Product name: Aloesin
Synonym name: Aloe resin B; Aloeresin
Catalogue No.: BP4356
Cas No.: 30861-27-9
Formula: C₁₉H₂₂O₉
Mol Weight: 394.376
Botanical Source:
Type of Compound:

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle


The product could be supplied from milligrams to grams
Inquire for bulk scale.

Aloesin is isolated from freshAloe veraleaves, as well as from other species ofAloe. It is a moderately high molecular weight hydroxy C-glycosylated chromone derivative.

It is a natural compound that has demonstrated appreciable depigmenting activity due to its ability to inhibittyrosinase activity. It is among the top choices for cosmetic and therapeutic applications to lighten skin.

The reputable Aloe vera or Aloe barbadensis has been scientifically proven for all forms of burn, be it radiation, thermal, or solar. It has also been demonstrated that it has a prophylactic effect if used before, during, and after these skin-damaging events. Aloe vera is a uniquely effective moisturizer and healing agent for the skin.

References
1.Modulation of melanogenesis by aloesin: a competitive inhibitor of tyrosinase 

Pigment Cell Res 2002 Oct;15(5):335-40. 

Abstract

Aloesin, [2-acetonyl-8-beta-d-glucopyranosyl-7-hydroxy-5-methylchromone], a compound isolated from the Aloe plant, is shown in these studies to modulate melanogenesis via competitive inhibition of tyrosinase. Aloesin inhibits purified tyrosinase enzyme and specifically inhibits melanin production in vitro. Enzyme kinetics studies using normal human melanocyte cell lysates and cell-based melanin production demonstrated that aloesin is a competitive inhibitor of tyrosinase from mushroom, human and murine sources. Tyrosine hydroxylase and 3,4-dihydroxyphenylalanine (DOPA) oxidase activities of tyrosinase from normal human melanocyte cell lysates were inhibited by aloesin in a dose dependent manner. In a percutaneous absorption study a finite dose of aloesin penetrated the skin slowly and was recovered primarily in the surface wash. Aloesin shows promise as a pigmentation-altering agent for cosmetic or therapeutic applications. 

2. Effects of aloesin on melanogenesis in pigmented skin equivalents.

Int J Cosmet Sci. 2008 Apr;30(2):121-30

3. The effects of aloesin and arbutin on cultured melanocytes in a synergetic method

Zhonghua Zheng Xing Wai Ke Za Zhi. 2004 Sep;20(5):369-71

4.Aloesin and arbutin inhibit tyrosinase activity in a synergistic manner via a different action mechanism.

Arch Pharm Res. 1999 Jun;22(3):232-6.

5. Anti-inflammatory constituents, aloesin and aloemannan in Aloe species and effects of tanshinon VI in Salvia miltiorrhiza on heart

Yakugaku Zasshi. 2003 Jul;123(7):517-32.

HPLC of Aloesin

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

Introduction/Overview

Aloe vera, as an ancient medicinal plant, has a history of application spanning thousands of years and is found in multiple civilizations around the world. Traditionally, aloe gel has been widely used to treat skin burns, wounds and inflammation. With the development of modern separation and identification techniques, numerous bioactive components in aloe vera have been revealed, and one important class of chromogenic ketone derivatives, Aloesin (also known as Aloeresin), has gradually become a research hotspot. Aloe vera extract (CAS number: 30861-27-9) is a natural tyrosinase inhibitor known for its excellent skin whitening properties in the cosmetics industry. However, in recent years, in-depth research has continuously expanded the boundaries of its biological significance, revealing its potential pharmacological value in multiple aspects such as anti-inflammatory, UV protection, antibacterial, promoting skin repair, and even anti-tumor. Especially in the field of skin repair, it exhibits multi-target and multi pathway effects by regulating the expression of matrix metalloproteinases (MMPs), growth factors (such as EGF, FGF, VEGF), and extracellular matrix (ECM) components (such as collagen), providing new candidate molecules for the development of novel skin repair therapies. This article aims to systematically review the chemical properties, plant sources, pharmacological activities, molecular mechanisms of action, pharmacological evaluation, and clinical application prospects of aloe vera extract, in order to provide comprehensive scientific references for the deep development and transformation research of this natural product.

Chemical structure and physicochemical properties

Aloe vera extract is a C-glycosylated chromone derivative. Its core structure is a chromogen ketone parent nucleus (benzo - γ - pyranone), which is connected to a glucose group through a carbon carbon bond at the C-8 position of the parent nucleus. Compared to common O-glycosidic bonds, this C-glycosidic bond has stronger chemical stability and resistance to enzymatic hydrolysis, which to some extent explains its stability exhibited in in vitro and in vivo experiments.

Its molecular formula is C19H22O9 and its molecular weight is 394.3760 g/mol. From the perspective of drug formation, its topological polar surface area (TPSA) is 157.66 Å ², which is relatively high, indicating strong molecular polarity and good interaction ability with water molecules. The calculated lipid water partition coefficient (LogP) is approximately 0.0333, belonging to the category of hydrophilic compounds. The theoretically predicted water solubility value is 4.2132 (usually measured in mg/mL or log mol/L, indicating moderate to high solubility), and these physicochemical parameters collectively indicate that aloin has good water solubility, which is beneficial for its application in water-based formulations and oral dissolution and absorption.

However, higher polarity and TPSA also mean that its ability to penetrate biofilms may be limited. The prediction shows that its blood-brain barrier (BBB) permeability is low, suggesting that its main pharmacological effects may be concentrated in the peripheral system, especially in local application scenarios such as the skin, while also reducing the potential risk of central nervous system toxicity. In terms of early safety indicators, its Ames test value is 1.2 (usually considered negative if less than 2), indicating no significant mutagenicity; If there is no inhibitory activity on hERG potassium channels, the serious risk of inducing QT interval prolongation and apical torsion type ventricular tachycardia has been preliminarily ruled out, providing preliminary positive signals for its safety.

Plant sources and extraction methods

Aloe vera extract mainly comes from the genus Aloe in the lily family（Aloe）Plants, especially aloe vera in Curacao（Aloe barbadensis Miller， Also known as Aloe vera）The leaf skin (i.e. green outer skin) and the yellow latex layer at the junction of leaf flesh and outer skin are relatively abundant in content. Different varieties of aloe vera, planting conditions, harvesting sites, and growth years can all affect the content of aloin.

Extracting aloe vera extract from plant materials usually follows the conventional process of natural product chemistry. First, the fresh aloe leaves need to be pretreated, washed and separated from the skin and gel. The target compound is mainly extracted from dried powder of the outer skin or whole leaves.
1. Solvent extraction method The most commonly used method is to use polar solvents for extraction. Methanol, ethanol, water, or alcohol water mixed solvents in different proportions are effective extraction media. For example, using a 70% -80% ethanol aqueous solution for extraction under heating or ultrasound assistance can efficiently dissolve aloe vera extract.
2. ​Purification and Separation After filtering and concentrating the crude extract, a paste rich in aloe vera extract is obtained. Further purification requires the use of column chromatography technology, often using silica gel, reverse phase silica gel (such as C18), or macroporous adsorption resin as the stationary phase, and using gradient elution systems such as chloroform methanol, water methanol, or water ethanol for separation. High performance liquid chromatography (HPLC) and preparative thin layer chromatography (PTLC) are key steps in obtaining high-purity monomers.
3. ​appraisal The isolated compounds were structurally confirmed by nuclear magnetic resonance (NMR, including 1H-NMR and 13C-NMR), mass spectrometry (MS), infrared spectroscopy (IR), and chromatographic behavior (such as HPLC retention time) compared to standard samples.

In recent years, some green extraction techniques such as supercritical CO2 extraction, microwave-assisted extraction, and pressurized liquid extraction have also been explored to improve extraction efficiency and selectivity, but large-scale production still relies mainly on low-cost solvent extraction combined with column chromatography.

Pharmacological activity research

Aloe vera extract exhibits a wide range of pharmacological activities, and its potential for application far exceeds the initial scope of skin whitening.

1. Tyrosinase inhibition and skin whitening This is the earliest and most famous activity of aloe vera extract. It competitively inhibits the activity of tyrosinase, effectively blocking the key step in the melanin synthesis pathway - the conversion of tyrosine to dopaquinone, thereby reducing melanin production. Its effect is clear, and due to its natural origin and relatively mild characteristics, it is widely added to whitening cosmetics.
2. anti-inflammatory activity Aloe vera extract has shown significant anti-inflammatory effects in various acute and chronic inflammation models. It can inhibit the excessive production of nitric oxide (NO), prostaglandin E2 (PGE2), and pro-inflammatory cytokines (such as TNF - α, IL-1 β, IL-6) in macrophages induced by stimuli such as lipopolysaccharide (LPS). Its anti-inflammatory mechanism is closely related to the inhibition of the activation of inflammatory signaling pathways such as nuclear factor kappa B (NF - κ B) and mitogen activated protein kinases (MAPKs).
3. Ultraviolet (UV) protection Research has shown that aloe vera extract can absorb ultraviolet radiation, especially in the UVB band, and has a certain physical shielding effect. More importantly, it can alleviate cellular oxidative stress caused by UV radiation, enhance the activity of intracellular antioxidant enzymes (such as superoxide dismutase (SOD) and glutathione peroxidase (GPx)), eliminate free radicals, thereby protecting skin cells from photodamage and preventing photoaging.
4. Antibacterial effect Aloe vera extract exhibits inhibitory activity against various Gram positive and Gram negative bacteria, such as Staphylococcus aureus and Escherichia coli. Its antibacterial mechanism may involve disrupting the integrity of bacterial cell membranes, inhibiting bacterial biofilm formation, or interfering with their metabolic processes.
5. Promote skin repair and wound healing This is an important direction of current research. Aloe vera extract can accelerate the healing process of experimental animal skin wound models. Its function is reflected in multiple stages such as reducing inflammation, promoting granulation tissue formation, increasing collagen deposition, and promoting epithelial regeneration.
6. Antitumor activity Preliminary research has revealed the anti-tumor potential of aloe vera extract. In ovarian cancer research, it can induce apoptosis of cancer cells and inhibit their proliferation. Its pro apoptotic effect may be related to activating the caspase cascade, regulating the proportion of Bcl-2 family proteins, and inducing mitochondrial dysfunction.

Mechanism of action and molecular targets

The multiple pharmacological activities of aloe vera extract stem from its multi-target regulation of cellular signaling networks. In the core application scenario of skin repair, its mechanism of action involves fine regulation of multiple links such as extracellular matrix metabolism, cell proliferation and migration, angiogenesis, and inflammatory response, with clear molecular targets:

• Regulating matrix metalloproteinases (MMPs)MMPs are key enzymes that degrade extracellular matrix (ECM), and their overexpression is the main cause of delayed wound healing, chronic ulcers, and skin photoaging. Aloe vera extract can significantly downregulate MMP-1(Interstitial collagenase, which degrades type I and III collagen)MMP-2 and MMP-9 Expression and activity of gelatinase, which degrades type IV collagen and denatured collagen. This helps protect the ECM structure and provides a stable scaffold for cell migration and tissue reconstruction.
• Affects the growth factor signaling pathway：
  • Epidermal growth factor receptor (EGFR)Aloe vera extract may affect the proliferation and migration of keratinocytes and fibroblasts by regulating the phosphorylation or downstream signaling of EGFR, which is crucial for epithelialization and granulation tissue formation.
  • Fibroblast Growth Factor 2 (FGF2) and Vascular endothelial growth factor A (VEGFA)Aloe vera extract may positively regulate the expression of these angiogenic factors, promote neovascularization (angiogenesis) at the wound site, and provide sufficient oxygen and nutrition for tissue repair.
  • Transforming Growth Factor Beta 1 (TGFB1)TGFB1 is a potent stimulant for collagen synthesis. Aloe vera extract may promote the differentiation of fibroblasts into myofibroblasts and stimulate their growth by affecting the TGFB1/Smad signaling pathway Type I collagen (COL1A1) and Type III collagen (COL3A1) and Type IV collagen (COL4A1) The synthesis of ECM increases the deposition of ECM and enhances tissue strength.
• Regulating cell adhesion and migration Integrin β 1（ITGB1）It is the main receptor for cell adhesion to ECM (such as collagen and fibronectin), mediating cell migration and signal transduction. Aloe vera extract may promote the directed migration of repair cells (such as keratinocytes and fibroblasts) to the wound area by affecting the expression or activation status of ITGB1.
• Synergistic anti-inflammatory effect Its ability to inhibit the NF - κ B and MAPK pathways not only directly reduces the inflammatory response, but also indirectly reduces the induced expression of MMPs by inflammatory factors (such as TNF - α, IL-1 β) and the damage to ECM, thereby creating a favorable microenvironment for repair.

In summary, aloe vera extract exerts a dual regulatory effect of "inhibiting MMP degradation of ECM" and "promoting growth factor mediated ECM synthesis and remodeling", synergistic with its anti-inflammatory, antioxidant, and pro angiogenic effects, forming a multi-target and multi-level skin repair network.

Evaluation of drug properties and pharmacokinetics

Based on its physical and chemical properties, aloe vera extract has shown certain potential for medicinal use, but there are also challenges.

• Absorption, distribution, metabolism, excretion (ADME)：
  • absorb Due to its good water solubility and medium molecular weight, it may have a certain degree of absorption in the small intestine after oral administration. However, its high polarity and TPSA may limit its passive transmembrane diffusion, and its bioavailability needs to be experimentally confirmed. Topical application is the most direct and effective route of administration, which can directly act on the target site.
  • distribution Predict low blood-brain barrier permeability, mainly distributed in peripheral tissues and organs. When applied locally on the skin, the key to its deep repair function is whether it can effectively penetrate the stratum corneum to reach the dermis layer, which may require the use of transdermal enhancers or nanocarriers.
  • Metabolism and excretion As a C-glycoside, aloe vera extract is relatively stable to intestinal glycosidase, but may undergo phase II metabolism in the liver (such as glucuronidation and sulfation). The prototype drug and its metabolites are mainly excreted through the kidneys and urine. Further in vivo pharmacokinetic studies are needed to clarify the specific metabolic profile and half-life.
• Optimization direction of drug properties：
  1. Improve bioavailability To address the issue of poor oral absorption, self microemulsions, liposomes, solid dispersions, and other formulations can be developed. For external use, transdermal drug delivery systems such as liposomes, delivery systems, and nanoemulsions can be considered to enhance their skin permeability and retention.
  2. Structural modification Chemical modification of the sugar moiety or substituents on the benzene ring while retaining its core pharmacophore (chromogen ketone) may optimize its LogP value, improve membrane permeability, or enhance affinity for specific targets.
  3. safety The existing preliminary data (Ames negative, no hERG inhibition) is positive, but a systematic preclinical safety evaluation is still needed, including acute toxicity, long-term toxicity, reproductive toxicity, etc., to comprehensively evaluate its safety window.

Clinical application prospects and prospects

Aloe vera extract is gradually moving from a traditional plant component to a modern drug candidate with clear molecular targets, and its clinical application prospects are broad

1. Dermatology drugs and high-end functional skincare products：
   • Wound healing and treatment of chronic ulcers: Based on its clear repair promotion mechanism, develop local treatment drugs (gel, spray, dressing) for chronic refractory wounds such as diabetes foot ulcer, venous ulcer, pressure injury, etc.
   • Anti photoaging and skin repair Compound it with other antioxidants such as vitamin C and E to develop drugs or cosmetics for preventing and treating photoaging, improving skin elasticity, and reducing wrinkles.
   • Postoperative repair and scar management Used in plastic surgery and burn surgery to inhibit excessive inflammation and MMPs expression, promote normal tissue regeneration, and may help reduce pathological scar formation.
2. neoadjuvant therapy The activity of inducing apoptosis in tumors such as ovarian cancer deserves further exploration. Or it can be used as a sensitizer for chemotherapy/radiotherapy, or to alleviate side effects such as skin and mucosal inflammation caused by radiotherapy and chemotherapy.
3. Other potential areas Its anti-inflammatory activity may be suitable for adjuvant treatment of certain mild to moderate inflammatory skin diseases, such as atopic dermatitis, acne, etc.

Future research priorities should include:
* In depth mechanism research Using techniques such as gene knockout, CRISPR-Cas9, proteomics, etc., to more accurately elucidate its direct interactions with key targets such as EGFR and TGFB1 receptors.
* Preclinical and clinical research Conduct standardized animal pharmacology, pharmacokinetics, and toxicology studies, and ultimately advance them to human clinical trials to verify their effectiveness and safety in different indications.
* Development of new formulations Vigorously developing targeted delivery systems based on nanotechnology to improve the efficiency of local or systemic drug delivery.
* Structural Optimization and Synthetic Biology Through chemical synthesis or synthetic biology methods (such as microbial heterologous synthesis), efficient and sustainable production of aloe vera extract can be achieved, providing a material basis for obtaining more active derivatives.

Conclusion

Aloe vera extract, as a natural active molecule discovered from the ancient medicinal plant aloe vera, has evolved from traditional experience to a model of modern scientific interpretation in its research process. From the initial tyrosinase inhibitor to the pharmacological value revealed in multiple dimensions such as skin repair, anti-inflammatory, antioxidant, antibacterial, and even anti-tumor, its biological connotation has been continuously enriched. Of particular importance is that its mechanism of action in skin repair has been extensively studied at the level of key molecular targets such as MMPs, growth factors and their receptors, and extracellular matrix components, outlining a clear multi-target action network. Although there are still challenges in terms of drug development, such as bioavailability and delivery efficiency, its good water solubility, preliminary safety, and clear mechanism of action have laid a solid foundation for its further development. With the deep integration of modern pharmacy, medicinal chemistry, and molecular biology technologies, aloe vera extract is expected to successfully transform from a cosmetic efficacy ingredient into an innovative drug for treating skin damage, chronic ulcers, and related diseases, fully reflecting the sustained vitality and enormous potential of natural products in contemporary new drug research and development.