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Histatin-1

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

Histatin-1 is an antibacterial peptide isolated from Macaca fascicularis. It shows antibacterial and antifungal activity.

Category

Functional Peptides

Catalog number

BAT-012391

CAS number

101056-53-5

Molecular Formula

C217H298N69O64P

Molecular Weight

4928

Specification
Reference Reading

IUPAC Name

(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-3-phosphonooxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid

Synonyms

HTN1 protein, human; Histatin 1, human; H-Asp-Ser(PO3H2)-His-Glu-Lys-Arg-His-His-Gly-Tyr-Arg-Arg-Lys-Phe-His-Glu-Lys-His-His-Ser-His-Arg-Glu-Phe-Pro-Phe-Tyr-Gly-Asp-Tyr-Gly-Ser-Asn-Tyr-Leu-Tyr-Asp-Asn-OH

Purity

98.3%

Sequence

DSpHEKRHHGYRRKFHEKHHSHREFPFYGDYGSNYLYDN

Storage

Store at -20°C

InChI

InChI=1S/C217H298N69O64P/c1-112(2)71-144(193(325)270-150(78-120-45-55-132(293)56-46-120)197(329)280-161(91-178(309)310)207(339)283-163(213(345)346)89-169(223)295)266-195(327)149(77-119-43-53-131(292)54-44-119)271-205(337)159(88-168(222)294)279-208(340)164(102-287)255-172(298)101-244-181(313)146(75-117-39-49-129(290)50-40-117)268-206(338)160(90-177(307)308)254-171(297)100-243-180(312)145(74-116-37-47-128(289)48-38-116)267-198(330)151(73-114-25-8-4-9-26-114)281-211(343)167-36-22-70-286(167)212(344)162(79-115-27-10-5-11-28-115)282-192(324)143(59-62-175(303)304)263-186(318)139(34-20-68-241-216(228)229)262-199(331)154(82-123-94-234-107-248-123)277-209(341)165(103-288)284-204(336)158(86-127-98-238-111-252-127)276-203(335)157(85-126-97-237-110-251-126)273-188(320)136(31-14-17-65-220)258-191(323)142(58-61-174(301)302)264-200(332)153(81-122-93-233-106-247-122)275-196(328)148(72-113-23-6-3-7-24-113)269-187(319)135(30-13-16-64-219)256-184(316)137(32-18-66-239-214(224)225)259-185(317)138(33-19-67-240-215(226)227)261-194(326)147(76-118-41-51-130(291)52-42-118)253-170(296)99-245-182(314)152(80-121-92-232-105-246-121)272-202(334)156(84-125-96-236-109-250-125)274-189(321)140(35-21-69-242-217(230)231)260-183(315)134(29-12-15-63-218)257-190(322)141(57-60-173(299)300)265-201(333)155(83-124-95-235-108-249-124)278-210(342)166(104-350-351(347,348)349)285-179(311)133(221)87-176(305)306/h3-11,23-28,37-56,92-98,105-112,133-167,287-293H,12-22,29-36,57-91,99-104,218-221H2,1-2H3,(H2,222,294)(H2,223,295)(H,232,246)(H,233,247)(H,234,248)(H,235,249)(H,236,250)(H,237,251)(H,238,252)(H,243,312)(H,244,313)(H,245,314)(H,253,296)(H,254,297)(H,255,298)(H,256,316)(H,257,322)(H,258,323)(H,259,317)(H,260,315)(H,261,326)(H,262,331)(H,263,318)(H,264,332)(H,265,333)(H,266,327)(H,267,330)(H,268,338)(H,269,319)(H,270,325)(H,271,337)(H,272,334)(H,273,320)(H,274,321)(H,275,328)(H,276,335)(H,277,341)(H,278,342)(H,279,340)(H,280,329)(H,281,343)(H,282,324)(H,283,339)(H,284,336)(H,285,311)(H,299,300)(H,301,302)(H,303,304)(H,305,306)(H,307,308)(H,309,310)(H,345,346)(H4,224,225,239)(H4,226,227,240)(H4,228,229,241)(H4,230,231,242)(H2,347,348,349)/t133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,159-,160-,161-,162-,163-,164-,165-,166-,167-/m0/s1

InChI Key

CUOPXNHMMIAXEF-AKRYILKSSA-N

Canonical SMILES

CC(C)CC(C(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC(=O)O)C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CC(=O)N)NC(=O)C(CO)NC(=O)CNC(=O)C(CC3=CC=C(C=C3)O)NC(=O)C(CC(=O)O)NC(=O)CNC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)C6CCCN6C(=O)C(CC7=CC=CC=C7)NC(=O)C(CCC(=O)O)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC8=CN=CN8)NC(=O)C(CO)NC(=O)C(CC9=CN=CN9)NC(=O)C(CC1=CN=CN1)NC(=O)C(CCCCN)NC(=O)C(CCC(=O)O)NC(=O)C(CC1=CN=CN1)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(CCCCN)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC1=CC=C(C=C1)O)NC(=O)CNC(=O)C(CC1=CN=CN1)NC(=O)C(CC1=CN=CN1)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCCN)NC(=O)C(CCC(=O)O)NC(=O)C(CC1=CN=CN1)NC(=O)C(COP(=O)(O)O)NC(=O)C(CC(=O)O)N

1. Histatin-1 Attenuates LPS-Induced Inflammatory Signaling in RAW264.7 Macrophages

Sang Min Lee, Kyung-No Son, Dhara Shah, Marwan Ali, Arun Balasubramaniam, Deepak Shukla, Vinay Kumar Aakalu Int J Mol Sci. 2021 Jul 23;22(15):7856. doi: 10.3390/ijms22157856.

Macrophages play a critical role in the inflammatory response to environmental triggers, such as lipopolysaccharide (LPS). Inflammatory signaling through macrophages and the innate immune system are increasingly recognized as important contributors to multiple acute and chronic disease processes. Nitric oxide (NO) is a free radical that plays an important role in immune and inflammatory responses as an important intercellular messenger. In addition, NO has an important role in inflammatory responses in mucosal environments such as the ocular surface. Histatin peptides are well-established antimicrobial and wound healing agents. These peptides are important in multiple biological systems, playing roles in responses to the environment and immunomodulation. Given the importance of macrophages in responses to environmental triggers and pathogens, we investigated the effect of histatin-1 (Hst1) on LPS-induced inflammatory responses and the underlying molecular mechanisms in RAW264.7 (RAW) macrophages. LPS-induced inflammatory signaling, NO production and cytokine production in macrophages were tested in response to treatment with Hst1. Hst1 application significantly reduced LPS-induced NO production, inflammatory cytokine production, and inflammatory signaling through the JNK and NF-kB pathways in RAW cells. These results demonstrate that Hst1 can inhibit LPS-induced inflammatory mediator production and MAPK signaling pathways in macrophages.

2. Histatin 1 enhanced the speed and quality of wound healing through regulating the behaviour of fibroblast

Liuhanghang Cheng, et al. Cell Prolif. 2021 Aug;54(8):e13087. doi: 10.1111/cpr.13087. Epub 2021 Jul 13.

Objectives: Histatin 1(Hst 1) has been proved to promote wound healing. However, there was no specific study on the regulation made by Hst 1 of fibroblasts in the process of wound healing. This research comprehensively studied the regulation of Hst 1 on the function of fibroblasts in the process of wound healing and preliminary mechanism about it. Materials and methods: The full-thickness skin wound model was made on the back of C57/BL6 mice. The wound healing, collagen deposition and fibroblast distribution were detected on days 3, 5 and 7 after injury. Fibroblast was cultured in vitro and stimulated with Hst 1, and then, their biological characteristics and functions were detected. Results: Histatin 1 can effectively promote wound healing, improve collagen deposition during and after healing and increase the number and function of fibroblasts. After healing, the mechanical properties of the skin also improved. In vitro, the migration ability of fibroblasts stimulated by Hst 1 was significantly improved, and the fibroblasts transformed more into myofibroblasts, which improved the function of contraction and collagen secretion. In fibroblasts, mTOR signalling pathway can be activated by Hst 1. Conclusions: Histatin 1 can accelerate wound healing and improve the mechanical properties of healed skin by promoting the function of fibroblasts. The intermolecular mechanisms need to be further studied, and this study provides a direction about mTOR signalling pathway.

3. Histatin-1 alleviates high-glucose injury to skin keratinocytes through MAPK signaling pathway

Li Pan, Xuanfen Zhang, Qiong Gao J Cosmet Dermatol. 2022 Nov;21(11):6281-6291. doi: 10.1111/jocd.15235. Epub 2022 Jul 27.

Background: Damage to keratinocytes and other skin cells in a high-glucose environment has been proven to be an important reason for the poor wound healing ability of chronic diabetes mellitus. Histatin-1 has been preliminarily proven to stimulate the wound healing process of the oral and non-oral mucosa and has been found to be related to the activation of extracellular signal-regulated kinase (ERK). Aim of the study: The purpose of this study was to investigate the effect of histatin-1 on high-glucose-injured keratinocytes and the role of the Ras-Raf-MEK-ERK signaling pathway on the effect of histatin-1 to improve diabetic wound healing. Methods: A human keratinocyte model damaged by high glucose was constructed, cell proliferation was detected by the Cell Counting Kit-8 assay, and cell apoptosis was detected by flow cytometry. The expression level of 8-hydroxy-2'-deoxyguanosine (8-OHdG) was detected by ELISA, and the mitogen-activated protein kinase (MAPK) signaling pathway protein expression level was detected by Western blot. C-fos mRNA expression was detected by real-time PCR. Results: The results indicated that histatin-1 promoted proliferation and reduced the rate of apoptosis and 8-OHdG content in keratinocytes with high-glucose injury. In addition, histatin-1 down-regulated MEK phosphorylation in keratinocytes with high-glucose injury. However, with the extension of the intervention, the effect of histatin-1 on c-fos mRNA expression was different. At the early stage of high-glucose injury (12 h), the expression of c-fos mRNA was not increased in high-glucose-injured keratinocytes treated with histatin-1 but then c-fos mRNA expression was gradually upregulated. Conclusion: Histatin-1 could alleviate keratinocyte injury caused by high glucose levels and promoted wound healing in vitro. In addition, histatin-1 could exert anti-apoptotic and antioxidant damage effects under high-glucose injury states. These effects of histatin-1 may be related to its regulation of the MAPK signaling pathway. Therefore, these findings provide an essential theoretical basis for histatin-1 to become a safe and effective new peptide biological agent to promote wound healing in patients with diabetes.