Product name: Prosaikogenin G
Synonym name: Prosapogenin G；Prosaikosaponin G
Catalogue No.: BP2117
Cas No.: 99365-23-8
Formula: C36H58O8
Mol Weight: 618.852
Botanical Source: Bupleuri Radix
Type of Compound: Triterpenoids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
For Reference Standard and R&D, Not for Human Use Directly.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
128.8400
4.2399
4.2399
.0044
.8032
2.3913
Low
81.9742
6.8272
No
No
No
No
No
No
0.0
Yes
No
No
No
Prosaikogenin G (CAS No.: 99365-23-8) is a natural triterpene saponin compound isolated from the roots of the traditional Chinese medicine Bupleurum spp. As one of the important active components in Bupleurum, Bupleurum Saponin G is not only a metabolic derivative of Saikosaponin d in the gastrointestinal tract but also attracts attention for its remarkable biological activity. In recent years, with in-depth research into the pharmacological effects of natural products, Bupleurum Saponin G has demonstrated unique potential in anti-inflammation, antiviral, and renal protection, especially in inhibiting angiotensin II (Ang II)-induced mesomesangial cell proliferation in rats, indicating its value in the prevention and treatment of chronic kidney disease.
This review aims to systematically summarize the chemical structure and physicochemical properties of Bupleurum hyposaponin G, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics, and to explore its potential prospects for clinical application. By reviewing current research progress, the study provides theoretical basis and research directions for the drug development of Bupleurum Saponin G, promoting its clinical translation.
Bupleurum Saponin G belongs to the triterpene saponin class with a molecular weight of 618.8520. Its chemical structure is based on the pentacyclic triterpene skeleton, with multiple glycosyl residues attached. Its molecular structure exhibits typical saponin characteristics, namely a lipophilic triterpene core and hydrophilic sugar chains, giving it both hydrophobic and hydrophilic properties. The LogP value of Bupleurum hyposaponin G was 4.2399, indicating strong lipid solubility that facilitates penetration of cell membranes, but its water solubility is low (0.0044), limiting its solubility and bioavailability in the aqueous phase. Its topological pole surface area (TPSA) is 128.8400, suggesting the presence of multiple polar groups in its molecules, which may affect its membrane permeability and pharmacokinetic properties.
In terms of safety, Bupleurum hyposaponin G did not show hERG channel inhibitory activity, reducing potential cardiotoxicity risk; The Ames test result was 0.0, indicating no significant genotoxicity. Additionally, Bupleurum Saponin G has a relatively low blood-brain barrier penetration ability, suggesting its effect is mainly limited to peripheral tissues, reducing the risk of central nervous system side effects.
Bupleurum Saponin G mainly originates from the roots of Bupleurum. Bupleurum plants are widely distributed in East Asia and are commonly used in traditional Chinese medicine as a medicine for releasing the exterior and regulating liver qi. Bupleurum hyposaponin G, as a gastrointestinal metabolite of Saikosaponin d, has its content greatly influenced by plant variety, growing environment, harvest time, and processing technology.
The extraction of Bupleurum hyposaponin G is usually done using organic solvent extraction combined with column chromatography separation technology. Common steps include:
In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has improved the extraction efficiency and purity of Bupleurum Saponin G, while also offering greater environmental advantages.
The pharmacological effects of Bupleurum Saponin G cover multiple aspects including anti-inflammation, antiviral, anti-renal fibrosis, and cell proliferation regulation, with particularly outstanding performance in kidney protection and antiviral fields.
Bupleurum hyposaponin G significantly inhibited the proliferation of rat mesangial cells induced by Ang II. Ang II, as a key pro-fibrotic factor in renal pathology, promotes mesangial cell proliferation and extracellular matrix deposition, thereby aggravating glomerular injury. Bupleurum Saponin G intervenes in the cell cycle and signaling pathways, inhibits excessive proliferation of mesangial cells, slows the progression of renal fibrosis, and demonstrates good kidney protective potential.
Bupleurum saponin G exhibits certain inhibitory activity against influenza virus-related targets. Its targets include neuraminidase (NA), hemagglutinin (HA), M2 ion channel protein, as well as viral RNA polymerase subunits PB2 and PA. These targets play a key role in viral replication and infection. Bupleurum hyposaponin G, through its multi-target synergistic effect, blocks viral invasion and replication, offering potential anti-influenza effects.
In addition to the main activities mentioned above, Bupleurum hyposaponin G also exhibits anti-inflammatory, immunomodulatory, and antioxidant effects. By regulating inflammatory factor expression and signaling pathways, it reduces tissue inflammatory responses and promotes tissue repair. In addition, Bupleurum Saponin G has also been preliminarily reported to have protective effects on the liver and gastrointestinal tract, indicating its broad pharmacological effects.
The mechanism of action of Bupleurum Saponin G involves multiple signaling pathways and molecular targets, reflecting its multi-target and multi-pathway pharmacological characteristics.
Bupleurum hyposaponin G blocks cell proliferation signals induced by Ang II by regulating cell cycle-related proteins (such as Cyclin D1, CDK4/6) and apoptosis-related factors. It may inhibit the MAPK/ERK and PI3K/Akt signaling pathways, reduce cell proliferation and fibrotic reactions, and protect glomerular structure and function.
For influenza viruses, Bupleurum saponin G binds to and inhibits NA and HA proteins, blocking viral release and cellular invasion. At the same time, it inhibits the function of M2 ion channels, disrupts the acidification process within the virus, and affects viral replication. Additionally, Bupleurum saponin G inhibits viral RNA polymerase subunits PB2 and PA, further blocking viral gene expression and replication, forming a multi-layer antiviral barrier.
Bupleurum hyposaponin G can inhibit activation of the NF-κB signaling pathway, reduce the release of pro-inflammatory cytokines (such as TNF-α, IL-6), and alleviate inflammatory responses. It may also regulate the functions of T cells and macrophages, enhancing the body's immune regulatory capacity.
The druggability parameters of Bupleurum Saponin G show certain advantages and challenges.
Bupleurum hyposaponin G has a relatively large molecular weight (618.8520) and low water solubility (0.0044), which poses certain obstacles to its oral absorption and bioavailability. The LogP value was 4.2399, indicating good lipid solubility and facilitating cell membrane penetration, but the highly polar TPSA value (128.8400) may limit its passive diffusion. Its blood-brain barrier penetration ability is relatively low, suggesting it mainly acts on peripheral targets to reduce the risk of central nervous system toxicity.
Bupleurum saponin G did not show hERG channel inhibition, reducing the risk of arrhythmias. The Ames test was negative, indicating no significant genotoxicity and relatively good safety. Current in vitro and animal experiments have not shown significant toxic side effects, but further systematic toxicological evaluation is needed.
Currently, pharmacokinetic research on Bupleurum Saponin G is relatively limited. As a metabolite of saikosaponin d, its stability and conversion rate in the gastrointestinal tract affect its concentration and duration of action in the body. In the future, studies on in vivo and in vitro metabolic kinetics are needed to clarify its absorption, distribution, metabolism, and excretion (ADME) characteristics, providing a basis for dosage formulation design and administration protocol optimization.
Bupleurum Saponin G, with its multi-target and multifunctional pharmacological activity, demonstrates broad clinical application potential.
The inhibitory effect of Bupleurum hyposaponin G on Ang II-induced mesangial cell proliferation provides new ideas for the prevention and treatment of chronic kidney diseases, especially glomerulosclerosis and renal fibrosis. Combining its anti-inflammatory and antioxidant effects, it is expected to become a natural candidate for kidney protection.
The multi-target inhibitory mechanism targeting influenza viruses gives Bupleurum Saponin G the potential for development as an anti-influenza drug. Especially against the backdrop of increasing viral resistance, natural products offer new drug structures and modes of action.
The immunomodulatory and anti-inflammatory effects of Bupleurum Saponin G suggest its application prospects in autoimmune diseases, inflammatory diseases, and liver protection. In the future, integrating modern drug delivery technologies (such as nanocarriers and liposomes) to optimize bioavailability will further expand its clinical value.
The low water solubility and oral bioavailability of Bupleurum Saponin G are the main bottlenecks for its clinical transformation. Systematic pharmacokinetic and toxicological studies are needed to clarify the safe dosage range and metabolic pathways in vivo. At the same time, it deeply analyzes its molecular mechanisms of action and target network, combining structural modification and dosage form innovation to enhance its efficacy and safety. The implementation of multicenter clinical trials will be key to verifying their clinical efficacy and safety.
Bupleurum hyposaponin G, as an important natural triterpene saponin derivative of Bupleurum, has become a hot topic in pharmacological research of natural products due to its unique chemical structure and significant pharmacological activity, especially its potential in kidney protection and antiviral fields. Its multi-target and multi-pathway mechanisms provide valuable scientific evidence for the development of novel natural drugs. In the future, by optimizing extraction and purification processes, improving drug formulations, and conducting in-depth pharmacokinetics and toxicology research, Bupleurum Saponin G is expected to become an important candidate drug for clinical treatment of chronic kidney disease and viral infections. Ongoing basic and clinical research will drive the drug development progress of Bupleurum hyposaponin G, promoting its application and promotion in modern medicine.
