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Product name: Atractyloside potassium salt
Synonym name:
Catalogue No.: BP0219
Cas No.: 102130-43-8
Formula: C30H44K2O16S2
Mol Weight: 802.983
Botanical Source: Siberian Cocklour Fruit
Physical Description:
Type of Compound: Diterpenoids
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.
Chengdu Biopurify Phytochemicals Ltd. is a leading company in the research, development, manufacture and marketing of High Quality Phytochemicals and Extracts(especially Active Ingredients from Traditional Chinese Medicine，TCM), Natural Active Pharmaceutical Ingredients worldwide.
The main services:
A. Supply active ingredients and reference standards of TCM, from mgs to kgs scale
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E. TCM compounds library for drug screen,more than 3000 compounds available, many of them are rare and unique.
HPLC of Atractyloside potassium salt
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
300.0000
-3.0000
-5.0000
No
No
No
Atractyloside potassium salt (CAS No. 102130-43-8), as a bioactive compound derived from a natural product, has attracted widespread attention in pharmacological research in recent years. Its main mechanism of action is the efficient and specific inhibition of mitochondrial ADP/ATP transporter (ANT), thereby affecting cellular energy metabolism and apoptosis signaling pathways. Potassium atractyloside salt is not only used as a molecular tool for mitochondrial function regulation in basic biological research, but also exhibits various potential pharmacological activities, including autophagy activation, tumor suppression, and intervention in metabolic diseases. This paper aims to systematically review the chemical structure, origin, pharmacological activity, mechanism of action, and druggability evaluation of Cangzhu glycoside potassium salt, explore its potential and challenges in clinical application, and provide a theoretical foundation and reference direction for subsequent research.
The molecular formula of potassium atractyloside salt is C_35H_58K_2O_16, with a molecular weight of 795.0300, making it a natural glycoside compound with a large molecular weight. Its structural core is atractyloside, which forms potassium salts through potassium ion coordination, enhancing its water solubility and stability. In terms of physicochemical properties, potassium atractyloside salt exhibits low lipid solubility (LogP about -3.0), indicating strong hydrophilicity, a polar surface area (TPSA) of up to 300, and containing 16 hydrogen bond receptors. These features limit its ability to cross the blood-brain barrier (BBB negative). Additionally, potassium cangzhagioside salt does not exhibit significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition, suggesting that its safety is somewhat controllable.
Structurally, potassium atractyloside salt contains multiple hydroxyl and glycosidic bonds, giving it strong water solubility and potential for binding to protein targets. Its specific ability to inhibit mitochondrial ADP/ATP transporters is closely related to the precise matching of the glycoside portion in its molecule to the protein-binding site.
Atractylodes glycoside potassium salt mainly comes from Atractylodes lancea and its related species, a plant in the Asteraceae family. Atractylodes is a traditional Chinese medicinal herb widely distributed in East Asian regions such as China, Japan, and South Korea. The rhizome of Atractylodes is rich in polysaccharides, volatile oils, and various glycosides, among which Atractyloside is one of its important active components.
The extraction method typically uses water extraction combined with alcohol precipitation or column chromatography purification techniques. The specific steps include: crushing the dried Atractylodes rhizome, reflux extraction with water or 70% ethanol, concentration, separation and purification using ion exchange resin or silica gel column chromatography, and finally obtaining high-purity potassium atractyloside salt. Modern extraction processes are gradually introducing ultrasound-assisted extraction and high-performance liquid chromatography (HPLC) purification technologies to improve yield and purity.
The pharmacological activity of potassium atractyloside salt mainly revolves around its regulation of mitochondrial function. As a highly effective and specific mitochondrial ADP/ATP transport inhibitor, potassium atractyloside salt can block the exchange of ADP and ATP on the mitochondrial membrane, directly affecting cellular energy metabolism and thereby regulating apoptosis, autophagy, and metabolic homeostasis.
Potassium atractyloside salt demonstrated significant antitumor activity in non-small cell lung cancer (NSCLC) models. Research shows that by inhibiting mitochondrial ADP/ATP transport, it induces an energy crisis in tumor cells, activates the AMPK signaling pathway, suppresses mTOR activity, promotes autophagy and apoptosis, and thus suppresses tumor cell proliferation. Additionally, potassium atractyloside salt regulates the mitochondrial membrane potential and ROS levels of tumor cells, further enhancing its anti-cancer effect.
Potassium atractyloside can inhibit hepatic steatosis and improve lipid metabolism disorders. It activates the AMPK pathway, inhibits the expression of fat-synthesizing enzymes, promotes fatty acid oxidation, and reduces liver fat deposition. In addition, potassium atractyloside glycoside salt demonstrates potential in glucose metabolism regulation by modulating various hyperglycemia-related targets (such as AMPK, SGLT2, GCK, etc.), providing new approaches for the treatment of metabolic syndrome and diabetes.
Potassium atractyloside salt effectively activates cellular autophagy, by which it inhibits the mTOR signaling pathway and promotes p-AMPK activation. Autophagy, as an important homeostatic regulatory mechanism within cells, helps clear damaged mitochondria and protein aggregates, maintaining stable cell function. Potassium atractyloside salt demonstrates potential cellular protection by regulating autophagy pathways, especially in inhibiting chloride ion channels in the mitochondrial membrane of the heart.
Although potassium atractyloside salt has multiple pharmacological activities, its nephrotoxicity should not be ignored. The study pointed out that potassium atractyloside salt may induce tubular cell damage through mitochondrial dysfunction, limiting its safe window for clinical application. Therefore, in-depth analysis of its toxic mechanisms and finding effective detoxification strategies are important directions for future research.
The core mechanism of action of atractylodin potassium salt is the specific inhibition of mitochondrial ADP/ATP transporter protein (ANT). ANT, as a key transport protein on the inner mitochondrial membrane, is responsible for transporting ADP from the cytoplasm into the mitochondrial matrix, while ATP produced by mitochondria is transported to the cytoplasm to maintain cellular energy balance. Potassium atractyloside salt binds to ANT, blocking ADP/ATP exchange, causing mitochondrial energy metabolism disorders and triggering cellular energy depletion and apoptosis signals.
Additionally, potassium atractyloside salt inhibits the expression of ANT2 subtypes and regulates cellular metabolic states. ANT2 is highly expressed in various tumor cells and is involved in regulating cell proliferation and metabolic reprogramming. Inhibiting ANT2 helps suppress tumor growth.
Beyond mitochondrial regulation, potassium atractyloside salt activates the AMPK (5' AMP-activated protein kinase) signaling pathway. AMPK acts as a cellular energy sensor, regulating metabolic balance and autophagy. Potassium atractyloside salt promotes AMPK phosphorylation activation (p-AMPK), inhibits the mTOR (mammalian rapamycin target protein) signaling pathway, thereby initiating autophagy and promoting cellular self-repair and metabolic regulation.
The inhibitory effect of potassium atractyloside salt on chloride channels in rat heart mitochondrial membranes suggests that it may stabilize mitochondrial membrane potentials by regulating ion channels, affecting apoptosis and oxidative stress responses.
Regarding hyperglycemia-related targets, potassium atractyloside glycoside has potential regulatory relationships with multiple proteins such as EHMT2, UBP2, PAI1, SGLT2, GCK, APP, BACE1, CES1, and PTPN1, suggesting that it may regulate glucose metabolism, inflammatory responses, and cellular metabolic homeostasis through multi-target synergistic effects.
The drugability of potassium atractyloside salt is significantly influenced by its physicochemical properties. Its high polarity and large molecular weight limit oral bioavailability and tissue penetration, especially its inability to cross the blood-brain barrier, restricting its potential for central nervous system diseases. Nevertheless, potassium atractyloside salt does not exhibit hepatotoxicity, cardiotoxicity, or hERG channel inhibition, indicating a solid safety foundation.
Pharmacokinetics, potassium atractyloside salt has good water solubility and is easily distributed in hydrophilic tissues such as blood and kidneys, but its metabolic pathway has not been fully elucidated. Given its nephrotoxicity, future research should focus on renal metabolism and excretion mechanisms to optimize administration regimens to reduce toxic side effects.
Through structural modification and drug carrier technologies (such as nanoparticle encapsulation and liposome delivery), it is expected to improve the pharmacokinetic properties of potassium atractyloside glycosides, enhance its in vivo stability and targeting, and enhance its clinical application potential.
As a mitochondrial function regulator, potassium atractyloside salt shows broad application prospects in tumor treatment, metabolic diseases, and cardiovascular diseases. Its potential to combat non-small cell lung cancer offers new ideas for tumor metabolism targeted therapy, especially when combined with traditional chemotherapy or targeted drug therapies, which may exert synergistic effects.
In metabolic diseases, potassium atractyloside salt has the ability to regulate glycolipid metabolism by activating AMPK and inhibiting steatosis, making it a promising candidate for novel drugs for treating non-alcoholic fatty liver disease (NAFLD), diabetes, and related metabolic syndromes.
However, the nephrotoxicity and druggability of potassium atractyloside salt limit its direct clinical application. Future research should focus on reducing toxicity, optimizing administration methods, and structural modifications to enhance safety and efficacy. At the same time, in-depth analysis of its multi-target mechanisms will help in precisely designing combination treatment strategies.
Moreover, the utility value of potassium atractyloside salt in autophagy regulation and mitochondrial function research cannot be overlooked, helping to promote basic research and new drug development for mitochondria-related diseases.
As a naturally derived mitochondrial ADP/ATP transport inhibitor, atractyloside potassium salt demonstrates significant research and application value in anti-tumor, metabolic disease, and autophagy regulation due to its unique mechanism of action and diverse pharmacological activities. Despite nephrotoxicity and druggability challenges, with advances in extraction and purification technologies, structural optimization, and drug delivery systems, potassium atractyloside salt is expected to become an important candidate for new therapeutic drugs in the future. Future research should focus on in-depth analysis of its mechanism of action, safety evaluation, and clinical translation, promoting its widespread application in natural product pharmacology and modern medicine.
Shenshuai
Wenjing
Hedandan
