Product name: Prosaikogenin F
Synonym name: Prosapogenin F；Prosaikosaponin F
Catalogue No.: BP2118
Cas No.: 99365-20-5
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.

HPLC of Prosaikogenin F

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Prosaikogenin F, an important monosaccharide natural product of Bupleurum spp., has attracted widespread attention in recent years due to its diverse biological activity. As a traditional Chinese medicinal herb, Bupleurum has long been used to soothe the liver, relieve depression, and harmonize the nutritive and defensive qi. Modern pharmacological research has found that its main active ingredients include various saponins, among which Bupleurum hyposaponin F shows remarkable anti-cancer and hemolytic properties. In addition, the therapeutic potential of Bupleurum Saponin F in neuropsychiatric disorders, especially depression, is gradually being revealed, with related targets covering neurotransmitter metabolizing enzymes, receptors, and signal transduction molecules. This paper aims to systematically review the chemical structure, origin, pharmacological activity, mechanism of action, and druggability evaluation of Bupleurum Saponin F, exploring its clinical application prospects as a candidate molecule for novel natural medicines.

Chemical structure and physicochemical properties

Bupleurum hyposaponin F has the molecular formula C_33H_54O_11 and molecular weight 618.8520, belonging to the triterpene saponin compound. Its structural feature is that it uses a pentacyclic triterpene as the parent nucleus, connecting monosaccharide residues to form monosaccharide saponins. In terms of physicochemical properties, Bupleurum hyposaponin F has a LogP value of 4.2377, indicating strong hydrophobicity and extremely low water solubility (0.0044 mg/mL), which poses challenges for bioavailability and drug delivery. The topological pole surface area (TPSA) is 128.8400, indicating high polarity, which may limit its ability to penetrate cell membranes and the blood-brain barrier. In terms of drug safety, Bupleurum saponin F showed no hERG channel inhibitory activity, and Ames-induced mutagenic test results were zero, indicating a low genotoxicity risk.

Plant Origins and Extraction Methods

Bupleurum saponin F is mainly found in Bupleurum species, especially the roots of Bupleurum chinense DC. and Bupleurum scorzonerifolium Willd. In traditional Chinese medicine processing, Bupleurum root is widely used, and its saponins are obtained by decoction or alcohol extraction.

Modern extraction techniques mostly use alcohol-water mixed solvents (such as 70% ethanol) for extraction and extraction, followed by liquid-liquid separation, column chromatography (such as silica gel columns, C18 reversed-phase columns), and high-performance liquid chromatography (HPLC) for separation and purification. The application of ultrasound-assisted extraction and microwave-assisted extraction technologies improves extraction efficiency and purity. The purified Bupleurum hyposaponin F is structurally identified using mass spectrometry (MS) and nuclear magnetic resonance (NMR) techniques to ensure its purity and structural accuracy.

Pharmacological activity research

Anticancer activity

Bupleurum saponin F exhibits significant cytotoxicity and tumor growth inhibition in various cancer cell lines. In vitro experiments have shown that it can induce cancer cell apoptosis and inhibit cell proliferation and migration. The mechanism involves regulating cell cycle-related proteins, activating mitochondrial-dependent apoptotic pathways, and inhibiting the NF-κB signaling pathway. Some studies have indicated that Bupleurum hyposaponin F promotes cancer cell apoptosis by upregulating the expression of p53 and Bax proteins, while downregulating the anti-apoptotic protein Bcl-2, enhancing the sensitivity of chemotherapy drugs.

Hemolytic properties

Bupleurum saponin F has certain hemolytic activity, which can affect the stability of red blood cell membranes and promote rupture. This characteristic may have the potential to modulate hemorheology in certain pathological conditions, but it also suggests that dose-dependent safety issues should be considered in clinical applications. The hemolytic mechanism may be related to the surface activity of saponins and the interaction between membrane lipids.

Antidepressant potential

Research on Bupleurum Saponin F has been gradually deepening in the field of neuropsychiatric diseases, especially showing great potential in its antidepressant effects. Its targets include key molecules such as monoamine oxidase A (MAOA), monoamine oxidase B (MAOB), glycogen synthase kinase 3β (GSK3B), serotonin transporter (SLC6A4), 5-hydroxytryptamine 1A receptor (HTR1A), γ-aminobutyric acid receptor subunit 1 (GABRA1), cAMP reactive factor-binding protein 1 (CREB1), brain-derived neurotrophic factor (BDNF), and catechol-O-methyltransferase (COMT), among others. Bupleurum Saponin F improves neurotransmitter metabolism by modulating these targets, promoting neuroplasticity, and thus exerting antidepressant effects.

Mechanism of action and molecular targets

The multi-target mechanism of Bupleurum Saponin F reflects its complex pharmacological properties. Its anticancer effects mainly work by regulating apoptosis-related signaling pathways, including p53, NF-κB, and mitochondrial pathways, promoting programmed death of cancer cells. Its hemolytic action interacts with the surface activity of saponin molecules and membrane lipids, leading to rupture of the red blood cell membrane.

In terms of antidepressant mechanisms, Bupleurum hyposaponin F reduces the degradation of neurotransmitters (such as serotonin, norepinephrine, dopamine) by inhibiting MAOA and MAOB activity, thereby increasing the effective concentration of neurotransmitters. Its inhibitory effect on GSK3B helps regulate neuronal signaling and cell survival. By activating the HTR1A receptor and modulating the SLC6A4 transporter, Bupleurum saponin F improves neurotransmitter balance. Additionally, Bupleurum Saponin F promotes the expression of CREB1 and BDNF, enhancing neuroplasticity and neuroprotective effects. Its regulation of GABRA1 may relieve anxiety and improve emotional stability.

Druggability evaluation and pharmacokinetics

Bupleurum hyposaponin F has a relatively large molecular weight (618.8520 Da) and high polarity (TPSA 128.84), which limits its oral bioavailability and ability to cross the blood-brain barrier (low blood-brain barrier permeability). The LogP value was 4.2377, indicating it has some lipophilic properties that facilitate cell membrane penetration, but its water solubility is extremely low (0.0044 mg/mL), which may affect its distribution and absorption in vivo.

In terms of safety, Bupleurum saponin F did not show hERG channel inhibition, reducing the risk of cardiotoxicity; A negative Ames test suggests a low risk of genotoxicity. Pharmacokinetic data are still incomplete, but based on its physicochemical properties, Bupleurum Saponin F may need to be designed in special formulations (such as nanocarriers and liposomes) to improve bioavailability and targeting.

Prospects and outlooks for clinical applications

Bupleurum Saponin F, as a multifunctional natural product, possesses multiple pharmacological activities including anticancer, hemolysis, and antidepressant, demonstrating broad clinical application potential. In the field of tumor treatment, its role in inducing cancer cell apoptosis and enhancing chemotherapy sensitivity deserves further clinical validation. Its hemolytic properties suggest its potential for application in hematologic disease regulation, but safety should be carefully evaluated.

The multi-target mechanism of antidepressant action provides a theoretical basis for the development of novel antidepressant drugs. Given the current issues of delayed efficacy and side effects of antidepressants, Bupleurum Saponin F is expected to become an alternative or adjunctive treatment option from natural sources. However, its low blood-brain barrier permeability and poor water solubility limit the efficacy of central nervous system drugs. In the future, it will be necessary to optimize its pharmacokinetic properties through chemical modifications or carrier systems.

In addition, Bupleurum hyposaponin F has good safety, providing favorable conditions for its clinical development. In the future, in vivo pharmacokinetic research, toxicological evaluation, and preclinical model validation should be strengthened to advance toward the clinical trial stage.

Conclusion

Bupleurum hyposaponin F, as an important active component among bupleurum saponins, demonstrates therapeutic potential in anti-cancer, hemolysis, and antidepressant areas due to its unique chemical structure and multiple pharmacological activities. Its multi-target mechanism of action provides rich scientific evidence for the development of natural product drugs. Despite druggability challenges such as low water solubility and poor blood-brain barrier penetration, reasonable drug design and formulation improvements are expected to overcome these limitations. In the future, Bupleurum hyposaponin F is expected to become an innovative molecule in the field of natural medicines, opening new avenues for the treatment of tumors and neuropsychiatric diseases. Systematic pharmacokinetic studies and preclinical evaluations will be key to driving its clinical translation. In summary, Bupleurum Saponin F has the potential to become a versatile natural drug and is worth further exploration and development.