长沙上禾生物staherb龙胆苦甙Gentiopicroside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：龙胆苦甙 / Gentiopicroside（C₁₆H₂₀O₉，CAS 20831-76-9，龙胆科龙胆属 Gentiana scabra/manshurica/triflora/rigescens/macrophylla 干燥根及根茎裂环烯醚萜苷，(5R-trans)-构型，UV 270 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：龙胆苦甙不是单一受体激动剂，而是"裂环烯醚萜苷内酯氧化还原调制 + 极苦激活口腔 TAS2R 迷走反射 + 肝胆转运蛋白上调 + NF-κB/MAPK/JAK-STAT 多靶抗炎 + Nrf2/ARE 抗氧化"五维嵌合。它本身含 C-1 内酯羰基与 C-6 葡萄糖苷，体内可部分代谢为苦龙胆酯甙/脱糖产物；Staherb 明载 极苦阈值≈1:20000 水、胆汁流量+30–50%、CCl₄/酒精/APAP 降 ALT/AST，占龙胆根苦甙 80%–90%、是《中国药典》龙胆≥3.0%/坚龙胆≥1.5% DW 的唯一定量标记。

Staherb 双页锚定功效：① 保肝利胆（王牌主轴）② 抗炎镇痛 ③ 苦味健胃与促消化 ④ 抗菌抗病毒（探索）⑤ 抗肿瘤与神经保护（细胞动物/临床前）。

核心功效（Core Efficacy）

• 保肝利胆（王牌主轴）：对 CCl₄、酒精、对乙酰氨基酚、D-半乳糖胺 诱导肝损伤，降血清 ALT/AST/ALP/GGT/TBIL，减肝细胞坏死与脂肪变性；利胆效应强于一线 UDCA 背景——通过激活 CAR/PXR → MRP3/MRP4↑，并上调肝细胞膜胆管侧 BSEP/MRP2 胆汁酸外排泵，增加胆汁流量 30%–50%，改善 ANIT 胆汁淤积；抗肝纤维化抑 TGF-β1/Smad 与 AngII-AT1R → 肝星状细胞活化↓；NAFLD 背景下调 TLR4/NF-κB、上调 AMPK/Nrf2，降 TC/TG/MDA、升 SOD/GSH-Px。

• 抗炎镇痛：抑 IKKβ→IκBα 磷酸化↓→NF-κB p65 核转阻断 → TNF-α/IL-6/IL-1β/COX-2/iNOS↓；调 JNK/p38 MAPK、JAK-STAT3、NLRP3 炎症小体；在角叉菜胶耳肿/棉球肉芽肿/UC 模型显著消肿；镇痛双路——外周抑 PGE₂、中枢下调前扣带回 GluN2B 与促 μ-阿片内源释放，无成瘾性。

• 苦味健胃与促消化：极苦激活舌背 TAS2R 苦味受体→迷走神经反射→唾液/胃液/胰液分泌↑、胃肠蠕动↑，传统"苦味健胃"已确证；伴轻度胃黏膜保护，辅助功能性消化不良/食欲不振/腹胀。

• 抗菌抗病毒（探索）：体外抑 金葡/大肠/幽门螺杆菌/白色念珠菌，破生物膜；抑 流感/RSV/HSV/HBV 复制背景，作感染辅助非主轴。

• 抗肿瘤与神经保护（临床前）：多靶——PI3K/Akt、Bax/Bcl-2、细胞周期阻滞+凋亡，对肝癌/胃癌/结肠/乳腺/肺癌细胞动物背景；易过血脑屏障，抑小胶质神经炎症、调 5-HT/GABA/BDNF，阿尔茨海默/帕金森/抑郁为细胞动物背景，不叫卖"治病"。

药理作用机制（Pharmacological Mechanism）

龙胆苦甙药理来自"内酯氧化还原调制 + TAS2R 苦味反射 + CAR/PXR→MRP/BSEP 利胆 + NF-κB/MAPK/JAK-STAT 抗炎 + TLR4/AMPK/Nrf2 保肝抗氧化"五维嵌合：

1. 肝胆轴：CAR/PXR 核受体激活 → MRP3/MRP4（基底侧）与 BSEP/MRP2（胆管侧）↑ → 胆汁酸外排↑；PPARα/γ 调脂、Nrf2→HO-1/SOD/GSH↑ 抗 ROS、TGF-β1/Smad 阻 HSC 活化。

2. 炎症轴：IKKβ 抑 → IκBα 不降解 → p65 滞留胞质；JNK/p38↓、STAT3↓、NLRP3 自噬降解 HMGB1 → TNF/IL-6/IL-1β/COX-2/iNOS↓。

3. 消化轴：口腔 TAS2R→迷走→胃壁 G 细胞/壁细胞反射性兴奋，胃液唾液↑、胃排空↑。

4. 肿瘤/神经轴：PI3K/Akt 调制、线粒体 Bax/Bcl-2 移位 caspase 级联；脑内小胶质 NF-κB/MAPK 抑 + BDNF↑。

⚠️ Staherb 合规边界：原料页统一表述"Gentiopicroside (CAS 20831-76-9, C₁₆H₂₀O₉) as secoiridoid glycoside from Gentiana spp. root, bitter principle & ChP marker, hepatobiliary/stomachic/anti-inflam traditional background; CAR/PXR→MRP3/4 BSEP/MRP2↑, NF-κB/MAPK/JAK-STAT↓, TAS2R reflex"；不跨境宣称治疗肝炎/胆囊炎/类风湿/阿尔茨海默/肿瘤（属药品范畴），保肝利胆/抗炎/苦味健胃为传统功效+细胞动物与观察性研究背景；水溶性好但吸湿光敏，2–8℃ 密封避光、单体 -20℃ 充氮，脾胃虚寒者慎用。

English Core Efficacy & Pharmacological Actions｜EN

Product: Gentiopicroside (syn. gentiopicrin, (5R-trans)-6-(β-D-glucopyranosyloxy)-5,6-dihydro-5-ethenyl-1H,3H-pyrano[3,4-c]pyran-1-one, secoiridoid glycoside from Gentianaceae Gentiana scabra/manshurica/triflora/rigescens/macrophylla dried root, CAS 20831-76-9, C₁₆H₂₀O₉)

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

Chemical basis: Gentiopicroside is not a single-receptor agonist but "secoiridoid lactone redox-modulatory + extreme-bitter TAS2R vagal reflex + hepatobiliary transporter upreg + NF-κB/MAPK/JAK-STAT multi-target anti-inflam + Nrf2/ARE antioxid" five-dimensional embed. C-1 lactone carbonyl + C-6 glucoside, partially metabolizes to amarogentin/aglycone; Staherb states bitter threshold ~1:20000 water, bile flow +30–50%, CCl₄/ethanol/APAP ↓ALT/AST, 80–90% of root bitter-glycosides, sole ChP marker (gentian ≥3.0% / rigid gentian ≥1.5% DW).

Staherb dual-page anchored efficacy: ① hepatobiliary protect (flagship) ② anti-inflammatory analgesic ③ bitter stomachic & digestion ④ antimicrobial/antiviral (explore) ⑤ anti-tumor & neuroprotect (preclinical).

Core Efficacy

• Hepatobiliary protect (flagship): vs CCl₄/ethanol/acetaminophen/D-galactosamine injury, lowers ALT/AST/ALP/GGT/TBIL, cuts necrosis/steatosis; choleretic effect stronger than UDCA background — activates CAR/PXR → MRP3/MRP4↑, upregulates canalicular BSEP/MRP2 bile-acid efflux pumps, bile flow +30–50%, improves ANIT cholestasis; anti-fibrosis inhibits TGF-β1/Smad & AngII-AT1R → HSC activation↓; NAFLD background downreg TLR4/NF-κB, upreg AMPK/Nrf2, ↓TC/TG/MDA, ↑SOD/GSH-Px.

• Anti-inflammatory analgesic: inhibits IKKβ→IκBα phosphoryl↓→NF-κB p65 nuclear block → TNF-α/IL-6/IL-1β/COX-2/iNOS↓; modulates JNK/p38 MAPK, JAK-STAT3, NLRP3 inflammasome; significant in carrageenan ear-edema/cotton-pellet granuloma/UC models; analgesia dual — peripheral PGE₂↓, central anterior-cingulate GluN2B↓ + μ-opioid endogenous release, non-addictive.

• Bitter stomachic & digestion: extreme bitter activates tongue TAS2R → vagal reflex → saliva/gastric/pancreatic secretion↑, gut motility↑, traditional "bitter stomachic" established; mild gastric mucosal protect, adjunct functional dyspepsia/anorexia/bloating.

• Antimicrobial/antiviral (explore): in vitro vs S. aureus/E. coli/H. pylori/C. albicans, biofilm disrupt; vs influenza/RSV/HSV/HBV replicate background, infection-adjunct not spine.

• Anti-tumor & neuroprotect (preclinical): multi-target — PI3K/Akt, Bax/Bcl-2, cell-cycle arrest+apoptosis in hepato/gastro/colon/breast/lung cell-animal; crosses BBB, microglial inflam↓, 5-HT/GABA/BDNF mod, Alzheimer/Parkinson/depression cell-animal only, never "treats".

Pharmacological Mechanism

Gentiopicroside pharmacology from "lactone redox-modulatory + TAS2R bitter reflex + CAR/PXR→MRP/BSEP choleresis + NF-κB/MAPK/JAK-STAT anti-inflam + TLR4/AMPK/Nrf2 hepatoprotect-antioxid" five-dimensional embed:

1. Hepatobiliary axis: CAR/PXR nuclear receptor activate → MRP3/MRP4 (basolateral) & BSEP/MRP2 (canalicular)↑ → bile-acid efflux↑; PPARα/γ lipid-mod, Nrf2→HO-1/SOD/GSH↑ anti-ROS, TGF-β1/Smad block HSC activate.

2. Inflammation axis: IKKβ inhibit → IκBα not degrade → p65 cytosol-retain; JNK/p38↓, STAT3↓, NLRP3 autophagic HMGB1 degrade → TNF/IL-6/IL-1β/COX-2/iNOS↓.

3. Digestion axis: oral TAS2R→vagus→gastric G/parietal cell reflex excitation, saliva/gastric-juice↑, gastric emptying↑.

4. Tumor/neural axis: PI3K/Akt modulate, mitochondrial Bax/Bcl-2 shift caspase cascade; brain microglial NF-κB/MAPK↓ + BDNF↑.

Supplier note: Staherb labels "Gentiopicroside (CAS 20831-76-9, C₁₆H₂₀O₉) as secoiridoid glycoside from Gentiana spp. root, bitter principle & ChP marker, hepatobiliary/stomachic/anti-inflam traditional background; CAR/PXR→MRP3/4 BSEP/MRP2↑, NF-κB/MAPK/JAK-STAT↓, TAS2R reflex"; no cross-border "treats hepatitis/cholecystitis/RA/Alzheimer/cancer" claim (drug scope), hepatobiliary/anti-inflam/bitter-stomachic traditional+fundamental-cell-animal background only; water-soluble but hygroscopic light-sensitive, 2–8℃ sealed dark, monomer -20℃ N₂, caution spleen-stomach deficiency-cold.

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

☎：19573130018 杨经理（微信同号）