novel effective agents to combat P. aeruginosa biofilm infections, a series of the BmKn‒2 Scorpion Venom Peptide and its truncated derivatives were synthesized and their antibiofilm activities assessed. Among the Peptides tested, BmKn‒22 Peptide, which was a modified Peptide of the parental BmKn‒2 Scorpion Venom Peptide, clearly demonstrated the most potential inhibitory activity against P. aeruginosa biofilms without affecting the bacterial growth. This Peptide was not only capable of inhibiting the formation of P. aeruginosa biofilms, but also disrupting the established biofilms of P. aeruginosa. Additionally, BmKn‒22 Peptide was able to inhibit the production of key virulence factor pyocyanin of P. aeruginosa. Our results also showed that BmKn‒22 Peptide significantly reduced lasI and rhlR expression, and suggested that BmKn‒22 Peptide-mediated inhibition of P. aeruginosa biofilms and virulence factors was achieved through the components of quorum-sensing systems. Combination of BmKn‒22 Peptide with azithromycin resulted in a remarkable reduction P. aeruginosa biofilms. Since this Peptide exhibited low toxicity to mammalian cells, all our results therefore indicate that the BmKn‒22 Peptide is a promising antibiofilm agent against P. aeruginosa and warrant further development of this Peptide as a novel therapeutic for treatment of P. aeruginosa‒associated biofilm infections.
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A Scorpion Venom Peptide derivative BmKn‒22 with potent antibiofilm activity against Pseudomonas aeruginosa.
PLOS ONE, 2019Co-Authors: Kittitat Teerapo, Anchalee Sistayanarain, Sittiruk Roytrakul, Duangkamol KunthalertAbstract:Pseudomonas aeruginosa is a leading cause of nosocomial and serious life-threatening infections and infections caused by this bacterium continue to pose a major medical challenge worldwide. The ability of P. aeruginosa to produce multiple virulence factors and in particular to form biofilms makes this bacterium resistant to all known antibiotics. As a consequence, standard antibiotic therapy are increasingly become ineffective to clear such infections associated with biofilms. In search for novel effective agents to combat P. aeruginosa biofilm infections, a series of the BmKn‒2 Scorpion Venom Peptide and its truncated derivatives were synthesized and their antibiofilm activities assessed. Among the Peptides tested, BmKn‒22 Peptide, which was a modified Peptide of the parental BmKn‒2 Scorpion Venom Peptide, clearly demonstrated the most potential inhibitory activity against P. aeruginosa biofilms without affecting the bacterial growth. This Peptide was not only capable of inhibiting the formation of P. aeruginosa biofilms, but also disrupting the established biofilms of P. aeruginosa. Additionally, BmKn‒22 Peptide was able to inhibit the production of key virulence factor pyocyanin of P. aeruginosa. Our results also showed that BmKn‒22 Peptide significantly reduced lasI and rhlR expression, and suggested that BmKn‒22 Peptide-mediated inhibition of P. aeruginosa biofilms and virulence factors was achieved through the components of quorum-sensing systems. Combination of BmKn‒22 Peptide with azithromycin resulted in a remarkable reduction P. aeruginosa biofilms. Since this Peptide exhibited low toxicity to mammalian cells, all our results therefore indicate that the BmKn‒22 Peptide is a promising antibiofilm agent against P. aeruginosa and warrant further development of this Peptide as a novel therapeutic for treatment of P. aeruginosa‒associated biofilm infections.
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Anti-Proliferative Mechanism of BmKn2 Peptide on Colon Cancer Cells
Journal of the Medical Technologist Association of Thailand, 2017Co-Authors: Pornpimol Treeyos, Teerakul Arpornsuwan, Suthathip Kittisenachai, Sittiruk RoytrakulAbstract:Colon cancer is one of the most fatal cancers in the world. A Scorpion Venom Peptide BmKn-2 showed potent cytotoxic effects towards human cancer cells with the concurrent induction of apoptosis. The aim of this study was to investigate the protein expression profiles associated with anti-proliferative effects of synthetic BmKn2 Peptide in human colon cancer SW620 cells using shotgun proteomics technique. MTT assay demonstrated cytotoxic activity of BmKn2 with IC 50 of 40 µM in SW620 cells at 24h. SDS-PAGE analysis showed at least 4 higher intensity protein bands in BmKn2-treated than in untreated cells. LC-MS analysis of these protein bands in both samples identified 31 proteins which are differentially expressed. These proteins have been implicated in various cellular processes including transcription, metabolic process, cell proliferation, transport, cytoskeleton, immune response and cell signaling. Analysis based on the STITCH 4.0 database predicted the interaction of SUPT16H (SUPT16H), HEAT repeat-containing protein 6 (HEATR6), Nucleosome assembly protein 1-like (NAP1L3), Wilms tumor 1 (WT1) and synaptophysin, isoform CRA_a (SYP) with the tumor suppressor P53 (TP53). Taken together, BmKn-2 Peptide exerts selective cytotoxic effects on human colon cancer cells by inducing P53 tumor suppressor pathway. It shows great promise as new potential therapeutic agent for colon cancer, with minimal effects on human healthy tissue and provides a framework for the development of Peptide-based anticancer technologies.
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The Scorpion Venom Peptide BmKn2 induces apoptosis in cancerous but not in normal human oral cells.
Biomedicine & Pharmacotherapy, 2016Co-Authors: Saranya Satitmanwiwat, Sittiruk Roytrakul, Chinarat Changsangfa, Anuson Khanuengthong, Kornkanok Promthep, Teerakul Arpornsuwan, Kulnasan Saikhun, Hathaitip SritanaudomchaiAbstract:Abstract Aim This study aimed to investigate the mechanism of the induction of apoptosis of human oral cancer cells by the Scorpion Venom Peptide BmKn2. Methods Human oral squamous carcinoma cells (HSC4), mouth epidermoid carcinoma cells (KB), human normal gingival cells (HGC) and dental pulp cells (DPC) were treated with BmKn-2 Peptide for 24 h. Cell viability was determined by the MTT assay. Apoptosis was assessed using phase contrast microscopy, by propidium iodide (PI) staining to assess nuclear morphology and by Annexin V staining. Apoptotic signaling pathways were investigated by quantitative reverse transcription–polymerase chain reaction (RT-qPCR) and Western blotting. Results BmKn-2 showed potent cytotoxic effects towards both HSC4 and KB cells with the associated induction of apoptosis. The cells showed distinct morphological changes, nuclear disintegration and an increase in the number of Annexin V-positive cells. Interestingly, at concentrations which kill cancerous cells, BmKn-2 did not affect cell viability or mediate the induction of apoptosis in normal HGC or DPC. Induction of apoptosis by BmKn-2 in HSC4 and KB cells was associated with the activation of tumor suppress p53. Pro-apoptotic BAX expression was increased, whereas antiapoptotic BCL-2 expression was decreased in BmKn-2 exposed HSC4 and KB cells. BmKn-2 treated-oral cancer cells showed distinct upregulation of initiator caspase-9, with no effect on caspase-8 expression. Increased expression levels of executor caspases-3 and −7 were also found in treated cells for both oral cancers. Conclusion This study has suggested for the first time that BmKn-2 exerts selective cytotoxic effects on human oral cancer cells by inducting apoptosis via a p53-dependent intrinsic apoptotic pathway. BmKn-2 Peptide originally derived from a natural source shows great promise as a candidate treatment for oral cancer, with minimal effects on healthy tissue.
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BmKn-2 Scorpion Venom Peptide for killing oral cancer cells by apoptosis.
Asian Pacific Journal of Cancer Prevention, 2015Co-Authors: Pirut Tong-ngam, Sittiruk Roytrakul, Hathaitip SritanaudomchaiAbstract:Scorpion Venom Peptides recently have attracted attention as alternative chemotherapeutic agents that may overcome the limitations of current drugs, providing specific cytotoxicity for cancer cells with an ability to bypass multidrug-resistance mechanisms, additive effects in combination therapy and safety. In the present study, BmKn-2 Scorpion Venom Peptide and its derivatives were chosen for assessment of anticancer activities. BmKn-2 was identified as the most effective against human oral squamous cells carcinoma cell line (HSC-4) by screening assays with an IC 50 value of 29 µg/ml. The BmKn-2 Peptide killed HSC-4 cells through induction of apoptosis, as confirmed by phase contrast microscopy and RT-PCR techniques. Typical morphological features of apoptosis including cell shrinkage and rounding characteristics were observed in treated HSC-4 cells. The results were further confirmed by increased expression of pro-apoptotic genes such as caspase-3, -7, and -9 but decrease mRNA level of anti-apoptotic BCL-2 in BmKn-2 treated cells, as determined by RT-PCR assay. In summary, the BmKn-2 Scorpion Venom Peptide demonstrates specific membrane binding, growth inhibition and apoptogenic activity against human oral cancer cells.
Duangkamol Kunthalert - One of the best experts on this subject based on the ideXlab platform.
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a Scorpion Venom Peptide derivative bmkn 22 with potent antibiofilm activity against pseudomonas aeruginosa
PLOS ONE, 2019Co-Authors: Kittitat Teerapo, Anchalee Sistayanarain, Sittiruk Roytrakul, Duangkamol KunthalertAbstract:Pseudomonas aeruginosa is a leading cause of nosocomial and serious life-threatening infections and infections caused by this bacterium continue to pose a major medical challenge worldwide. The ability of P. aeruginosa to produce multiple virulence factors and in particular to form biofilms makes this bacterium resistant to all known antibiotics. As a consequence, standard antibiotic therapy are increasingly become ineffective to clear such infections associated with biofilms. In search for novel effective agents to combat P. aeruginosa biofilm infections, a series of the BmKn‒2 Scorpion Venom Peptide and its truncated derivatives were synthesized and their antibiofilm activities assessed. Among the Peptides tested, BmKn‒22 Peptide, which was a modified Peptide of the parental BmKn‒2 Scorpion Venom Peptide, clearly demonstrated the most potential inhibitory activity against P. aeruginosa biofilms without affecting the bacterial growth. This Peptide was not only capable of inhibiting the formation of P. aeruginosa biofilms, but also disrupting the established biofilms of P. aeruginosa. Additionally, BmKn‒22 Peptide was able to inhibit the production of key virulence factor pyocyanin of P. aeruginosa. Our results also showed that BmKn‒22 Peptide significantly reduced lasI and rhlR expression, and suggested that BmKn‒22 Peptide-mediated inhibition of P. aeruginosa biofilms and virulence factors was achieved through the components of quorum-sensing systems. Combination of BmKn‒22 Peptide with azithromycin resulted in a remarkable reduction P. aeruginosa biofilms. Since this Peptide exhibited low toxicity to mammalian cells, all our results therefore indicate that the BmKn‒22 Peptide is a promising antibiofilm agent against P. aeruginosa and warrant further development of this Peptide as a novel therapeutic for treatment of P. aeruginosa‒associated biofilm infections.
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A Scorpion Venom Peptide derivative BmKn‒22 with potent antibiofilm activity against Pseudomonas aeruginosa.
PLOS ONE, 2019Co-Authors: Kittitat Teerapo, Anchalee Sistayanarain, Sittiruk Roytrakul, Duangkamol KunthalertAbstract:Pseudomonas aeruginosa is a leading cause of nosocomial and serious life-threatening infections and infections caused by this bacterium continue to pose a major medical challenge worldwide. The ability of P. aeruginosa to produce multiple virulence factors and in particular to form biofilms makes this bacterium resistant to all known antibiotics. As a consequence, standard antibiotic therapy are increasingly become ineffective to clear such infections associated with biofilms. In search for novel effective agents to combat P. aeruginosa biofilm infections, a series of the BmKn‒2 Scorpion Venom Peptide and its truncated derivatives were synthesized and their antibiofilm activities assessed. Among the Peptides tested, BmKn‒22 Peptide, which was a modified Peptide of the parental BmKn‒2 Scorpion Venom Peptide, clearly demonstrated the most potential inhibitory activity against P. aeruginosa biofilms without affecting the bacterial growth. This Peptide was not only capable of inhibiting the formation of P. aeruginosa biofilms, but also disrupting the established biofilms of P. aeruginosa. Additionally, BmKn‒22 Peptide was able to inhibit the production of key virulence factor pyocyanin of P. aeruginosa. Our results also showed that BmKn‒22 Peptide significantly reduced lasI and rhlR expression, and suggested that BmKn‒22 Peptide-mediated inhibition of P. aeruginosa biofilms and virulence factors was achieved through the components of quorum-sensing systems. Combination of BmKn‒22 Peptide with azithromycin resulted in a remarkable reduction P. aeruginosa biofilms. Since this Peptide exhibited low toxicity to mammalian cells, all our results therefore indicate that the BmKn‒22 Peptide is a promising antibiofilm agent against P. aeruginosa and warrant further development of this Peptide as a novel therapeutic for treatment of P. aeruginosa‒associated biofilm infections.
Wenxin Li - One of the best experts on this subject based on the ideXlab platform.
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antibacterial activity and mechanism of a Scorpion Venom Peptide derivative in vitro and in vivo
PLOS ONE, 2012Co-Authors: Zhongjie Li, Yingliang Wu, Yu Song, Wenxin LiAbstract:BmKn2 is an antimicrobial Peptide (AMP) characterized from the Venom of Scorpion Mesobuthus martensii Karsch by our group. In this study, Kn2-7 was derived from BmKn2 to improve the antibacterial activity and decrease hemolytic activity. Kn2-7 showed increased inhibitory activity against both Gram-positive bacteria and Gram-negative bacteria. Moreover, Kn2-7 exhibited higher antibacterial activity against clinical antibiotic-resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA). In addition, the topical use of Kn2-7 effectively protected the skin of mice from infection in an S. aureus mouse skin infection model. Kn2-7 exerted its antibacterial activity via a bactericidal mechanism. Kn2-7 killed S. aureus and E. coli rapidly by binding to the lipoteichoic acid (LTA) in the S. aureus cell wall and the lipopolysaccharides (LPS) in the E. coli cell wall, respectively. Finally, the hemolytic activity of Kn2-7 was significantly decreased, compared to the wild-type Peptide BmKn2. Taken together, the Kn2-7 Peptide can be developed as a topical therapeutic agent for treating bacterial infections.
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anti hiv 1 activity of a new Scorpion Venom Peptide derivative kn2 7
PLOS ONE, 2012Co-Authors: Yaoqing Chen, Maohua Zhong, Dihan Zhou, Benxia He, Yaoming Li, Qiaoli Li, Jingyi Yang, Jie Yu, Yan Zhang, Wenxin LiAbstract:For over 30 years, HIV/AIDS has wreaked havoc in the world. In the absence of an effective vaccine for HIV, development of new anti-HIV agents is urgently needed. We previously identified the antiviral activities of the Scorpion-Venom-Peptide-derived mucroporin-M1 for three RNA viruses (measles viruses, SARS-CoV, and H5N1). In this investigation, a panel of Scorpion Venom Peptides and their derivatives were designed and chosen for assessment of their anti-HIV activities. A new Scorpion Venom Peptide derivative Kn2-7 was identified as the most potent anti-HIV-1 Peptide by screening assays with an EC50 value of 2.76 µg/ml (1.65 µM) and showed low cytotoxicity to host cells with a selective index (SI) of 13.93. Kn2-7 could inhibit all members of a standard reference panel of HIV-1 subtype B pseudotyped virus (PV) with CCR5-tropic and CXCR4-tropic NL4-3 PV strain. Furthermore, it also inhibited a CXCR4-tropic replication-competent strain of HIV-1 subtype B virus. Binding assay of Kn2-7 to HIV-1 PV by Octet Red system suggested the anti-HIV-1 activity was correlated with a direct interaction between Kn2-7 and HIV-1 envelope. These results demonstrated that Peptide Kn2-7 could inhibit HIV-1 by direct interaction with viral particle and may become a promising candidate compound for further development of microbicide against HIV-1.
Wei-hua Dong - One of the best experts on this subject based on the ideXlab platform.
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effects of Scorpion Venom Peptide b5 on hematopoietic recovery in irradiated mice and the primary mechanisms
Scientific Reports, 2015Co-Authors: Caixia Wang, Meixun Zhou, Yan Wang, Baiqian Xing, Tianhan Kong, Wei-hua DongAbstract:Scorpion Venom Peptide B5 (SVP-B5) stimulates recovery of hematopoiesis after exposure to radiation. However, its radioprotective effects and mechanisms are still unclear. The aim of this study was to investigate the effects of SVP-B5 on hematopoietic recovery in mice after total body irradiation (TBI) at a dose of 7.5 Gy and 6 Gy and to explore the possible primary mechanisms. SVP-B5 at a dose of 2.63 μg/kg significantly reduced the mortality rate of mice after TBI (p < 0.05). It showed markedly protective effects against radiation injury. SVP-B5 also significantly increased the number of bone marrow nucleated cells (BMNCs) and increased the colony forming unit (CFU) number in irradiated mice, accelerated the post-irradiation recovery of peripheral blood leukocytes and platelets in mice. SVP-B5 treatment markedly reduced the Reactive Oxygen Species (ROS) levels in BMNCs after TBI, reduced γH2AX levels, and decreased the relative expression levels of p16 and p21 mRNA at day 14 (d14) after irradiation. Our study indicated that SVP-B5 could partially mitigate radiation-induced DNA damage, enhance the post-radiation hematopoietic recovery, and improve the survival rate probably through the ROS-p16/p21 pathway.
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Effect of Scorpion Venom Peptide on haematopoietic stem and progenitor cells in mice with radiation injury
2007Co-Authors: Wei-hua DongAbstract:Objective To investigate the effect of different components of Scorpion Venom Peptide (SVP)on stem and progenitor cells in irradiated mice. Methods Mice were exposed to 6.0 Gy X-rays. The number of colony-forming unit of spleen (CFU-S) was calculated at the 10th day after irradiation, and the methyleellulose culture method was used to detect the CFU-Mix on the irradiated mice at different time in vivo and in vitro. Results The study of SVP components in vivo showed that the number of CFU-S was significantly elevated by SVPⅣafter the irradiation, and CFU-Mix was also increased by both SVPⅣ and SVPⅤ. In vitro experiment showed that the number of CFU-Mix was much higher in SVPⅣ, SVPⅤ and cytokines groups respectively, as compared with control group. Both SVP Ⅳ and SVP Ⅴ had prominent effects in the formation of CFU-Mix when combined with cytokines. Conclusion SVP has a protective effect on the bone marrow hematopoietie stem and progenitor cells in irradiated mice. Key words: Scorpion Venoms; Radiation injuries; Colony-forming unit; Stem cell; Progenitor cell
Kittitat Teerapo - One of the best experts on this subject based on the ideXlab platform.
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a Scorpion Venom Peptide derivative bmkn 22 with potent antibiofilm activity against pseudomonas aeruginosa
PLOS ONE, 2019Co-Authors: Kittitat Teerapo, Anchalee Sistayanarain, Sittiruk Roytrakul, Duangkamol KunthalertAbstract:Pseudomonas aeruginosa is a leading cause of nosocomial and serious life-threatening infections and infections caused by this bacterium continue to pose a major medical challenge worldwide. The ability of P. aeruginosa to produce multiple virulence factors and in particular to form biofilms makes this bacterium resistant to all known antibiotics. As a consequence, standard antibiotic therapy are increasingly become ineffective to clear such infections associated with biofilms. In search for novel effective agents to combat P. aeruginosa biofilm infections, a series of the BmKn‒2 Scorpion Venom Peptide and its truncated derivatives were synthesized and their antibiofilm activities assessed. Among the Peptides tested, BmKn‒22 Peptide, which was a modified Peptide of the parental BmKn‒2 Scorpion Venom Peptide, clearly demonstrated the most potential inhibitory activity against P. aeruginosa biofilms without affecting the bacterial growth. This Peptide was not only capable of inhibiting the formation of P. aeruginosa biofilms, but also disrupting the established biofilms of P. aeruginosa. Additionally, BmKn‒22 Peptide was able to inhibit the production of key virulence factor pyocyanin of P. aeruginosa. Our results also showed that BmKn‒22 Peptide significantly reduced lasI and rhlR expression, and suggested that BmKn‒22 Peptide-mediated inhibition of P. aeruginosa biofilms and virulence factors was achieved through the components of quorum-sensing systems. Combination of BmKn‒22 Peptide with azithromycin resulted in a remarkable reduction P. aeruginosa biofilms. Since this Peptide exhibited low toxicity to mammalian cells, all our results therefore indicate that the BmKn‒22 Peptide is a promising antibiofilm agent against P. aeruginosa and warrant further development of this Peptide as a novel therapeutic for treatment of P. aeruginosa‒associated biofilm infections.
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A Scorpion Venom Peptide derivative BmKn‒22 with potent antibiofilm activity against Pseudomonas aeruginosa.
PLOS ONE, 2019Co-Authors: Kittitat Teerapo, Anchalee Sistayanarain, Sittiruk Roytrakul, Duangkamol KunthalertAbstract:Pseudomonas aeruginosa is a leading cause of nosocomial and serious life-threatening infections and infections caused by this bacterium continue to pose a major medical challenge worldwide. The ability of P. aeruginosa to produce multiple virulence factors and in particular to form biofilms makes this bacterium resistant to all known antibiotics. As a consequence, standard antibiotic therapy are increasingly become ineffective to clear such infections associated with biofilms. In search for novel effective agents to combat P. aeruginosa biofilm infections, a series of the BmKn‒2 Scorpion Venom Peptide and its truncated derivatives were synthesized and their antibiofilm activities assessed. Among the Peptides tested, BmKn‒22 Peptide, which was a modified Peptide of the parental BmKn‒2 Scorpion Venom Peptide, clearly demonstrated the most potential inhibitory activity against P. aeruginosa biofilms without affecting the bacterial growth. This Peptide was not only capable of inhibiting the formation of P. aeruginosa biofilms, but also disrupting the established biofilms of P. aeruginosa. Additionally, BmKn‒22 Peptide was able to inhibit the production of key virulence factor pyocyanin of P. aeruginosa. Our results also showed that BmKn‒22 Peptide significantly reduced lasI and rhlR expression, and suggested that BmKn‒22 Peptide-mediated inhibition of P. aeruginosa biofilms and virulence factors was achieved through the components of quorum-sensing systems. Combination of BmKn‒22 Peptide with azithromycin resulted in a remarkable reduction P. aeruginosa biofilms. Since this Peptide exhibited low toxicity to mammalian cells, all our results therefore indicate that the BmKn‒22 Peptide is a promising antibiofilm agent against P. aeruginosa and warrant further development of this Peptide as a novel therapeutic for treatment of P. aeruginosa‒associated biofilm infections.