长沙上禾生物 Staherb千金藤素 Cepharanthin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｜Core Efficacy & Pharmacological Actions (CN)

千金藤素（Cepharanthine）是防己科千金藤属来源的双苄基异喹啉类生物碱（BBIA），亲脂性阳离子，可插入细胞膜。药理呈“膜效应+胞内多靶点”叠加，核心可归纳为五大块：

1. 升白细胞（日本 PMDA 经典获批功效）

盐酸千金藤素片（Cepharanthin®）自 1951 年起在日本用于放化疗、苯中毒、药物性白细胞减少症/粒细胞缺乏辅助。机制：活化网状内皮系统、刺激骨髓造血组织增生、促进中性粒细胞释放、上调 G-CSF 表达。

2. 广谱抗病毒（近年核心热点）

• 新冠：体外抗 SARS-CoV-2 IC₅₀≈1.90 μM，IC₉₀≈4.46 μM；阻断 S 蛋白/ACE2 膜融合、抑制 Nsp13 解旋酶、干预 ER 应激/HSF1 热休克反应；

  
  

• 流感：抑制病毒聚合酶活性，下调 JAK/STAT/NF-κB 介导的炎症因子风暴；

  
  

• 其他：对 HIV-1、登革、埃博拉、OC43 冠状病毒等有抑制报道。

  
  

3. 抗炎与免疫调节

抑制 NF-κB 核转位、激活 AMPK、降低 TNF-α/IL-6/IL-1β；对巨噬细胞、T 细胞呈双向免疫调节，用于脓毒症、慢性免疫性血小板减少等探索。

4. 抗肿瘤与逆转多药耐药（MDR）

诱导肿瘤细胞凋亡、阻周期（p21/p27 上调）、抑 EMT 与侵袭；关键特色是逆转 MDR——抑制 ABCB1/P-gp、ABCC10(MRP7) 外排泵，增加细胞内化疗药蓄积，与阿霉素联用增效（EAC/ADR 模型体外逆转倍数 13×，体内生命延长率 75.37%），并提高放射敏感性。

5. 抗纤维化 / 抗氧化 / 其他

抑制 TGF-β1/Smad 通路，减少肺、肝、肾纤维化基质沉积；清除自由基、稳定细胞膜，用于皮肤光老化、过敏性皮炎、口腔炎背景研究；另有抗疟、抑制血小板聚集、治蛇咬等旧适应症。

作用特点：亲脂性阳离子插入细胞膜 → 同时产生“膜效应”（刚性化、阻融合、抑外排）与“胞内效应”（NF-κB / AMPK / STAT3 / TGF-β 等通路调节）。

English｜Core Efficacy & Pharmacological Actions (EN)

Cepharanthine (Cepharanthin®) is a natural bisbenzylisoquinoline alkaloid (BBIA) from Stephania cephalanthaHayata. Its lipophilic cationic structure inserts into plasma membranes → concurrent “membrane effects” (rigidification, fusion block, efflux inhibition) and “intracellular effects” (NF-κB / AMPK / STAT3 / TGF-β axis modulation). Pharmacology reads as five pillars:

1. Leukocytosis (classic PMDA-approved action)

Cepharanthine HCl tablets have been used in Japan since 1951 as an adjuvant for leukopenia / agranulocytosis from radio-chemotherapy, benzene or drugs. Mechanism: activates reticuloendothelial system, stimulates bone-marrow hematopoietic tissue proliferation, promotes neutrophil release, up-regulates G-CSF.

2. Broad-spectrum antiviral (major recent focus)

• SARS-CoV-2: IC₅₀ ≈ 1.90 μM, IC₉₀ ≈ 4.46 μM; blocks Spike/ACE2 membrane fusion, inhibits Nsp13 helicase, reverses ER-stress/HSF1-mediated viral hijacking;

  
  

• Influenza A: impairs viral polymerase activity, dampens JAK/STAT/NF-κB-driven cytokine storm;

  
  

• Also reported active against HIV-1, dengue, Ebola, HCoV-OC43, etc.

  
  

3. Anti-inflammatory & immunomodulation

Inhibits NF-κB nuclear translocation, activates AMPK, lowers TNF-α/IL-6/IL-1β; bidirectionally modulates macrophages and T-cells—explored in sepsis, chronic immune thrombocytopenia.

4. Antitumor & MDR reversal

Induces apoptosis, arrests cell cycle (p21/p27↑), suppresses EMT/invasion. Distinctive value: reverses multidrug resistance by inhibiting ABCB1/P-gp and ABCC10/MRP7 efflux pumps, increasing intracellular chemo-drug accumulation; with doxorubicin in EAC/ADR model 13-fold in-vitro reversal and 75.37% in-vivo life-extension, plus radio-sensitization.

5. Anti-fibrotic / antioxidant / misc.

Suppresses TGF-β1/Smad signaling to reduce lung/liver/renal fibrosis; scavenges free radicals, stabilizes membranes (skin photoaging, allergic dermatitis, oral mucositis research); legacy uses include antimalarial, antiplatelet, snakebite.

Mechanistic hallmark: a lipophilic cation that inserts into plasma membranes → “membrane effect” (fusion block, efflux pump inhibition) + “intracellular effect” (NF-κB / AMPK / STAT3 / TGF-β modulation) at once.

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

☎：19573130018 杨经理（微信同号）