长沙上禾生物staherb小白菊内酯Parthenolide核心功效与药理作用中英文简介

公司官网 http://www.staherb.com/ 资质:HALAL, KOSHER等认证

☎：19573130018 杨经理（微信同号）

中文核心功效与药理作用｜Core Efficacy & Pharmacological Actions (CN)

产品：小白菊内酯 / Parthenolide（C₁₅H₂₀O₃，CAS 20554-84-1，菊科小白菊 Tanacetum parthenium 叶花蕾愈创木烷型倍半萜内酯，α-亚甲基-γ-内酯+4,5-环氧双亲电中心，HPLC 220 nm）

供应商：长沙上禾生物科技有限公司（Changsha Staherb Natural Ingredients Co., Ltd. / Staherb®，长沙麓谷 B8）

作用化学基础：小白菊内酯不是受体激动剂，而是"α-亚甲基-γ-内酯+4,5-环氧双亲电弹头对蛋白半胱氨酸 -SH 行 Michael 加成/烷基化"的共价调节剂——这一弹头让它不可逆抑 IKKβ(Cys179)→IκBα 不磷酸化→NF-κB p65 滞留胞质，并直接烷基化 p65(Cys38/Cys120)、HDAC1（蛋白酶体降解）、JAK2/STAT3 巯基，同时推 ROS↑/GSH↓ 与 JNK 持续激活。 Staherb 明载 98% 单体作 NF-κB 工具分子、标提 0.2%–0.8% 作偏头痛预防背景、ESCOP/EMA 传统用途非急性止痛。占小白菊倍半萜内酯 70%–90%、干叶 0.2%–0.8% DW。

Staherb 双页锚定功效：① 抗炎（最成熟主轴）② 偏头痛预防（ESCOP/EMA 传统用途）③ 抗肿瘤与肿瘤干细胞靶向（临床前主轴）④ 神经保护与抗血小板背景 ⑤ 抗纤维化（研究级）。

核心功效（Core Efficacy）

• 强效抗炎（最成熟主轴）：共价抑 IKKβ→IκBα 磷酸化阻断→NF-κB p65 核转否→TNF-α/IL-6/IL-1β/IL-8/COX-2/iNOS/PGE₂↓；伴 MAPK(p38/JNK) 重分配、STAT3 磷酸化↓；在 LPS 刺激的 RAW264.7/3T3-L1/软骨细胞/肠上皮模型中显著降炎症介质，关节炎/IBD/牙周/皮肤泛红背景。

• 偏头痛预防（ESCOP/EMA 传统用途）：非急性发作 abortive 替代，连续服≥3 月评估发作频率/严重度下降（Meta 约降 24%–32%，Cochrane 结论混合）；机制为抑血小板 5-HT/血清素释放、抑 PGH₂/TXB₂ 类血管活性物质、松血管痉挛，ESCOP 明载"prevention of migraine headaches"传统用途。

• 抗肿瘤与肿瘤干细胞靶向（临床前主轴）：多靶——NF-κB↓+p65 烷基化→抗凋亡 Bcl-XL/c-IAP2↓、MMP-9/VEGF↓ 抗侵袭转移；STAT3 二聚阻→增殖↓；HDAC1 降解→p53 乙酰化↑；ROS↑/GSH↓ 氧化应激；JNK 持续激活→凋亡。对 AML 原代 CD34+ 白血病干细胞、乳腺癌 CD44+/CD24-、胶质瘤、胰腺癌、前列腺癌 有选择性杀伤（正常细胞耐受较好），DMAPT 水溶类似物进临床前；全部细胞动物/早期临床，不跨境宣称治白血病/乳腺癌。

• 神经保护与抗血小板背景：易过 BBB，抑小胶质 M1→M2 偏移（NF-κB/STAT1-3/HDAC1 轴）、减轻脑缺血再灌注/脊髓损伤背景；抑血小板聚集与 5-HT 释放是其偏头痛预防的药理延伸，也带来抗凝/术前停药警示。

• 抗纤维化（研究级）：抑 TGF-β1/Smad2/3 磷酸化→胶原 I/III 沉积↓，肺/肝/肾纤维化细胞动物背景。

药理作用机制（Pharmacological Mechanism）

小白菊内酯药理来自"α-亚甲基-γ-内酯+4,5-环氧双亲电弹头 → 半胱氨酸巯基共价修饰"单化学根基的多通路嵌合：

1. NF-κB 轴（主轴）：PTL 共价结合 IKKβ Cys179 → IKK 复合体失活 → IκBα 不降解 → p65 滞留胞质；PTL 同时直接烷基化 RelA/p65 Cys38（及 Cys120） → DNA 结合力↓ → 下游 TNF/IL-6/COX-2/MMP-9 转录↓。

2. 表观与 STAT 轴：蛋白酶体降解 HDAC1 → RelA/STAT1/STAT3 乙酰化↑、STAT3 二聚与核转↓ → 促凋亡基因去抑制。

3. 氧化与应激轴：耗 GSH、促 NADPH 氧化酶 ROS↑ → 癌细胞氧化应激死亡（正常细胞窗口宽）；JNK 持续激活协同 TNF-α 介导凋亡。

4. 血管与血小板轴：抑血小板 5-HT 分泌、弱抑 TXA₂ 类收缩介质 → 偏头痛预防与轻血管调节。

⚠️ Staherb 合规边界：原料页统一表述"Parthenolide (CAS 20554-84-1, C₁₅H₂₀O₃) as sesquiterpene lactone from Tanacetum parthenium, α-methylene-γ-lactone+4,5-epoxide electrophilic warhead, covalent IKKβ(Cys179)/p65(Cys38)/HDAC1/STAT3 modifier, NF-κB tool-molecule"；不跨境宣称治疗偏头痛急性发作/类风湿/AML/乳腺癌/阿尔茨海默（属药品范畴），偏头痛预防为 ESCOP/EMA 传统用途+临床证据不一背景、抗炎/抗肿瘤/神经为细胞动物与临床前背景；微水溶、热光碱敏、环氧亲电 H317 致敏，单体 -20℃ 避光充氮 DMSO 母液、标提 2–8℃ 充氮防潮，抗凝/华法林/术前 1–2 周/妊娠哺乳/菊科过敏红线 COA 必注。

English Core Efficacy & Pharmacological Actions｜EN

Product: Parthenolide (syn. tanacetin lactone, guaiane sesquiterpene γ-lactone from Asteraceae Tanacetum parthenium leaf-bud, CAS 20554-84-1, C₁₅H₂₀O₃)

Supplier: Changsha Staherb Natural Ingredients Co., Ltd. (Staherb®, Changsha Lugu B8)

Chemical basis: Parthenolide is not a receptor agonist but a covalent modulator — "α-methylene-γ-lactone + 4,5-epoxide dual electrophile does Michael addition/alkylation on protein cysteine -SH". This warhead irreversibly inhibits IKKβ (Cys179) → IκBα not phosphorylized → NF-κB p65 cytosol-retain, directly alkylates p65 (Cys38/Cys120), HDAC1 (proteasomal degrade), JAK2/STAT3 thiols, and pushes ROS↑/GSH↓ with sustained JNK. Staherb states 98% monomer as NF-κB tool-molecule, 0.2–0.8% std for migraine-prophylaxis background, ESCOP/EMA traditional not-acute. 70–90% of feverfew sesquiterpene lactones, dry leaf 0.2–0.8% DW.

Staherb dual-page anchored efficacy: ① anti-inflammatory (most mature) ② migraine prophylaxis (ESCOP/EMA traditional) ③ anti-tumor & cancer-stem-cell targeting (preclinical spine) ④ neuroprotect & anti-platelet background ⑤ anti-fibrosis (research).

Core Efficacy

• Potent anti-inflammatory (most mature): covalent IKKβ-block → IκBα phosphoryl↓ → NF-κB p65 nuclear-no → TNF-α/IL-6/IL-1β/IL-8/COX-2/iNOS/PGE₂↓; companion MAPK(p38/JNK) re-partition, STAT3 phosphoryl↓; significant in LPS-stim RAW264.7/3T3-L1/chondrocyte/intestinal models, arthritis/IBD/periodontal/skin-redness background.

• Migraine prophylaxis (ESCOP/EMA traditional): not acute abortive substitute, assess ≥3 mo for frequency/severity drop (Meta ~24–32% drop, Cochrane mixed); mechanism = inhibit platelet 5-HT/serotonin release, suppress PGH₂/TXB₂-like vasoactive mediators, relax vascular spasm; ESCOP monograph "prevention of migraine headaches" traditional use.

• Anti-tumor & CSC-targeting (preclinical spine): multi-target — NF-κB↓ + p65 alkylate → anti-apopt Bcl-XL/c-IAP2↓, MMP-9/VEGF↓ anti-invasion; STAT3 dimer-block→prolif↓; HDAC1 degrade→p53 acetyl↑; ROS↑/GSH↓ oxidative; sustained JNK→apoptosis. Selective kill on primary CD34+ AML leukemia-stem, breast CD44+/CD24-, glioma, pancreatic, prostate (normal cells better tolerated), DMAPT water-soluble analog in preclinical; all cell-animal/early-clinical, no cross-border claim cures AML/breast-cancer.

• Neuroprotect & anti-platelet background: crosses BBB, microglial M1→M2 shift (NF-κB/STAT1-3/HDAC1 axis), cerebral I/R & spinal-cord-injury background; platelet 5-HT-release inhibit is migraine-mechanism extension but brings anticoag/pre-op stop warning.

• Anti-fibrosis (research): inhibits TGF-β1/Smad2/3 phosphoryl → collagen I/III deposit↓, pulmonary/hepatic/renal fibrosis cell-animal background.

Pharmacological Mechanism

Parthenolide pharmacology from "α-methylene-γ-lactone + 4,5-epoxide dual-electrophile → cysteine -SH covalent modification" single chemical root, multi-pathway embed:

1. NF-κB axis (spine): PTL covalently binds IKKβ Cys179 → IKK complex inactive → IκBα stable → p65 cytosol; PTL also directly alkylates RelA/p65 Cys38 (and Cys120) → DNA-binding↓ → TNF/IL-6/COX-2/MMP-9 transcription↓.

2. Epigenetic & STAT axis: proteasomal HDAC1 depletion → RelA/STAT1/STAT3 acetylation↑, STAT3 dimerization & nuclear translocation↓ → pro-apoptotic de-repressed.

3. Redox & stress axis: GSH consume, NADPH-oxidase ROS↑ → cancer-cell oxidative death (wide normal-cell window); sustained JNK activation cooperates TNF-α apoptosis.

4. Vascular & platelet axis: inhibit platelet 5-HT secretion, weakly TXA₂-like contractile mediators ↓ → migraine prophylaxis & mild vasomodulation.

Supplier note: Staherb labels "Parthenolide (CAS 20554-84-1, C₁₅H₂₀O₃) as sesquiterpene lactone from Tanacetum parthenium, α-methylene-γ-lactone+4,5-epoxide electrophilic warhead, covalent IKKβ(Cys179)/p65(Cys38)/HDAC1/STAT3 modifier, NF-κB tool-molecule"; no cross-border "treats acute-migraine/RA/AML/breast-cancer/Alzheimer" claim (drug scope), migraine-prophylaxis ESCOP/EMA traditional + mixed clinical + anti-inflam/anticancer cell-animal/preclinical background only; poorly water, heat/light/base-sensitive, epoxide electrophile H317 sensitization, monomer -20℃ dark N₂ DMSO stock, extract 2–8℃ N₂ dry, anticoag/warfarin/pre-op 1–2wk/pregnancy/lactation/Asteraceae-allergy redline on COA.

公司官网 http://www.staherb.com/ 资质:HALAL, KOSHER等认证

☎：19573130018 杨经理（微信同号）