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Product name: Aloin(mixture of A&B)
Synonym name: Barbaloin; Socaloin; Ugandaloin; Jafaloin; Cafaloin
Catalogue No.: BP0151
Cas No.: 8015-61-0
Formula: C21H22O9
Mol Weight: 418.398
Botanical Source: Aloe
Physical Description:
Type of Compound: Anthraquinones
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 Aloin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
180.6400
.1900
-.9700
Low
No
No
No
No
No
No
Aloin (also known as aloin glycoside) is an anthraquinone glycoside compound naturally found in plants of the Aloe genus. It is mainly composed of two diastereomers: aloin A (barbaloin) and aloin B (isobarbaloin). As one of the main active ingredients in aloe leaf exudate, aloe glycoside has attracted widespread attention in the field of natural product pharmacology in recent years due to its unique pharmacological activity and diverse biological effects. Its main pharmacological effects include laxative effects, anti-inflammatory, anti-tumor, osteogenesis promotion, and neuroprotection, demonstrating promising clinical application potential. This paper provides a systematic review of the chemical structure, source and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects of aloe vera glycoside, aiming to provide a theoretical basis and reference for in-depth research and development of this natural product.
Aloe veraside is an anthraquinone glycoside compound with a molecular formula of C21H22O9 and a molecular weight of 418.39. Its structural feature is that the anthraquinone backbone is partially connected to the glucoside by glycosidic bonds, forming a glycoside structure. Aloe glycosides are composed of two diastereomers, aloin A and aloe beta B. Although they differ in spatial configuration, their physicochemical properties are similar. Its appearance is a yellow-brown crystalline powder with a bitter taste.
In terms of physicochemical properties, aloe vera glycoside has a LogP value of 0.19, indicating strong hydrophilicity and good water solubility. The polar surface area (TPSA) is 180.64 Ų, and the number of hydrogen bond acceptors is 9, indicating that its molecules possess strong polarity and hydrogen bond formation ability. The blood-brain barrier penetration capacity is low, with no significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition. Ames-induced mutagenic assays were negative, indicating good safety and drug potential.
Aloin is mainly found in the leaf exudate of Aloe genus plants, detected in at least 68 species of aloe plants, with content reaching 6.6% of the dry leaf weight and 3% to 35% of total exudate. Additionally, the aloe glycoside content in 17 species of aloe plants remains unclear. The content of aloe glycosides is greatly influenced by plant species, harvest time, geographical environment, and extraction process.
Traditional extraction methods mostly use water or ethanol as solvents, and isolate aloe glycosides from aloe leaf exudate through cold immersion, hot reflux, and ultrasound-assisted extraction techniques. The extract is purified through concentration, precipitation, column chromatography, and other steps to obtain high-purity aloe vera glycosides. Modern extraction technologies such as supercritical fluid extraction and membrane separation are also applied to improve extraction efficiency and purity. Optimizing the extraction process not only affects yield but also affects the biological activity and stability of aloe veraside.
Aloe veraside was first widely used in the field of laxatives. As a stimulant laxative that stimulates intestinal peristalsis and promotes water secretion, it induces bowel movements and treats constipation. Its laxative mechanism involves excitation of intestinal smooth muscle and increased intestinal fluid secretion, promoting stool excretion. Clinical and animal experiments have confirmed that aloe veraside has good laxative effects and relatively high safety.
Aloe glycosides and their associated aloe components (such as aloe extract and aloe gel) exhibit significant anti-inflammatory activity. Studies have shown that aloin can significantly improve intestinal inflammatory responses in DSS-induced ulcerative colitis rat models, reducing mucosal damage and infiltration of inflammatory cells. Its anti-inflammatory mechanism may be closely related to inhibiting the release of inflammatory factors, regulating immune cell function, and antioxidant effects.
As a natural anthraquinone glycoside, aloin exhibits strong antitumor activity. In vitro experiments showed that aloin has a significant anti-proliferative effect on various tumor cells at physiological concentrations, with an IC50 of about 97 μM. Its mechanism of action includes inducing cell cycle blockade in the S phase, promoting apoptosis, and significantly increasing the apoptosis rate of HeLa S3 cells (up to 24%). Additionally, aloe veraside has iron-chelating activity, which can influence tumor cell metabolism and growth by regulating intracellular iron homeostasis.
Recent studies have found that aloin can promote osteoblast differentiation and has potential therapeutic value for osteoporosis. Aloin induces MC3T3-E1 cells to differentiate into osteoblasts by activating MAPK-mediated Wnt and Bmp signaling pathways. Alkaline phosphatase (ALP), an early marker of osteoblast differentiation, showed significantly enhanced activity in the aloe glycoside-treated group, suggesting that aloin can promote bone formation and mineralization processes.
Aloin also shows promising potential in the field of neuroprotection. Research shows that aloin can reduce cerebral edema, decrease blood-brain barrier disruption, and improve cortical damage in traumatic brain injury (TBI) models. Its neuroprotective effects may be related to anti-inflammation, antioxidant, and regulatory apoptosis-related signaling pathways, offering new approaches for treating traumatic brain injury.
The multiple pharmacological effects of aloin are based on its complex molecular mechanisms and multi-target regulation. Its main mechanisms of action include:
Signal path regulation
Aloin promotes osteoblast differentiation by activating the MAPK signaling pathway, regulating the Wnt and BMP signaling pathways. This mechanism involves the regulation of the expression of various downstream transcription factors and bone formation-related genes.
Regulation of the cell cycle and apoptosis
Aloe vera glycoside induces tumor cell cycle blockade in the S phase, activates endogenous apoptosis pathways, and increases the cell apoptosis rate. It may regulate cell fate by regulating apoptosis-related proteins such as BCL2 family proteins and MCL1.
Anti-inflammatory and immunomodulatory
Aloe vera glycoside can inhibit the release of pro-inflammatory cytokines, regulate immune cell activity, and reduce inflammatory responses. Relevant targets include immune regulatory factors such as IDO1 and EHMT2.
Iron ion chelation
The iron-chelating ability of aloin helps regulate intracellular iron homeostasis, affects oxidative stress levels and cellular metabolism, thereby exerting antitumor and neuroprotective effects.
Regulation of atherosclerosis-related targets
Aloin has shown potential in regulating key targets such as AMPK (PRKAA1), LOX-1, and ABCA1 in atherosclerosis studies, potentially slowing pathological progression by improving lipid metabolism and suppressing inflammatory responses.
Druggability evaluation of aloe veraside shows it has good potential for drug development. Its molecular weight is moderate (418.39 Da) and its LogP value is low (0.19), indicating good water solubility and moderate lipid solubility, which are beneficial for absorption and distribution in the body. High TPSA and the number of hydrogen bond receptors suggest strong polarity, which may limit the blood-brain barrier penetration ability, but this aligns with its local mechanism of neuroprotective action.
Toxicological evaluation showed that aloin had no significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition, and Ames mutagenicity test was negative, indicating relatively high safety. The low blood-brain barrier penetration suggests limited distribution in the central nervous system, but effective targeting can be achieved through local administration or modified formulations.
In terms of pharmacokinetics, current research is relatively limited. Aloin is absorbed quickly after oral administration, but its bioavailability is limited by gastrointestinal metabolism and first-pass effects. In the future, systematic pharmacokinetic studies, including absorption, distribution, metabolism, and excretion (ADME) characteristics, are needed to guide clinical drug use and formulation design.
As a versatile natural product, aloe veraside has broad clinical application potential. As a stimulant laxative, it has been widely used clinically and is safe and effective. In the future, the development of aloin in the following fields is worth attention:
Anti-inflammatory and intestinal diseases
The improvement effect of aloin on ulcerative colitis and other inflammatory bowel diseases provides a foundation for the development of novel anti-inflammatory drugs. Combined with modern drug delivery technologies, targeted therapy is expected to be achieved.
Anti-tumor treatment
The apoptotic and anti-proliferative effects of aloin make it a candidate molecule for natural anti-tumor drugs, especially with potential value in treating solid tumors such as cervical cancer. More in vivo and in vitro mechanism studies and preclinical safety evaluations are needed in the future.
Osteoporosis and bone repair
By promoting osteoblast differentiation, aloe glycosides are expected to become adjunctive therapies for osteoporosis and fracture repair, combining biomaterials and tissue engineering technologies to develop functional bone repair agents.
Neuroprotection and brain injury
The protective effect of aloin in traumatic brain injury offers new ideas in the field of nerve repair, and future exploration of its combined use with other neuroprotectants and optimization of dosage forms may be explored.
Cosmetic applications
The tyrosinase-inhibiting activity of aloin makes it an ideal whitening agent for treating hyperpigmentation, and it has been used in various cosmetic formulations with broad market prospects.
Although aloe veraside exhibits multiple biological activities, its clinical application still faces some challenges, including low bioavailability, complex metabolism in vivo, and a lack of systematic clinical trial data. Future research should strengthen systematic evaluation of its pharmacokinetics, toxicology, and clinical efficacy, while exploring structural modification and novel delivery systems to enhance its efficacy and safety.
As an important active ingredient in the Aloe genus, aloe glycoside demonstrates promising natural drug development potential due to its unique chemical structure and diverse pharmacological activities. Its research in laxatives, anti-inflammation, anti-tumor, osteogenesis promotion, and neuroprotection has deepened, providing new strategies and ideas for the treatment of related diseases. In the future, combining modern drug development technologies with multidisciplinary research is expected to promote the transformation of aloe veraside from a natural product into clinical drugs, making greater contributions to human health.
Shenshuai
Wenjing
Hedandan
