Heterophyllin B
(Synonyms: 太子参环肽B) 目录号 : GC38168
Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla, which provides a novel strategy for the treatment of esophageal cancer.
Cas No.:145459-19-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla, which provides a novel strategy for the treatment of esophageal cancer.
[1] Tantai JC, et al. Mol Med Rep. 2016 Feb;13(2):1097-104.
| Cas No. | 145459-19-4 | SDF | |
| 别名 | 太子参环肽B | ||
| Canonical SMILES | O=C([C@@](CCC1)([H])N1C([C@](NC(CNC(CNC2=O)=O)=O)([H])CC(C)C)=O)N(CCC3)[C@]3([H])C(N(CCC4)[C@]4([H])C(N[C@@](C(N[C@H]2CC5=CC=CC=C5)=O)([H])[C@@H](C)CC)=O)=O | ||
| 分子式 | C40H58N8O8 | 分子量 | 778.94 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2838 mL | 6.419 mL | 12.838 mL |
| 5 mM | 0.2568 mL | 1.2838 mL | 2.5676 mL |
| 10 mM | 0.1284 mL | 0.6419 mL | 1.2838 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Heterophyllin B, a cyclopeptide from Pseudostellaria heterophylla, improves memory via immunomodulation and neurite regeneration in i.c.v.Aβ-induced mice
Food Res Int 2022 Aug;158:111576.PMID:35840261DOI:10.1016/j.foodres.2022.111576.
Pseudostellaria heterophylla, has historically been used as medicine food homology plant for thousand years in China. Our previous studies had indicated that daily intake of Pseudostellaria heterophylla extract enhanced cognitive memory. Herein, Heterophyllin B (HET-B), a brain permeable cyclopeptide from Pseudostellaria heterophylla was determined, and the molecular mechanism underlying its memory improvement effects was investigated. Pseudostellaria heterophylla extract as well as HET-B reversed Aβ25-35-induced axonal atrophy and neuronal apoptosis in cultured cortical neurons of mice. HET-B could enhance memory retrieval, modulate splenic T helper cell, and ameliorate neuroinflammation in i.c.v. Aβ1-42 injected Alzheimer's disease (AD) mice. To explore the mechanism of action, network pharmacology was performed to predict protein targets and pathways of HET-B against AD. Five key targets were identified related to the effect of HET-B in AD intervention, and were clarified involved in axonal regeneration. We revealed for the first time that HET-B promoted memory retrieval through axonal regeneration and anti-neuroinflammation. This study provides a basis to research on HET-B as nutritional supplements for brain healthy.
Protective effects of Heterophyllin B against bleomycin-induced pulmonary fibrosis in mice via AMPK activation
Eur J Pharmacol 2022 Apr 15;921:174825.PMID:35283110DOI:10.1016/j.ejphar.2022.174825.
Pulmonary fibrosis (PF) is a chronic interstitial lung disease with unknown etiology. In the present study, we evaluated the anti-fibrotic effects of Heterophyllin B, a natural product from Radix Pseudostellariae having anti-inflammatory and tyrosinase inhibitory activities. In bleomycin (BLM)-induced PF mouse model, Heterophyllin B treatments (5 or 20 mg/kg/d) significantly attenuated BLM-induced alveolar cavity collapse, inflammatory cell infiltration, alveolar wall thickening and collagen deposition. When compared to model group, Heterophyllin B treatments also increased adenosine 5'-monophosphate (AMP)-activated protein kinase (AMPK) phosphorylation levels by 359% (P < 0.001) and reduced the expression of stimulator of interferon genes (STING) by 73% (P < 0.001). Furthermore, co-administration of Heterophyllin B with AMPK inhibitor dorsomorphin (Compound C) significantly blocked the improvement effects of Heterophyllin B on BLM-damaged lung tissue, and also increased the protein expression of STING which was inhibited by Heterophyllin B in fibrotic lungs (P < 0.001). It is known that alveolar epithelia and lung fibroblasts exert prominent roles in the fibrosis progression. In the present study we found that, in vitro, Heterophyllin B significantly inhibited alveolar epithelial mesenchymal transition (EMT) and lung fibroblast transdifferentiation. We also found that the inhibition of Heterophyllin B on lung fibroblast transdifferentiation and STING expression was reversed by Compound C. To summarize, Heterophyllin B exhibited protective effects on BLM-induced lung fibrosis potentially by inhibiting TGF-Smad2/3 signalings and AMPK-mediated STING signalings.
Heterophyllin B, a cyclopeptide from Pseudostellaria heterophylla, enhances cognitive function via neurite outgrowth and synaptic plasticity
Phytother Res 2021 Sep;35(9):5318-5329.PMID:34328653DOI:10.1002/ptr.7212.
Neurite outgrowth-induced construction of neural circuits and networks is responsible for memory generalization, consolidation, and retrieval. In this study, we found that the traditional Chinese medicine Pseudostellaria heterophylla promoted neurite regrowth and enhanced cognitive function in normal mice. Further, we orally administered Pseudostellaria heterophylla water extracts (PHE) to ICR mice, and detected Heterophyllin B (HET-B), an important cyclopeptide, in the plasma and cerebral cortex. We demonstrated that neurites were significantly elongated after coculturing with HET-B for 4 days. Next, the intraperitoneal injection of HET-B on seven consecutive days in 3-month-old ICR mice significantly enhanced the object recognition memory and object location memory than that in control. Immunohistochemical analysis indicated significantly increased β3-tubulin-positive neurite density, synaptophysin, and postsynaptic density 95 in the perirhinal cortex and hippocampus after administering HET-B. Furthermore, the concentration of neurotransmitters was measured using HPLC analysis; HET-B significantly increased five-levels of HT in the hippocampus, and decreased metabolites of dopamine, dihydroxyphenylacetic acid, and homovanillic acid, in the prefrontal cortex and hippocampus. Taken together, HET-B induces neurite elongation and neurotransmitter regulation and possibly enhances cognitive memory.
Heterophyllin B an Active Cyclopeptide Alleviates Dextran Sulfate Sodium-Induced Colitis by Modulating Gut Microbiota and Repairing Intestinal Mucosal Barrier via AMPK Activation
Mol Nutr Food Res 2022 Sep;66(17):e2101169.PMID:35796402DOI:10.1002/mnfr.202101169.
Scope: Advances in pathology broaden the perception of the intimate interaction between gut microbiota dysbiosis and the pathogenesis of ulcerative colitis (UC), but the potential modulating roles remain to be elucidated. Methods and results: DSS-induced colitis is used to investigate the effect of Heterophyllin B (HB), a typical active cyclopeptide extracted from Pseudostellaria heterophylla, on colitis and gut microbiota. Administration of HB substantially mitigates the symptoms of UC as evidenced by increasing body weight and colon length, as well as decreased macrophages infiltration in the colon. Meanwhile, HB significantly alleviates intestinal mucosal barrier dysfunction by reducing the production of inflammatory cytokines, while all the mentioned beneficial effects are significantly eliminated by co-treatment with compound C, a selective AMPK inhibitor. In addition, 16S rDNA gene analyses and fecal microbiota transplantation also reveal that HB dramatically prevents against UC by reshaping intestinal dysbiosis, especially elevates the relative abundance of Akkermansia muciniphila. Conclusion: These findings illustrate that HB prominently improves intestinal epithelial homeostasis via activating AMPK and ameliorates the colonic inflammation in a gut microbiota-dependent manner, which provide evidence for microbial contribution to UC pathogenesis and suggesting a novel approach for colitis prevention.
The Biosynthesis of Heterophyllin B in Pseudostellaria heterophylla From prePhHB-Encoded Precursor
Front Plant Sci 2019 Oct 17;10:1259.PMID:31749814DOI:10.3389/fpls.2019.01259.
Plant cyclic peptides (CPs) are a large group of small molecule metabolites found in a wide variety of plants, including traditional Chinese medicinal plants. However, the majority of plant CPs have not been studied for their biosynthetic mechanisms, including Heterophyllin B (HB), which is one of the characteristic chemical components of Pseudostellaria heterophylla. Here, we screened the precursor gene (prePhHB) of HB in P. heterophylla and functionally identified its correctness in vivo and in vitro. First, we developed a new method to screen the precursors of HB from 16 candidate linear peptides. According to transcriptome sequencing data, we cloned the genes that encoded the HB precursor peptides and confirmed that the prePhHB-encoded precursor peptide could enzymatically synthesize HB. Next, we generated the transgenic tobacco that expressed prePhHB, and the results showed that HB was detected in transgenic tobacco. Moreover, we revealed that prePhHB gene expression is positively correlated with HB accumulation in P. heterophylla. Mutations in the prePhHB gene may influence the accumulation of HB in P. heterophylla. These results suggest that HB is ribosomally synthesized and posttranslationally modified peptide (RiPP) derived from the precursor gene prePhHB-encoded precursor peptide, and the core peptide sequence of HB is IFGGLPPP in P. heterophylla. This study developed a new idea for the rapid identification of Caryophyllaceae-type CP precursor peptides via RNA-sequencing data mining.