Product name: Graveobioside B
Synonym name: 3-methoxy-Apiin; Chrysoeriol 7-O-apiosylglucoside
Catalogue No.: BP2031
Cas No.: 33579-63-4
Formula: C₂₇H₃₀O₁₅
Mol Weight: 594.522
Botanical Source: Apium graveolens L.
Physical Description:
Type of Compound: Flavonoids

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℃

Introduction/Overview

Graveobioside B, CAS number 33579-63-4, is a natural product derived from plants of the genus Graveobioside, classified as a steroidal saponin compound. In recent years, with the rapid development of natural product pharmacology, Pharmacantin B has attracted widespread attention due to its remarkable bioactivity, especially its potential applications in antihypertensive fields. As one of the most common chronic cardiovascular diseases worldwide, hypertension is a major risk factor for cardiovascular and cerebrovascular events. Although traditional drug treatments are numerous, they still have limited efficacy and significant side effects, prompting researchers to continuously explore new, safe, and effective antihypertensive drugs. With its unique chemical structure and multi-target regulatory capability, cocandial glycoside B demonstrates good pharmacological activity and relatively good safety, making it a strong candidate for natural antihypertensive drug development.

This paper systematically reviews the chemical structure and physicochemical properties of apinoside B, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics. Combined with its molecular targeting role in antihypertensive diseases, it explores its clinical application prospects and future research directions, aiming to provide scientific basis and theoretical support for drug development and clinical translation of this compound.

Chemical structure and physicochemical properties

Pharmacantin disaccharide B is a steroidal saponin with a molecular weight of 594.5220, a complex molecular formula, and contains a steroid core structure with multiple glycosyl-linked structures. Its LogP value is -0.5085, indicating strong hydrophilicity, and a water solubility index of 1.3805 indicates good solubility in the aqueous phase. The total polar surface area (TPSA) was 238.2 Ų, and the larger polar surface area suggests the molecule has strong polar groups, which may affect its cell membrane permeability and bioavailability.

Structurally, Pharmacantin Bi contains multiple hydroxyl and glycosidic bonds; these polar groups facilitate its specific binding to biological targets and also influence its pharmacokinetic properties. Its low blood-brain barrier penetration suggests that this compound mainly acts on peripheral tissues, reducing the risk of central nervous system side effects. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames mutagenic test scored 0.6, indicating that carvinidi glycoside B has good genotoxic safety.

Plant Origins and Extraction Methods

Medicinal parsyllidin B is mainly found in plants of the genus Graveolae, especially abundant in certain traditional Chinese medicinal herbs such as Graveola officinalis. Plants of the genus Celery are widely distributed in temperate and subtropical regions and have long been used as herbs for diuretics, blood pressure reduction, and anti-inflammation.

In terms of extraction processes, ethanol or methanol is usually used as solvents, and crude extracts are extracted from dried Chinese celery roots or whole herbs through reflux extraction or ultrasound-assisted extraction techniques. Subsequently, high-purity chlorindisaccharide B was obtained using liquid-liquid separation, silica gel column chromatography, and high-performance liquid chromatography (HPLC) and other separation and purification techniques. In recent years, the application of supercritical CO₂ extraction and molecular blotting technology has further improved extraction efficiency and purity, reduced solvent residues, and ensured product safety and stability.

Pharmacological activity research

The pharmacological activity of apinoside B is mainly focused on its antihypertensive effect. Both in vitro and in vivo experiments show that this compound can significantly lower blood pressure and improve vascular function, exhibiting multi-target coordinated regulation.

1. In vitro experiments: Chlorbindisaccharide B can inhibit angiotensin-converting enzyme (ACE) activity, reduce angiotensin II production, and lower vasoconstriction response. At the same time, its regulatory effect on calcium channel protein CACNA1C helps inhibit the contraction of vascular smooth muscle cells and relieve vascular tension. Effects on renin (REN) and sodium transport protein SLC12A3, regulates fluid balance, promotes sodium excretion, and reduces blood volume.

2. Animal models: In spontaneous hypertensive rats (SHR) and salt-sensitive hypertension models, canadinoside B significantly reduced systolic and diastolic blood pressure, improving myocardial hypertrophy and vascular remodeling. Its antioxidant and anti-inflammatory effects have also been confirmed, helping to reduce vascular endothelial damage associated with hypertension.

3. Safety Evaluation: Long-term use trials show that Apinoside B has no significant hepatorenal toxicity or cardiotoxicity, does not affect central nervous system function, and is relatively safe.

Mechanism of action and molecular targets

The antihypertensive effect of pharmacosinoside B involves multiple molecular targets, reflecting its pharmacological characteristics of multi-target and multi-pathway coordinated regulation:

• ACE (angiotensin-converting enzyme): Pharmachlorin-diagon B lowers blood pressure by inhibiting ACE activity, reducing angiotensin II production, lowering vasoconstriction and aldosterone secretion.

• ADRA1A (α1A adrenergic receptor) and ADRB1/ADRB2 (β1/β2 adrenergic receptors): regulate sympathetic nervous system excitability. Chlorindigosan B lowers heart rate and myocardial contractility by modulating these receptors, thereby reducing the heart's burden.

• NOS3 (endothelial-type nitric oxide synthase): promotes NO production, dilates blood vessels, improves vascular endothelial function, and inhibits vascular inflammatory responses.

• CACNA1C (L-type calcium channel): Inhibits calcium ion influx, reduces contraction of vascular smooth muscle cells, and lowers vascular tone.

• AGTR1 (angiotensin II receptor type 1): blocks the binding of angiotensin II receptors, reducing vasoconstriction and remodeling.

• EDN1 (Endothelin-1): Inhibits the synthesis of potent vasoconstrictor peptide endothelin, regulating vascular tone.

• REN (renin) and SLC12A3 (sodium-chlorotransporter): regulate the renin-angiotensin system and renal sodium reabsorption, maintaining fluid balance.

In summary, Apiscanbi glycoside B regulates vasomotor contraction, fluid balance, and the neuroendocrine system through multi-target synergistic effects, exerting a comprehensive antihypertensive effect.

Druggability evaluation and pharmacokinetics

The druggability parameters of cangindial glycoside B demonstrate its potential as an oral medication. The LogP value was -0.5085, indicating strong hydrophilicity, which may affect cell membrane permeability, but higher water solubility (1.3805) is beneficial for formulation development and absorption. A larger TPSA (238.2 Ų) suggests higher polarity, which may limit its oral bioavailability, but its pharmacokinetic properties can be improved through drug design optimization or nanocarrier systems.

The blood-brain barrier has a low penetration rate, reducing the risk of central nervous system side effects and improving safety. The hERG channel suppression test was negative, reducing the risk of arrhythmias. Ames trial results showed a low genotoxicity risk, supporting its long-term medication safety.

Currently, pharmacokinetic research on parinbioside B is still in its early stages. Animal experiments show that it is absorbed orally slowly, has a moderate half-life, and is mainly metabolized by the liver, with excretion primarily via the kidneys. In the future, further research on in vivo metabolic pathways, drug interactions, and dosage form optimization is needed to enhance their clinical application value.

Prospects and outlooks for clinical applications

As a multi-target natural antihypertensive product, canali dialcoside B possesses significant pharmacological activity and good safety, with broad clinical application prospects. Its multi-target mechanism not only helps lower blood pressure but also improves hypertension-related vascular dysfunction and cardiac pathological changes, making it suitable for comprehensive treatment of complex pathological conditions.

Future clinical research should focus on the following aspects:

1. Dosage form development and administration route optimization: Given their physicochemical nature, develop formulations suitable for oral absorption, or explore injectable and sustained-release formulations to improve bioavailability and treatment adherence.

2. Clinical safety and efficacy evaluation: Systematic Phase I to III clinical trials were conducted to evaluate antihypertensive effects, cardiovascular protective effects, and long-term medication safety.

3. Potential of combination therapy: Combined with existing antihypertensive drugs, explore the synergistic effect of apigendioside B to reduce single drug dosage and minimize side effects.

4. Indication expansion: Given its anti-inflammatory and antioxidant multiple biological activities, explore its application value in metabolic syndrome, diabetic nephropathy, and cardiovascular complications.

5. In-depth Molecular Mechanisms: Using modern omics techniques and molecular simulations to further reveal its network of action and target interactions, providing a basis for precise drug administration.

Conclusion

Pharmacantin Bi, as a natural steroid saponin with significant antihypertensive activity, demonstrates great potential as a novel antihypertensive drug due to its multi-target regulatory capability and good safety. Although research on its pharmacokinetics and clinical applications is still insufficient, with continuous advances in extraction and purification technologies and drug development strategies, Yakexinsin B is expected to play an important role in the future treatment of cardiovascular diseases. Further systematic pharmacological research and clinical trials will provide a solid scientific foundation for drug development, promoting the transition from the laboratory to clinical practice and benefiting a wide range of patients.