Synonym name: Tenacissimoside C
Catalogue No.: BP1372
Cas No.: 191729-45-0
Formula: C42H66O14
Mol Weight: 794.976
Botanical Source: Marsdenia tenacissima
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Tenacissoside H is a natural product isolated from the traditional Chinese medicine Marsdenia tenacissima, and belongs to the class of saponins found in this plant. As a traditional Chinese medicinal herb, Tongguan Vine has always been widely used in the adjuvant treatment of anti-tumor and anti-inflammatory diseases. In recent years, with the deepening development of natural product pharmacology, Tongguan Tengzhi H has become a research hotspot due to its significant anti-tumor and anti fibrotic activities. This compound not only exhibits good biological activity, but also has excellent safety and potential as a drug, demonstrating its application prospects in the treatment of anti-tumor and anti fibrotic diseases.
This article will provide a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation and pharmacokinetic characteristics of Tongguan Vine Glycoside H. Finally, it will explore its potential clinical applications and future research directions, aiming to provide comprehensive and authoritative reference materials for researchers in related fields.
The molecular formula of Tongguan Vine Glycoside H is C42H66O15, with a molecular weight of 794.9760. Its structure belongs to the macrocyclic saponin class, with a typical steroid saponin skeleton that connects multiple sugar residues. The LogP value of this compound is 3.3084, indicating that it has moderate lipid solubility, which is beneficial for cell membrane penetration. The polar surface area (TPSA) is 178.04 Å ², indicating that the molecule has strong polar groups that may affect its absorption and distribution characteristics.
The low water solubility (0.0162 mg/mL) to some extent limits its oral bioavailability, but also provides room for improvement in formulation design. Guanguan Tengzhi H does not have hERG channel inhibitory activity, indicating a low risk of cardiac toxicity. The Ames test result is 0.0, indicating no significant mutagenicity and high safety. The low penetration ability of the blood-brain barrier may limit its direct effects on central nervous system diseases, but also reduce the risk of central nervous system side effects.
In the chemical structure of Tongguan Tengzhi H, the binding of the steroid core to the sugar group endows it with the potential for multi-target regulation, making it suitable for the treatment of complex diseases such as tumors and fibrosis.
Guanguan Vine Glycoside H mainly comes from Marsdenia tenacissima, a perennial climbing herbaceous plant widely distributed in southern China and Southeast Asia. Tongguan Vine is used in traditional Chinese medicine as a medicinal herb for detoxification, reducing swelling, promoting blood circulation, removing blood stasis, and anti-tumor effects.
The process of extracting Guanguan Vine Glycoside H usually includes the following steps:
In recent years, the introduction of ultrasound assisted extraction and microwave-assisted extraction technologies has significantly improved extraction efficiency and purity, providing technical support for large-scale preparation.
Guanguan Vine Glycoside H, as an important component of Guanguan Vine Saponins, exhibits significant anti-tumor activity. In vitro cell experiments showed that Tongguanoside H could inhibit the proliferation of many tumor cell lines, including lung cancer, liver cancer, gastric cancer and breast cancer cells. Its mechanism of action involves inducing cell apoptosis, blocking the cell cycle, and inhibiting tumor cell migration and invasion.
In vivo experiments, Tongguan Tengzhi H significantly inhibited tumor growth in mouse tumor models with minimal toxic side effects and demonstrated good therapeutic efficacy. In addition, Tongguan Tengzhi H can enhance the efficacy of chemotherapy drugs, reduce chemotherapy related toxic side effects, and has potential adjuvant therapeutic value.
Fibrosis is a pathological process regulated by multiple cytokines and signaling pathways, leading to the destruction of tissue structure and function. The research on the anti fibrotic effects of Tongguan Tengzhi H is gradually increasing, mainly focusing on disease models such as pulmonary fibrosis, liver fibrosis, and myocardial fibrosis.
Research has shown that Tongguan Vine Glycoside H can significantly downregulate the expression of fibrosis related genes, including matrix metalloproteinase MMP2, transforming growth factor beta 1 (TGFB1), alpha smooth muscle actin (ACTA2), type I collagen protein (COL1A1), and tissue inhibitory factor TIMP1, thereby inhibiting fibroblast activation and collagen deposition, and reducing fibrosis progression.
The multi-target mechanism of action of Tongguan Tengzhi H is an important basis for its pharmacological activity. Its main targets and mechanisms include:
MMP2 (Matrix Metalloproteinase 2)
MMP2 plays a crucial role in extracellular matrix degradation and tissue remodeling. Guanguan Vine Glycoside H promotes the remodeling and balance of fibrous tissue by regulating the expression and activity of MMP2, preventing excessive fibrosis.
TGFB1 (Transforming Growth Factor β 1)
TGFB1 is a core regulatory factor in the fibrosis signaling pathway, promoting fibroblast proliferation and collagen synthesis. Guanguan Tengzhi H can inhibit the signaling of TGFB1, block the initiation and progression of fibrosis.
ACTA2 (alpha smooth muscle actin)
ACTA2 is a biomarker for activated fibroblasts, involved in cytoskeleton remodeling and contractile function. Guanguan Tengzhi H reduces the expression of ACTA2, inhibits the activation of fibroblasts, and slows down the formation of fibrous tissue.
COL1A1 (type I collagen)
COL1A1 is the main type of collagen protein in fibrotic tissues, and overexpression leads to tissue sclerosis. Guanguan Tengzhi H inhibits the synthesis of COL1A1 and reduces collagen deposition.
TIMP1 (tissue inhibitor of matrix metalloproteinase 1)
TIMP1 regulates the activity of MMPs and maintains the balance of matrix metabolism. Guanguan Tengzhi H regulates the expression of TIMP1, promoting the dynamic balance between matrix degradation and synthesis.
In addition, Tongguan Tengzhi H may exert comprehensive anti-tumor and anti fibrotic effects by regulating apoptosis related proteins (such as the Bcl-2 family), inflammatory factors (such as the NF - κ B signaling pathway), and oxidative stress response.
The pharmacological evaluation of Guanguan Tengzhi H shows that it has certain development potential:
In terms of pharmacokinetics, existing research is relatively limited. Preliminary in vivo experiments have shown that the absorption of Tongguan Tengzhi H is slow after oral administration, with a moderate plasma half-life. It is mainly metabolized through the liver and excreted through bile and urine. In the future, further systematic research is needed on its absorption, distribution, metabolism, and excretion (ADME) characteristics to guide clinical dosing regimen design.
As a natural product, Tongguan Vine Glycoside H has shown broad clinical application prospects due to its multi-target and multi mechanism anti-tumor and anti fibrotic activities. Its potential in adjuvant therapy for tumors is particularly prominent, as it can enhance the efficacy of existing chemotherapy regimens, reduce side effects, and improve patients' quality of life.
In the field of anti fibrosis, Tongguan Tengzhi H provides a new treatment approach for difficult to treat diseases such as pulmonary fibrosis and liver fibrosis. By regulating key fibrotic targets, Guantongteng H is expected to become an important candidate molecule for the development of anti fibrotic drugs.
Future research directions should focus on:
In addition, by combining modern drug design techniques such as structural modification and nanocarrier delivery, it is expected to further enhance the efficacy and drug properties of Guantongteng H.
Guanguan Vine Glycoside H, as an important active ingredient in Guanguan Vine, has become a research hotspot in the field of natural product pharmacology due to its unique chemical structure and multi-target pharmacological activity. Its potential application in anti-tumor and anti fibrotic diseases reflects the important value of natural products in modern drug development. Although the research on its pharmacokinetics and clinical application is still in the preliminary stage, with the deepening of research and technological progress, Tongguan Tengzhi H is expected to become a new generation of safe and effective therapeutic drugs, bringing new hope for the treatment of related diseases. In the future, interdisciplinary cooperation should be strengthened to promote the transition of Guantongteng H from laboratory to clinical practice and realize its clinical translational value.
