Histatin 5
(Synonyms: 富组蛋白5) 目录号 : GC31898
Histatin 5可抑制基质金属蛋白酶MMP-2和MMP-9的活性，IC50值分别为0.57μM和0.25μM。
Cas No.:115966-68-2
Sample solution is provided at 25 µL, 10mM.
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Histatin 5 suppresses the activities of matrix metalloproteinases MMP-2 and MMP-9 with IC50 values of 0.57 and 0.25μM, respectively[1]. Histatin 5 significantly inhibited the growth of a variety of Candida species by binding to Candida cell wall proteins (Ssa1/2) and glycans with MIC50 values of 10-20μg/ml[2]. Histatin 5 has been widely used in metal ion binding studies and antifungal studies[3].
In vitro, Histatin 5 at a concentration of 3200μg/mL for 24 hours was significantly cytotoxic to human gingival fibroblasts and dramatically inhibited cell viability[4]. Treatment of human gingival fibroblasts with 10μg/ml Histatin 5 for 20 minutes inhibited the production of inflammatory cytokines (IL-6 and IL-8) induced by P. gingivalis and lipopolysaccharides[5].
In vivo, Histatin 5 gel at a dose of 100μg/mL three times daily applied to the tongues of mice for three days prevented the occurrence of oral ulcers and significantly inhibited Candida albicans[6]. Administration of Histatin 5 (80μM) to the cornea three times daily for one day promoted wound healing in a mouse corneal injury model[7].
References:
[1] Gusman H, Travis J, Helmerhorst E J, et al. Salivary histatin 5 is an inhibitor of both host and bacterial enzymes implicated in periodontal disease[J]. Infection and immunity, 2001, 69(3): 1402-1408.
[2] Puri S, Edgerton M. How does it kill?: understanding the candidacidal mechanism of salivary histatin 5[J]. Eukaryotic cell, 2014, 13(8): 958-964.
[3] Zolin G V S, Fonseca F H, Zambom C R, et al. Histatin 5 metallopeptides and their potential against Candida albicans pathogenicity and drug resistance[J]. Biomolecules, 2021, 11(8): 1209.
[4] Moffa E B, Mussi M C M, Xiao Y, et al. Histatin 5 inhibits adhesion of C. albicans to reconstructed human oral epithelium[J]. Frontiers in Microbiology, 2015, 6: 885.
[5] Imatani T, Kato T, Minaguchi K, et al. Histatin 5 inhibits inflammatory cytokine induction from human gingival fibroblasts by Porphyromonas gingivalis[J]. Oral microbiology and immunology, 2000, 15(6): 378-382.
[6] Kong E F, Tsui C, Boyce H, et al. Development and in vivo evaluation of a novel histatin-5 bioadhesive hydrogel formulation against oral candidiasis[J]. Antimicrobial agents and chemotherapy, 2016, 60(2): 881-889.
[7] Shah D, Son K N, Kalmodia S, et al. Wound healing properties of histatin-5 and identification of a functional domain required for histatin-5-induced cell migration[J]. Molecular Therapy Methods & Clinical Development, 2020, 17: 709-716.
Histatin 5可抑制基质金属蛋白酶MMP-2和MMP-9的活性，IC50值分别为0.57μM和0.25μM [1]。Histatin 5能通过结合念珠菌的细胞壁蛋白（Ssa1/2）和多糖，显著抑制多种念珠菌的生长，MIC50值为10-20μg/ml[2]。Histatin 5已广泛应用于金属离子结合研究和抗真菌研究[3]。
在体外，使用3200μg/mL浓度的Histatin 5处理人牙龈成纤维细胞 24 小时，可显著诱导细胞毒性并大幅降低细胞活力[4]。以10μg/ml浓度的Histatin 5 处理人牙龈成纤维细胞20分钟，能抑制牙龈卟啉单胞菌和脂多糖诱导的炎症细胞因子（IL-6和IL-8）产生[5]。
在体内，在小鼠舌面涂抹100μg/mL的Histatin 5凝胶（每日3次，连续3天），可预防口腔溃疡的发生并显著抑制白色念珠菌生长[6]。在小鼠角膜损伤模型中，每日3次局部施用80μM的Histatin 5（持续1天），可促进角膜伤口愈合[7]。
| Cell experiment [1]: | |
Cell lines | Human gingival fibroblast cells |
Preparation Method | The cytotoxic effect of Histatin 5 was assessed on human gingival fibroblast cells grown in Dulbeccco's modified Eagle medium supplemented with antibiotic-fungal solution and 10% v/v fetal bovine serum. The incubation temperature was 37°C with 5% CO2 in air and 95% air concentration. Cells were cultured to confluence (90%) and removed with trypsin (0.05%)/EDTA (0.02%) in 1×PBS. Medium was added to inactivate trypsin, and cells were then centrifuged at 2000rpm for 5min, resuspended, and re-seeded. The medium was changed two to three times a week. Total viable cell counts were performed in an incubator. Cell suspensions containing 2.0×104 cells/ml were incubated in 24-well plates for 48 hours at 37°C in a humidified environment with 5% CO2. At the end of the culture, the medium was discarded, and adherent cells remained at the bottom of the plate. Gradient dilutions of Histatin 5 (100, 200, 400, 800, 1600, 3200, 6400, and 12800μg/mL) were performed with fresh medium. The plates were incubated at 37°C in an atmosphere of 5% CO2 and 95% air for 24 hours. MTT assay was used to measure mitochondrial dehydrogenase activity. After the cells were grown in the control or test medium for 24h, 100μL of MTT stock solution was added to each well. The culture plates were incubated at 37°C in 5% CO2 for 4 hours. At the end of incubation, the cultures were removed from the incubator and 100μL of MTT solubilization solution was added to dissolve the resulting formazan crystals. The plates were then shaken until the crystals were completely dissolved, and the absorbance was measured at a wavelength of 570nm by spectrophotometry; all experiments were performed three times. |
Reaction Conditions | 100, 200, 400, 800, 1600, 3200, 6400, and 12800μg/mL; 24h |
Applications | Histatin 5 at concentrations above 3200μg/mL was significantly cytotoxic, resulting in an apparent reduction in gingival fibroblast cell viability. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | The C57BL/6J mice aged between twelve and nineteen weeks received anesthesia through an intraperitoneal injection containing ketamine at 100mg/kg and xylazine at 5mg/kg. A circular 2.0-mm central epithelial segment was delineated with a 2-mm biopsy punch following 2 drops of topical 0.5% proparacaine, then removed with a brush. Histatin 5 (80μM), SHRGY (80μM) was applied to the cornea three times a day during the treatment (n = 7) or the control (n = 7) group. At 0, 18, and 24h, corneas were stained with fluorescein and imaged using a photo-slit lamp with a camera. The remaining wound areas were measured with the ImageJ software at each indicated time point and were compared with the baseline wound area for each mouse. The percentage of the remaining wound area was calculated for each time point. |
Dosage form | 80μM for three times a day; apply to the cornea |
Applications | Histatin 5 treatment significantly promoted wound healing in a mouse corneal injury model. |
References: | |
| Cas No. | 115966-68-2 | SDF | |
| 别名 | 富组蛋白5 | ||
| Canonical SMILES | Asp-Ser-His-Ala-Lys-Arg-His-His-Gly-Tyr-Lys-Arg-Lys-Phe-His-Glu-Lys-His-His-Ser-His-Arg-Gly-Tyr | ||
| 分子式 | C133H195N51O33 | 分子量 | 3036.29 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.3293 mL | 1.6467 mL | 3.2935 mL |
| 5 mM | 0.0659 mL | 0.3293 mL | 0.6587 mL |
| 10 mM | 0.0329 mL | 0.1647 mL | 0.3293 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >98.00%
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