Camptothecin: Nature’s Potent Topoisomerase Inhibitor for Oncology & Analysis | Supplier & Manufacturer
1. What is Camptothecin?
Camptothecin (CPT) is a pentacyclic quinoline alkaloid initially remoted from the bark/stems of the Chinese language Comfortable Tree (Camptotheca acuminata). It features as a potent topoisomerase I (Topo I) inhibitor, binding to the Topo I-DNA advanced and stopping DNA religation throughout replication. This triggers replication fork collapse, double-strand DNA breaks, 그리고 S-phase selective apoptosis in quickly dividing cells. Its distinctive mechanism underpins its significance in oncology therapeutics 그리고 most cancers biology analysis.
2. 공급, 화학적 특성 및 식별자
-
공급: 주로 다음에서 추출됨 Camptotheca acuminata bark/seeds. Semi-synthesis from plant precursors is widespread.
-
화학적 특성:
-
화학명: (S)-4-Ethyl-4-hydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
-
분자 구성 요소: C₂₀H₁₆N₂O₄
-
분자량: 348.36 g/mol
-
모습: Pale yellow to gentle inexperienced crystalline powder
-
용해도: Lactone ring pH-dependence – Soluble in DMSO, DMF, chloroform (closed lactone kind, energetic); hydrolyzes to inactive carboxylate kind in aqueous pH >7.
-
안정: Mild and pH-sensitive. Requires strict management of lactone ring integrity for bioactivity.
-
-
주요 식별자:
-
CAS: 7689-03-4
-
EC 수량(EINECS): 231-684-4
-
MF: C₂₀H₁₆N₂O₄
-
MW: 348.36
-
3. Purity, Efficacy, Security & Dosage
-
최적의 제품: The “finest” camptothecin options >99% HPLC purity, >95% lactone kind content material (important for exercise), and undetectable contaminants. Shaanxi Zhonghong achieves this by way of proprietary pH-controlled crystallization 그리고 동결건조.
-
Well being Benefits & Functions:
-
Anticancer Exercise: Core mechanism: Topo I inhibition → DNA harm → S-phase apoptosis. Foundation for FDA-approved derivatives (Irinotecan, Topotecan) treating colorectal, ovarian, SCLC, cervical cancers.
-
Antiviral/Antiparasitic Analysis: Rising exercise towards HIV-1, HSV, Leishmania in preclinical fashions.
-
(Be aware: Nattokinase primarily exhibits anticoagulant/thrombolytic results; direct kidney advantages are much less established vs. potential CPT nephrotoxicity issues).
-
-
Dosage & Administration:
-
NOT a dietary complement. Used clinically as IV derivatives below strict medical supervision.
-
Analysis doses differ (usually 0.1-100 µM 시험관 내에서; mg/kg ranges 생체 내). No secure each day consumption for self-administration exists.
-
-
Important Precautions & Aspect Results:
-
Extreme Toxicity: Myelosuppression (neutropenia, thrombocytopenia), extreme diarrhea (cholinergic & delayed), hemorrhagic cystitis, hepatotoxicity.
-
Lactone Instability: Speedy hydrolysis to inactive carboxylate at physiological pH reduces efficacy.
-
금기사항: Being pregnant/lactation (teratogenic), pre-existing bone marrow melancholy, energetic infections.
-
다음을 처리합니다. Cytotoxic – Requires PPE (gloves, masks, lab coat). Keep away from inhalation/pores and skin contact.
-
4. Shaanxi Zhonghong: Your Premier Camptothecin Supply
Shaanxi Zhonghong Investment Technology Co., Ltd. is a cGMP/ISO-certified chief in high-purity plant-derived APIs. With 28+ years in bioactive phytochemistry, we focus on:
-
핵심 역량:
-
과학적 우수성: 5개 대학 공동 연구실, 20개 이상의 특허 (incl. CPT stabilization tech), Unique Natural Compound Library.
-
Slicing-Edge Analytics: HPLC-PDA/ELSD (purity), UPLC-QTOF-MS (impurity profiling), Superconducting FT-NMR (construction ID), ICP-MS (중금속) GC-MS/MS (residual solvents). Purity >99%, exceeding USP by 20%.
-
국제적 성취: 제공합니다 80개 이상의 국가 – Pharma, Biotech, Tutorial Analysis.
-
수직적 통합: 지속 가능한 소싱 → GMP Extraction → pH-Managed Purification → 동결건조.
-
5. 엄격한 제품 사양
오염 물질 종류 | 매개변수 | 사양 제한 | 기술을 살펴보세요 |
---|---|---|---|
살충제 | 클로르피리포스 | ≤ 0.01mg/kg | GC-MS/MS |
시페르메트린 | ≤ 0.05mg/kg | GC-ECD | |
완전히 다른 살충제 | ≤ 0.1 mg/kg (매) | EU 2021/601 | |
중금속 | 납 | ≤ 1.0mg/kg | ICP-MS(USP <232>) |
처럼 | ≤ 0.5mg/kg | ICP-MS(USP <232>) | |
CD | ≤ 0.5mg/kg | ICP-MS(USP <232>) | |
Hg | ≤ 0.1mg/kg | CVAAS (USP <232>) | |
미생물학 | TAMC | ≤ 10³ CFU/g | USP <61> |
TYMC | ≤ 10² CFU/g | USP <61> | |
대장균 | 10g에는 없음 | USP <62> | |
살모넬라균 종 | Absent in 375g | USP <62> | |
Important High quality | Camptothecin Purity | ≥ 99.0% (HPLC) | HPLC-PDA(USP <621>) |
Lactone Kind | ≥ 95.0% | pH-Particular HPLC | |
수분 함량 | ≤ 2.0% | Karl Fischer (USP <921>) | |
잔류 용매 | Class 1/2 Solvents: Undetected | GC-FID(ICH Q3C) |
6. 우수한 제조 워크플로
-
지속 가능한 수확: Camptotheca acuminata cultivated below GACP tips.
-
선택적 추출: Ethanol/Water 또는 초임계 CO₂ extraction of bark/seeds.
-
주요 정화: 액체-액체 분배 (CH₂Cl₂/H₂O), adsorbent chromatography (SiO₂, polyamide).
-
Lactone Stabilization: pH-controlled crystallization (pH 3.5-4.5) to maximise lactone yield.
-
Last Purification: 분취용 HPLC (C18 column, MeOH/H₂O/TFA cell section).
-
건조: 동결건조 (-50°C, <10 Pa) to protect lactone ring & stability.
-
QC 출시: 가득한 코에이 verifying identification, purity, lactone content material, contaminants.
7. Key Application Areas
-
Oncology Medicine: Precursor for Irinotecan (CPT-11), Topotecan, Belotecan.
-
Most cancers Analysis: Software compound for DNA harm response, 세포사멸, drug resistance research.
-
Drug Supply Techniques: Loaded into liposomes, nanoparticles, polymer conjugates to boost solubility/concentrating on.
-
Antiviral/Antiparasitic Improvement: Investigational agent for novel therapeutics.
8. cGMP 고품질 관리 프로토콜
산시성 중홍(Shaanxi Zhonghong)은 다음과 같은 직원을 고용합니다. tiered QC technique:
-
신분증: FT-NMR (¹H/¹³C), HPLC-UV/PDA spectral match vs. USP reference customary.
-
Assay & Impurities: HPLC-ELSD/PDA quantifies CPT (≥99.0%) and detects ≤0.1% associated compounds (10-deacetylcamptothecin, camptothecin carboxylate).
-
Lactone Content: Validated pH-specific RP-HPLC methodology distinguishes lactone/carboxylate types.
-
Contaminants: ICP-MS for heavy metals (USP <232>), GC-MS/MS for 500+ pesticides (EU 2021/601), LC-MS/MS for mycotoxins, USP <61>/<62> for microbiology.
-
안정: Actual-time & accelerated ICH Q1A(R2) research verify 24-month shelf-life at -20°C (desiccated, argon ambiance).
9. Safe Packaging & Logistics
-
메이저 팩: Amber glass vials sealed below argon, full of desiccant.
-
보조 팩: Vacuum-sealed aluminum luggage 내부에 UN-certified HDPE containers.
-
저장: -20°C ± 5°C; defend from gentle/moisture.
-
배달: International cold-chain logistics (-15°C to -25°C) by way of DHL FedEx UltraCold.
10. Mechanisms, Functions & Challenges
-
기구: Traps Topo I-DNA cleavable complexes → Collision with replication forks → DSBs → ATR/Chk1 activation → p53-mediated apoptosis.
-
Innovation: 중홍의 PEGylated liposomal CPT (Patent: CN202210XXXXXX) enhances tumor concentrating on.
-
분석 프런티어:
-
Novel Analogues: 7-Silylcamptothecins (improved lactone stability).
-
Mixture Therapies: With PARP inhibitors, immunotherapy.
-
Biomarkers: Predictive biomarkers for CPT sensitivity (ERCC1, Topo I ranges).
-
-
과제: Lactone instability, myelosuppression, ABCG2-mediated drug resistance, tumor heterogeneity.
11. Steadily Requested Questions (FAQ)
-
Q1: Can I take Camptothecin as a complement?
-
A: Completely NOT. CPT is a potent cytotoxic compound with extreme unintended effects. Use solely below medical supervision in FDA-approved by-product types (e.g., Irinotecan) or for managed analysis.
-
-
Q2: Why is lactone kind important?
-
에이: Solely the closed lactone ring binds Topo I. The open carboxylate kind is inactive and will trigger renal toxicity. Zhonghong ensures ≥95% lactone content material by way of lyophilization.
-
-
Q3: How does Camptothecin differ from Nattokinase for kidneys?
-
에이: CPT carries nephrotoxicity dangers (tubular harm). Nattokinase, a fibrinolytic enzyme, lacks strong proof for direct kidney advantages. Neither is nephroprotective.
-
-
This autumn: What analytical strategies verify Zhonghong’s CPT purity?
-
에이: HPLC-PDA/ELSD (purity), UPLC-QTOF-MS (impurities), FT-NMR (construction), pH-HPLC (lactone quantification), ICP-MS (heavy metals).
-
-
Q5: Do you supply Camptothecin derivatives?
-
에이: Sure. GMP-grade 10-Hydroxycamptothecin, SN-38 (Irinotecan metabolite), customized synthesis obtainable.
-
12. The place to Purchase?
Supply research-grade & GMP Camptothecin:
-
이메일: liaodaohai@gmail.com
-
인터넷: www.aiherba.com
-
요구: COA, MSDS, customized synthesis quotes.
13. 결론
Camptothecin stays a cornerstone of topoisomerase-targeted oncology. Its medical impression by way of semisynthetic derivatives underscores its irreplaceable function. Success hinges on securing ultra-pure, lactone-stabilized materials with verifiable traceability. Shaanxi Zhonghong delivers >99% HPLC purity CPT ~을 통해 특허받은 안정화 전문성, cGMP 준수, 그리고 unmatched analytical rigor – empowering drug discovery and superior therapeutics.
14. 참고문헌
-
Wall ME, et al. (1966). J Am Chem Soc. 88:3888–3890. [DOI:10.1021/ja00968a057]
-
Hsiang YH, et al. (1985). J Biol Chem. 260:14873–14878. [PMID:2997227]
-
Pommier Y. (2006). Nat Rev Most cancers. 6:789–802. [DOI:10.1038/nrc1977]
-
USP-NF Monograph: Camptothecin. USP44-NF39.
-
ICH Q3C (R8): Residual Solvents. (2021).
-
FDA Steerage: Irinotecan Label. (2023).
-
Thomas CJ, et al. (2004). J Med Chem. 47:3972–3981. [DOI:10.1021/jm030660+]
-
Du W, et al. (2022). Acta Pharm Sin B. 12:3006–3025. [DOI:10.1016/j.apsb.2022.03.011]
-
GLS-010-IPHASE Research Protocol (NCT04501563).
-
EMA Evaluation Report: Topotecan (2020). EMA/CHMP/89262/2020.
리뷰
아직 리뷰가 없습니다.