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Objective: Ocular chemical burns are a leading cause of blindness. The cornea is injured by alkali-induced oxidative disturbances and an inflammatory response. The aim of this study was to evaluate the protective effects of aloin, an antioxidant, and anti-inflammatory compound, on corneal alkali burn. Materials and methods: Mice eyes were injured by NaOH and subsequently treated with aloin eye drop and intraperitoneal injection. Pathological characteristics of the eyes were examined, and corneal samples were collected for further analysis. Results: Aloin diminished neutrophil infiltration and the production of proinflammatory cytokines. Aloin also attenuated apoptosis in human corneal epithelial cells (HCEs) by reducing oxidative stress through the activation of the Nrf2 pathway. Additionally, aloin suppressed the formation of neutrophil extracellular traps (NETs) and inhibited their deposition on the cornea. Moreover, aloin mitigated alkali-induced apoptosis in HCEs caused by NETs. Conclusions: These findings suggest that aloin has potential as an antioxidant and anti-inflammatory compound for treating corneal alkali burn by inhibiting NETs formation and promoting Nrf2. [ABSTRACT FROM AUTHOR]

Aim The objective of this in-vitro study was to assess the cytotoxicity and alkaline phosphatase (ALP) activity of curcumin and aloin extracted from Curcuma longa and Aloe vera, and mineral trioxide aggregate (MTA) on human dental pulp stem cells. Methods Human dental pulp stem cells (Lonza Group, Switzerland), curcumin (Sigma-Aldrich, USA), aloin (Sigma-Aldrich, USA), and ProRoot MTA (Dentsply, USA) were used in the study. 2.5-6.75-12.5-25-50 μg/ml of curcumin and aloin, 25%-50%-75%-100% of MTA were prepared; pulp cells unincubated with a material were assessed as controls. Cytotoxicity of all doses/concentrations of materials was analysed on days of 1, 2, 3, and 7 by WST-1 test. 2.5-6.75 μg/ml of curcumin and aloin, 25%–50% of MTA incubated with cells for 7–14 days were evaluated for ALP activity by ELISA test. Data was statistically analysed by One Way ANOVA, Tukey, and Sidak tests at GraphPad Prism 6. Results The findings have shown that 2.5 μg/ml of curcumin, all doses of aloin, 25% and 50% of MTA increased cell proliferation significantly on day 1 (P < 0.05). Curcumin, aloin, and MTA decreased the cell viability as dose/concentration and exposure time increased. All materials have shown no significant increases in ALP activity (P > 0.05) on 7 and 14 days. Conclusion Data of this study revealed that 2.5 - 6.75 μg/ml of curcumin/aloin, 25%–50% of MTA have promoted cell viability and proliferation of human dental pulp cells; and none of the materials have significantly increased the ALP activity at 7–14 days.

The prevention of enzymatic browning through the application of tyrosinase inhibitors has become a research focus in food industry. In this article, multi-spectroscopic and computational simulation was used to study the binding behavior and inhibition mechanism of aloin to tyrosinase. It found that aloin was an effective inhibitor of tyrosinase activity with a mixed type inhibition. Aloin bound to tyrosinase through hydrophobic forces, causing a conformational change in the enzyme and resulting in its inherent fluorescence being quenched. There was a binding site for aloin with tyrosinase and the binding constant was approximately 104 L mol−1. Molecular simulations showed that hydrophobic and hydrogen-bonding forces were the main factors in the binding of aloin to tyrosinase. Aloin introduced into the active site of tyrosinase interacted with amino acid residues Gly281, His244, Val283, Ala286 and His263, occupying the catalytic center of the tyrosinase and blocking substrate entry, resulting in tyrosinase inhibition. Molecular dynamics simulation further indicated that the binding of aloin changed the secondary structure of tyrosinase with little effect on the microenvironment of tyrosinase amino acid residues. This study offers new understanding of the mechanisms of activity of aloin as a tyrosinase inhibitor. [ABSTRACT FROM AUTHOR]

The present analytical study focuses on the simultaneous estimation of Aloe emodin, aloin, and emodin as chemical markers commonly found in herbal formulations using the reversed-phase high-performance liquid chromatography (RP-HPLC) method. Aloin, Aloe emodin, and emodin are active components present in Aloe species, rhubarb, and cascara. A novel method based on RP-HPLC was developed for the simultaneous estimation of these chemical markers. A Waters Alliance-e2695 chromatograph with a 150 × 4.6 mm, 3.5 µm column, a mobile phase with acetonitrile, 0.1% formic acid, and methanol (20 : 50 : 30) were used for this analytical work. The flow rate was 1.0 mL/min, and detection was carried out by a PDA detector with an absorption wavelength of 237 nm at an ambient temperature of 25°C. The linearity ranges for Aloe emodin, aloin, and emodin were found to be 25–150, 12.5–75, and 2.5–15 µg/mL, respectively. The mean recoveries of Aloe emodin, aloin, and emodin were within the acceptance limit (98–102%). The relative standard deviation of precision and robustness was found to be less than 2%. Forced degradation studies were carried out for chemical markers with the help of the developed RP-HPLC method, and no considerable degradants were found. The developed stability-indicating method was applied for the quantification of the three markers in the Ayurvedic formulation of Aloe vera. [ABSTRACT FROM AUTHOR]

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Aim: The objective of this in-vitro study was to assess the cytotoxicity and alkaline phosphatase (ALP) activity of curcumin and aloin extracted from Curcuma longa and Aloe vera, and mineral trioxide aggregate (MTA) on human dental pulp stem cells. Methods: Human dental pulp stem cells (Lonza Group, Switzerland), curcumin (Sigma-Aldrich, USA), aloin (Sigma-Aldrich, USA), and ProRoot MTA (Dentsply, USA) were used in the study. 2.5-6.75-12.5-25-50 μg/ml of curcumin and aloin, 25%-50%-75%-100% of MTA were prepared; pulp cells unincubated with a material were assessed as controls. Cytotoxicity of all doses/concentrations of materials was analysed on days of 1, 2, 3, and 7 by WST-1 test. 2.5-6.75 μg/ml of curcumin and aloin, 25%-50% of MTA incubated with cells for 7-14 days were evaluated for ALP activity by ELISA test. Data was statistically analysed by One Way ANOVA, Tukey, and Sidak tests at GraphPad Prism 6. Results: The findings have shown that 2.5 μg/ml of curcumin, all doses of aloin, 25% and 50% of MTA increased cell proliferation significantly on day 1 (P < 0.05). Curcumin, aloin, and MTA decreased the cell viability as dose/concentration and exposure time increased. All materials have shown no significant increases in ALP activity (P > 0.05) on 7 and 14 days. Conclusion: Data of this study revealed that 2.5 - 6.75 μg/ml of curcumin/aloin, 25%-50% of MTA have promoted cell viability and proliferation of human dental pulp cells; and none of the materials have significantly increased the ALP activity at 7-14 days. [ABSTRACT FROM AUTHOR]

Infectious oral diseases are longstanding global public health concerns. However, traditional medical approaches to address these diseases are costly, traumatic, and prone to relapse. Here, we propose a foodborne prophylactic strategy using aloin to safeguard dental collagen. The effect of aloin on the stability of dental collagen was evaluated by treating dentin with a solution containing aloin (0.1 mg/mL) for 2 min. This concentration is comparable to the natural aloin content of edible aloe. Furthermore, we investigated the mechanisms underlying the interactions between aloin and dentin collagen. Our findings, obtained through fluorescence spectroscopy, attenuated total reflection Fourier transform infrared spectroscopy, Gaussian peak fitting, circular dichroism spectroscopy, and X‐ray diffraction, revealed that aloin interacts with dental collagen through noncovalent bonding, specifically hydrogen bonding in situ. This interaction leads to a reduction in the distance between molecules and an increase in the proportion of stable α‐helical chains in the dental collagen. The ultimate tensile strength and thermogravimetric analysis demonstrated that dental collagen treated with aloin exhibited improved mechanical strength and thermostability. Additionally, the release of hydroxyproline, cross‐linked carboxy‐terminal telopeptide of type I collagen, and C‐terminal cross‐linked telopeptide of type I collagen, along with weight loss, indicated an enhancement in the enzymatic stability of dental collagen. These findings suggest that aloin administration could be a daily, nondestructive, and cost‐effective strategy for managing infectious oral diseases. [ABSTRACT FROM AUTHOR]

Aloin is the main medicinal component extracted from Aloe vera. It is a natural anthraquinone compound, with anticancer, anti-in- flammatory and antibacterial and other biological functions. This paper reviews the pharmacological action and related mechanisms of aloin, in order to provide a theoretical basis for the development and utilization of aloin. [ABSTRACT FROM AUTHOR]

• Plants of A. arborescens were cultivated in pots using substrates at increasing amounts of biochar. • Pure biochar allowed a higher development of roots than pure commercial substrate. • Biochar favored the emission of bigger leaves, especially in the median stem portion. • Pure biochar induced the highest quantity of isoaloeresin D, aloin A and aloin A + aloin B in the median leaves. The leaves of the medicinal plant Aloe arborescens Mill. (Asphodelaceae) contain significant amounts of bioactive metabolites, including aloin (a mixture of the two diastereoisomers, aloin A and aloin B), aloesin, isoaloeresin D, and aloenin A. The presence of these metabolites varies considerably depending on the plant's growth conditions, including the used growing substrate. In recent years, there has been growing interest in using biochar for potted plants cultivation. However, there is currently no available information regarding the suitability of biochar for the containerized cultivation of A. arborescens. A pot experiment was conducted with the hypothesis that biochar could influence the growth and phytochemistry of A. arborescens. The growing medium was supplied with increasing proportions of biochar (1: 100 % commercial substrate; 2: mixed 50 % (v/v) substrate; 3: 100 % conifers wood biochar). Over the course of three years, the plants were closely monitored, and several key growth parameters were measured, including plant height, stem diameter, number and weight of leaves, and the number of suckers. After the first year, the content of selected active metabolites was assessed. This evaluation also involved a comparison of the respective levels in the leaves taken from the apical, median, and basal sections of the stem. The leaves collected from the median section of plants were found to be larger and exhibited the highest percentage of spikes, epidermis, and gel on fresh weight. As a general trend, it was observed that in plants cultivated within the highest amount of biochar, the leaves collected from the intermediate stem portion contained the highest quantity of secondary metabolites. [ABSTRACT FROM AUTHOR]

Hydrogels have been widely used in various biomedical applications, including skin regeneration and tissue repair. However, the capability of certain hydrogels to absorb exudate or blood from surrounding wounds, coupled with the challenge in their long-term storage to prevent bacterial growth, can pose limitations to their efficacy in biological applications. To address these challenges, the development of a multifunctional aloin-arginine-alginate (short for 3A) bio-patch capable of transforming into a hydrogel upon absorbing exudate or blood from neighboring wounds for cutaneous regeneration is proposed. The 3A bio-patch exhibits outstanding features, including an excellent porous structure, swelling properties, and biodegradability. These characteristics allow for the rapid absorption of wound exudates and subsequent transformation into a hydrogel that is suitable for treating skin wounds. Furthermore, the 3A bio-patch exhibits remarkable antibacterial and anti-inflammatory properties, leading to accelerated wound healing and scarless repair in vivo. This study presents a novel approach to the development of cutaneous wound dressing materials.

Background: Aloin, as a bioactive compound, has a variety of pharmacological functions, but its effects on combined allergic rhinitis and asthma syndrome (CARAS) have not been studied. To clarify the protective effect and mechanism of aloin in the treatment of CARAS by network pharmacology, molecular dynamics simulation and experiment. Methods: The targets of aloin, allergic rhinitis and asthma were obtained from various databases. The protein interaction network was constructed for the common targets, and molecular docking and molecular dynamics simulations were performed for the core targets. Functional and pathway enrichment analysis of common targets was also performed using R software. Varieties of biological experiments were conducted to verify the effect of aloin on the inflammatory changes of CARAS and its regulatory mechanism. Results: A total of 42 anti-allergic rhinitis and 58 anti-asthma targets were obtained, and 5 core anti-allergic rhinitis and 6 core anti-asthma targets were identified using topological analysis. GO and KEGG analyses showed that endopeptidase activity and MAPK signaling pathway played important roles in allergic rhinitis and asthma. Molecular docking and molecular dynamics simulations showed that aloin could stably bind to the core target proteins. Experimental verification showed that aloin significantly inhibited the expression of inflammatory factors, and may regulate CARAS by downregulating MAPK signaling related proteins. Conclusion: This study identified the protective effect, potential target and mechanism of aloin on CARAS. It provides reference for understanding the molecular mechanism and clinical application of aloin in the ameliorates of CARAS. [ABSTRACT FROM AUTHOR]

Aloe vera (L.) Burm.f. is an important medicinal plant which belonging to the Liliaceae family. This plant has widely been applied in the pharmaceutical, food, and cosmetic industries. In this study, Aloin was extracted from A. vera leaves using ultrasonic and stirring methods. The extract was purified, and their Aloin A and B percentages were determined using HPLC. According to the results, in all samples, the amount of Aloin B was significantly higher than Aloin A. The ethyl acetate extract of dried latex obtained by ultrasonic method had the highest yield (24.50 %) and amount of total Aloin (84.22%) compared to other samples and methods. Also, the relative percentages of Aloin B and A were 86.48 and 13.52%, respectively. Finally, the antioxidant and cytotoxic properties of Aloin-containing extracts were investigated by DPPH and MTT methods, respectively. According to the results, the ethyl acetate extract of dried latex obtained by ultrasonic method exhibited the highest antioxidant and cytotoxic activities. There was a significant correlation between extracts containing more Aloin and higher biological activity, and extracts with more Aloin had higher biological properties. Therefore, the extract of the dried latex obtained by ultrasonic method was the best sample in terms of the amount of Aloin and biological properties. In conclusion, using the ultrasonic method together with a dried sample provides the most Aloin and biological properties. [ABSTRACT FROM AUTHOR]

ABSTRACTExcessive glutamate can cause oxidative stress in neuronal cells and this can significantly contribute to the etiology of neurodegenerative disease. The present study mainly aims to investigate that aloe extract (AE) and fermented aloe extract (FAE) could protect against glutamate-induced cytotoxicity by modulating oxidative stress. In this study, both AE and FAE showed potent neuroprotective activity by inhibiting ROS and Ca2+ concentration, increasing mitochondria membrane potential, and activating glutathione-related enzymes against glutamate-insulted neurotoxicity in HT22 cells. In addition, the neuroprotective activity of FAE was more potent than that of AE. HPLC analysis reveals that the chemical composition of FAE is different from that of AE. Especially, the contents of aloin A, aloin B and aloenin were higher in FAE than in AE. In conclusion, this study indicates that both AE and FAE may have effective neuroprotective activity in glutamate-insulted pathological conditions such as Alzheimer’s disease by managing oxidative stress.

Background: Recent studies conducted by us indicate that aloin (ALO) could promote gastric cancer (GC) cell apoptosis, but the underlying mechanism remains unclear. The high mobility group box 1 (HMGB1) has been reported to regulate the apoptosis, proliferation, and migration of several cancer types. Bioinformatics analysis suggests a possible targeted regulatory relationship between miR5683 and HMGB1. Purpose: Herein, we aimed to investigate the possible role of the miR-5683/HMGB1 axis in ALO-induced GC cell apoptosis. Methods: The expression levels of miR-5683 and HMGB1 in GC tissue and adjacent normal tissue were investigated using bioinformatics analysis, and their expressions at the cellular levels were determined using reverse transcription quantitative real-time polymerase chain reaction and western blotting (WB) assays. The interaction between miR-5683 and HMGB1 was predicted in the TargetScan database and verified by a dual-luciferase assay. Cell viability and apoptosis were assessed by the cell counting kit 8 (CCK-8) assay, 4′,6-diamidino-2-phenylindole (DAPI) staining, and flow cytometry. WB was used to examine the expression levels of apoptosis-related proteins and HMGB1. Results: Our data showed that ALO promoted GC cell apoptosis, downregulated HMGB1, upregulated miR-5683 expression, and dual-luciferase assay confirmed the interaction between HMGB1 and miR-5683. Moreover, miR-5683 mimics enhanced ALO-induced GC cell apoptosis and the inhibitory effects of ALO on the levels of HMGB1. However, miR-5683 inhibitors showed the opposite effects. Conclusion: Our data suggested that ALO promotes GC cell apoptosis through the miR-5683/HMGB1 axis. [ABSTRACT FROM AUTHOR]

Breast cancer is the most commonly diagnosed cancer and is one of the leading causes of cancer mortality in women worldwide. Natural product compounds have attracted significant attention for their potent effects against human cancers. Aloin, a natural phytochemical anthraquinone glycoside extracted from Aloe sp., has been previously reported for its antitumor activity. Autophagy is a highly conserved process that mediates the degradation of dysfunctional cellular components, such as senescent proteins and organelles. In the present study, we verified the involvement of autophagy in tolerance to aloin, especially in breast cancer cells with negative estrogen receptors, and as an alternative pathway to promote cell death in cells expressing mutant p53 status, which often limits the efficacy and accounts for resistance to chemotherapy. We studied the effect of aloin on 2 types of breast cancer cell lines, estrogen receptor-positive (T47D) and triple negative (MDA-MB231), and compared to an anthraquinone analog, doxorubicin (Dox) as a reference compound. Aloin inhibited the cell growth of both T47D and MDA-MB231 cancer cells, in a time- and dose-dependent manner with a more pronounced effect in the 72 h exposure regimen, and in the ERα+ breast cell line. The autophagic activity of aloin was emphasized by the formation of autophagosomes and autolysophagosomes, as early and late autophagic compartments, respectively, as well as the accumulation of acidic vesicular organelles in the tumor cells. Also, upregulation in the protein expression of some marker genes of autophagy such as beclin 1 and LC3BII/LC3I, and conversely down-regulation in p-mTOR and p62 was recorded. The results suggest that autophagy can be regarded as one of the mechanistic modes of aloin cytotoxicity in breast cancer cells that evade apoptosis through genetic mutations in p53. [ABSTRACT FROM AUTHOR]

Aloe vera plant is known worldwide for its medicinal properties and application in gel-based products such as shampoo, soap, and sunscreen. However, the demand for these gel-based products has led to a surplus production of Aloe vera processing waste. An Aloe vera gel processing facility could generate up to 4000 kg of Aloe vera waste per month. Currently the Aloe vera waste is being disposed to the landfill or used as fertilizer. A sustainable management system for the Aloe vera processing waste should be considered, due to the negative societal and environmental impacts of the currents waste disposal methods. Therefore, this review focuses on various approaches that can be used to valorize Aloe vera waste into value-added products, such as animal and aquaculture feeds, biosorbents, biofuel and natural polymers. Researchers have reported Aloe vera waste for environmental applications biosorbents used for wastewater treatment of various pollutants. Several studies have also reported on the valorization of Aloe vera waste for production of biofuels such as bioethanol, mixed alcohol fuels, biogas and syngas. Aloe vera waste could also be valorized through isolation and synthesis of natural polymers for application in wound dressing, tissue engineering and drug delivery systems. Aloe vera waste valorization was also reviewed through extraction of value-added bioactive compounds such as aloe-emodin, aloin and aloeresin. These value-added bioactive compounds have various applications in the cosmetics (non-steroidal anti-inflammatory, tyrosinase inhibitors) and pharmaceutical (anticancer agent and COVID 19 inhibitors) industry. [ABSTRACT FROM AUTHOR]

The effect of aloin on mucosal immune response and disease resistance was elucidated in Labeo rohita infected with the bacterial fish pathogen, Aeromonas hydrophila. Fishes were divided into four groups: (i) control, (ii) vehicle control, (iii) bacteria infected and (iv) bacteria infected and aloin treated. Fish were intraperitoneally injected with A. hydrophila suspension at the dose of 2 × 106 CFU/fish at 0 day (d). Following bacterial injection at 0 d, fish were treated with aloin at a dose of 1 mg/kg body weight intraperitoneally at an interval of 24 h for 4 consecutive days. Mucus collected from fish of each group was analyzed at 2 d, 4 d, 6 d, 8 d and 10 d. In bacteria-infected fish, a significant decrease (P < 0.05) in the activity of certain enzymatic and non-enzymatic immune parameters was observed. The activity of these immune parameters showed a gradual recovery on administration of aloin in bacteria-infected fish. Cumulative mortality was also found to be low in the aloin-treated group as compared to that in the infected group. Thus, aloin could act as an immunostimulant and play a protective role against disease caused by bacteria. [ABSTRACT FROM AUTHOR]

Jia Gao,1,&ast; Sifu Yang,2,&ast; Guanqun Xie,3 Jieli Pan,4 Feiye Zhu4 1The Second Clinical Medical College, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, 310053, People’s Republic of China; 2Medical Oncology Department, Zhejiang Provincial People’s Hospital, Hangzhou, Zhejiang, 310014, People’s Republic of China; 3College of Basic Medical Science, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, 310053, People’s Republic of China; 4Academy of Chinese Medical Sciences, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, 310053, People’s Republic of China&ast;These authors contributed equally to this workCorrespondence: Jieli Pan; Feiye Zhu, Academy of Chinese Medical Sciences, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, 310053, People’s Republic of China, Email panjieli_zj@163.com; zhufeiye@163.comPurpose: This study was designed to evaluate the pharmacological mechanisms of Aloin against gastric cancer (GC) via network pharmacology analysis combined with experimental verification.Methods: Using network pharmacology methods, the potential targets of Aloin and targets related to GC were screened from public databases. The protein–protein interaction (PPI) network, Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis were performed to predict the core targets and pathways of Aloin against GC. The expressions of major targets predicted by network pharmacology in normal stomach tissues and GC tissues and their relationships with overall survival of GC were searched in GEPIA, HPA and DriverDBv3 database. The results of network pharmacology analysis were verified by in vitro experiments.Results: A total of 129 potential targets were retrieved by searching the intersection of Aloin and GC targets. PPI network analysis indicated that 10 targets, including AKT1 and CASP3, were hub genes. GO enrichment analysis involved 93 biological processes, 19 cellular components, and 37 molecular functions. KEGG enrichment analysis indicated that the anti-cancer effect of Aloin was mediated through multiple pathways, such as PI3K-AKT, FoxO and Ras signaling pathway. Among them, the PI3K-AKT signaling pathway, which contained the largest number of enriched genes, may play a greater role in the treatment of GC. The validation of key targets in GEPIA, HPA and DriverDBv3 database showed that the verification results for most core genes were consistent with this study. Then, the results of in vitro experiment indicated that Aloin could inhibit proliferation of NCI-N87 cells and induce cell apoptosis. The results also showed that Aloin could decrease the mRNA and protein expressions of PI3K and AKT, suggesting that Aloin can treat GC by inducing cell apoptosis and regulating the PI3K-AKT signaling pathway.Conclusion: This study identified the potential targets of Aloin against GC using network pharmacology and in vitro verification, which provided a new understanding of the pharmacological mechanisms of Aloin in treatment of GC.Keywords: gastric cancer, Aloin, pharmacological mechanisms, network pharmacology, experimental verification

The anti-diabetic effect of aloin was examined in vivo in the current study, similar to the study, which for four weeks examined how aloin affected the blood sugar, insulin, and antioxidant levels in both healthy and diabetic rats generated by streptozotocin. Adult male albino rats were experimentally given a single intraperitoneal injection of 60 mg/kg of streptozotocin to induced diabetes. The in vitro experiment utilized blood samples, and adult male albino rats' kidneys, pancreas and liver were separated. In comparison to control diabetic rats, aloin isolates (30 mg / kg) body weight for 30 days considerably decreased serum glucose and effectively boosted serum insulin levels. Liver and kidney congeners of malondialdehyde (MDA) were substantially decreased while, Catalase (CAT), superoxide dismutase (SOD) and Congeners Glutathione (GSH) were significantly boosted as contrasted to diabetic rats after aloin therapy. Moreover, a histological assessment of the pancreas was performed.These results show the promise of aloin at a dose of 30 mg/kg body weight for 30 days as an antidiabetic and antioxidant agent.

Background: Aloe ferox is an indigenous medicinal plant that is widely used for its various medicinal and pharmacological properties. Despite the medicinal importance and various applications of the species, it is surprising that little is known about the extent of geographical differences in its major chemical compounds. Also, the correlation between different geographic regions and variations in plant phytochemicals has received less attention. Aim: This study sought to investigate the presence of biologically active compounds in the leaf extracts of A. ferox from different geographical regions across South Africa. Setting: This study was set in different regions within South Africa. Methods: Phytochemical screening was performed qualitatively using established standard procedures involving chemical reagents such as hexane, chloroform and methanol and a series of reactions to determine the presence of phytocompounds of biological importance. Results: The study revealed that A. ferox leaves possess several classes of phytocompounds such as alkaloids, tannins, terpenoids, glycosides, phenolics, flavonoids, saponins and fixed oils and fats across various samples. Mucilage was absent across the samples. Conclusion: The study revealed eight classes of phytochemical compounds present on A. ferox leaves in three different geographic regions, which is consistent with the previous studies; however, further research is needed to enhance the study through qualitative research, gas chromatography–mass spectrometry and high-performance liquid chromatography analyses to validate phytochemical variations and their therapeutic effects. Contribution: This study contributes to the existing knowledge of the therapeutic Aloe genus.

As the feed-plant, Aloe barbadensis can enhance the immunity, prevent diseases, improve the animal survival rate and reproductive performance. Aloe barbadensis is rich in sugar compounds, quinones and flavonoids, and its main functional components are Aloe barbadensis polysaccharide, aloin, aloe emodin, aloesin, which have anti-microbial, anti inflammatory, antioxidant and immunomodulatory effects. The article reviews the various active components, biological functions and application of Aloe barbadensis in animal production, to provide reference for the rational application of Aloe barbadensis in animal production. [ABSTRACT FROM AUTHOR]

Box-behnken design-response surface method (BBD) was used to optimize the extraction conditions of aloin from aloe vera skin by ultrasonic alcohol extraction in order to improve the yield of aloin. The stability of aloin was preliminarily analyzed by single factor test. Extraction time, ultrasonic power, solid-liquid ratio and ethanol concentration were used as the single factors affecting the extraction of aloin. A response surface data model with four factors and three levels was established. The optimal extraction rate was obtained as follows: extraction time of 10 min, power of 700W, liquid-solid ratio of 1:50(g/mL), ethanol concentration 64%, the yield of aloin was 7.215 mg/g. According to the preliminary stability study, the related products are suitable to be stored at low temperature and protected from light. If they are in solution state, in ascorbic acid or citric acid need to be added (pH=5). [ABSTRACT FROM AUTHOR]

Excessive glutamate can cause oxidative stress in neuronal cells and this can significantly contribute to the etiology of neurodegenerative disease. The present study mainly aims to investigate that aloe extract (AE) and fermented aloe extract (FAE) could protect against glutamate-induced cytotoxicity by modulating oxidative stress. In this study, both AE and FAE showed potent neuroprotective activity by inhibiting ROS and Ca2+ concentration, increasing mitochondria membrane potential, and activating glutathione-related enzymes against glutamate-insulted neurotoxicity in HT22 cells. In addition, the neuroprotective activity of FAE was more potent than that of AE. HPLC analysis reveals that the chemical composition of FAE is different from that of AE. Especially, the contents of aloin A, aloin B and aloenin were higher in FAE than in AE. In conclusion, this study indicates that both AE and FAE may have effective neuroprotective activity in glutamate-insulted pathological conditions such as Alzheimer's disease by managing oxidative stress. [ABSTRACT FROM AUTHOR]

Aloe vera (L.) Burm.f. is a traditional Chinese medicine known for treating various ailments, including fungal infections. Aloin is one of the major components from A. vera, but its antifungal mechanism and therapeutic potential against oral candidiasis are not clear. This study aimed to examine the mechanism of aloin against Candida albicans and its inhibitory activity against oral candidiasis. In this study, we for the first time found that aloin could induce the formation of abnormal hyphae with smaller hyphal diameters and fewer branching points in C. albicans including 11 clinical isolates without growth inhibition. The transcriptome and further cell wall contents analysis indicated that aloin remodeled the cell wall to increase the contents of β-1,3-glucan and furtherly showed an antagonistic effect with micafungin. Aloin also significantly inhibited the cell damage of oral epithelial cells and oral candidiasis in mice infected by C. albicans due to its inhibitory actions on the hyphal development and expressions of virulence factors, including candidalysin (coded by ECE1). Our results suggest that aloin is a promising antifungal agent for controlling candidiasis and targeting hyphal development and pathogenesis represents a practical strategy for developing new antifungal drugs. KEY POINTS: • Aloin remodels the C. albicans cell wall to form avirulent hyphae. • Aloin inhibits C. albicans infections in oral epithelial cells and mouse mucosa without toxicity. • Aloin is a promising antifungal agent with therapeutic potential against C. albicans infections., Competing Interests: Declarations. Ethics approval: All animal experiments were conducted in strict accordance with ethical guidelines and were approved by the Ethics Committee of Sichuan University (WCHSIRB-D-2020–227). The research adhered to ethical standards for animal welfare. Conflict of interest: The authors declare no competing interests., (© 2025. The Author(s).)

This research aimed to investigate the antidiabetic activity, underlying mechanisms, and gut microbiota regulation of aloin. The insulin-resistant HepG2 (IR-HepG2) cell model and the type 2 diabetic (T2D) mouse model were successfully established using dexamethasone and a high-fat high-sucrose diet with low-dose streptozotocin, respectively. Aloin intervention increased glucose consumption and stimulated the activity of hexokinase and pyruvate dehydrogenase in IR-HepG2 cells. Additionally, it diminished the weight loss, reduced fasting blood glucose levels and hemoglobin A1c activity, and promoted glucose tolerance and fasting serum insulin activity in T2D mice. Histopathological analysis of the liver indicated hepatic protection by aloin. Additionally, aloin treatment inhibited the protein expression of c-Jun N-terminal kinases and activated that of IRS1/PI3K/Akt in the liver. Moreover, aloin modulated the bacterial community in the gut by raising the abundance of Bacteroidota and reducing the richness of Firmicutes, Proteobacteria, and Actinobacteriota. Thus, aloin ameliorated IR via activating IRS1/PI3K/Akt signaling pathway and regulating the gut microbiota, and it may be promising candidate as functional food for diabetic therapy.

In the present work, a two-dimensional qNMR method for the determination of sennosides was established. Using band-selective HSQC and the cross correlations of the characteristic 10–10' bonds, we quantified the total amount of the value-determining dianthranoids in five minutes, thus, rendering the method not only fast, but also specific and stability indicating. The validation of the method revealed excellent accuracy (recovery rates of 98.5 to 103%), precision (RSD values of 3.1%), and repeatability (2.2%) and demonstrated the potential of 2D qNMR in the quality control of medicinal plants. In a second method, the use of 2D qNMR for the single analysis of sennosides A, B, and A1 was evaluated with acceptable measurement times (31 min), accuracy (93.8%), and repeatability (5.4% and 5.6%) for the two major purgatives sennoside A and B. However, the precision for sennoside B and A1 was not satisfactory, mainly due to the low resolution of the HSQC signals of the two compounds. [ABSTRACT FROM AUTHOR]

Aloin is the main anthraquinone glycoside from Aloe species. Here, the anti-inflammatory functions of aloin against lipopolysaccharide (LPS)-induced vascular inflammatory responses were tested in endothelial cells or mice such as permeability, expressions of cell adhesion molecule (CAM), migration of leukocytes and lethality. Aloin was found to inhibit LPS-induced barrier disruption, CAM expression, and neutrophil adhesion/transendothelial migration to endothelial cells. Furthermore, aloin inhibited LPS-induced hyperpermeability, leukocyte migration, lethality in vivo. These results suggest that aloin has anti-inflammatory activities against LPS, thereby supporting its usefulness as a treatment for vascular inflammatory. [ABSTRACT FROM AUTHOR]

Aloe-vera extracted anthraquinones (aloin, aloe-emodin, rhein) possess a wide range of biological activities, have poor solubility and are sensitive to processing conditions. This work investigated the ultrasound-assisted encapsulation of these extracted anthraquinones (AQ) into casein micelles (CM). The particle size and zeta potential of casein micelles loaded with aloin (CMA), aloe-emodin (CMAE), rhein (CMR) and anthraquinone powder (CMAQ) ranged between 171–179 nm and −23 to −17 mV. The AQ powder had the maximum encapsulation efficiency (EE%) (aloin 99%, aloe-emodin 98% and rhein 100%) and encapsulation yield, while the whole leaf Aloe vera gel (WLAG) had the least encapsulation efficiency. Spray-dried powder (SDP) and freeze-dried powder (FDP) of Aloe vera showed a significant increase in size and zeta potential related to superficial coating instead of encapsulation. The significant variability in size, zeta potential and EE% were related to anthraquinone type, its binding affinity, and its ratio to CM. FTIR spectra confirmed that the structure of the casein micelle remained unchanged with the binding of anthraquinones except in casein micelles loaded with whole-leaf aloe vera gel (CMWLAG), where the structure was deformed. Based on our findings, Aloe vera extracted anthraquinones powder (AQ) possessed the best encapsulation efficiency within casein micelles without affecting its structure. Overall, this study provides new insights into developing new product formulations through better utilization of exceptional properties of casein micelles. [ABSTRACT FROM AUTHOR]

Abstract Background Osteosarcoma is a malignant tumor of bone and soft tissue in adolescents. Due to its tumor biological behavior pattern, osteosarcoma usually generates poor prognosis. Autophagy is an important self-defense mechanism in osteosarcoma. Methods Cell viability in IC50 testing and reverse assays was examined by the MTT assay. Cell apoptosis conditions were examined by flow cytometry, Hoechst 33,342 staining and apoptosis-related protein immunoblotting. Autophagy conditions were tested by autophagy-related protein immunoblotting, transmission electron microscopic observation and dual fluorescence autophagy flux detection. The possible targets of aloin were screened out by network pharmacology and bioinformatic methods. Osteosarcoma xenografts in nude BALB/c mice were the model for in vivo research on tumor suppression, autophagy induction, pathway signaling and toxicity tests. In vivo bioluminescence imaging systems, immunohistochemical assays, and gross tumor volume comparisons were applied as the main research methods in vivo. Results Aloin induced osteosarcoma apoptosis in a dose-dependent manner. Its possible effects on the PI3K/AKT pathway were screened out by network pharmacology methods. Aloin increased autophagic flux in osteosarcoma by downregulating the PI3K/AKT pathway. Aloin promoted autophagic flux in the osteosarcoma cell lines HOS and MG63 in a dose-dependent manner by promoting autophagosome formation. Chloroquine reversed the apoptosis-promoting and autophagy-enhancing effects of aloin. Autophagy induced by starvation and rapamycin significantly enhanced the autophagic flux and apoptosis induced by aloin, which verified the role of the PI3K/AKT axis in the pharmacological action of aloin. Therapeutic effects, autophagy enhancement and regulatory effects on the PI3K/AKT/mTOR pathway were demonstrated in a nude mouse xenogeneic osteosarcoma transplantation model. Conclusions Aloin inhibited the proliferation of osteosarcoma by inhibiting the PI3K/AKT/mTOR pathway, increasing autophagic flux and promoting the apoptosis of osteosarcoma cells.

• First study on Alo + TIE combination for CLP-induced sepsis in mice. • Alo + TIE combination boosts survival from 10 % to 75 % in 72 h. • Combination therapy suppresses IL-6, IL-1β, TNF-α, mitigates tissue damage. • Combination therapy lowers NK, CD8 + T, CD4 + T cells, boosts macrophages. • Combination therapy altered the peritoneal cavity microbiota composition, reducing pathogens. Despite the high mortality rate, sepsis lacks specific and effective treatment options. Conventional antibiotics, such as TIENAM (TIE; imipenem and cilastatin sodium for injection), face challenges owing to the emergence of bacterial resistance, which reduces their effectiveness and causes adverse effects. Addressing resistance and judicious drug use is crucial. Our research revealed that aloin (Alo) significantly boosts survival rates and reduces inflammation and bacterial load in mice with sepsis, demonstrating strong antimicrobial activity. Using a synergistic Alo + TIE regimen in a cecal ligation and puncture (CLP)-induced sepsis model, we observed a remarkable increase in survival rates from 10 % to 75 % within 72 h compared with the CLP group alone. This combination therapy also modulated inflammatory markers interleukin (IL)-6, IL-1β, and tumor necrosis factor (TNF)-α, mitigated tissue damage, regulated immune cells by lowering NK, activated CD8+ and CD4+ T cells while increasing peritoneal macrophages, and decreased the bacterial load in the peritoneal cavity. We noted a significant shift in the abdominal cavity microbiota composition post-treatment, with a decrease in harmful bacteria, such as Lachnospiraceae_NK4A136_group , Klebsiella , Bacillus , and Escherichia , and an increase in beneficial bacteria, such as Lactobacillus and Mucispirillum. Our study emphasizes the efficacy of combining Alo with TIE to combat sepsis, and paves the way for further investigations and potential clinical applications aiming to overcome the limitations of TIE and enhance the therapeutic prospects of Alo. [ABSTRACT FROM AUTHOR]

• The pharmacological importance of the west African aloe species was appraised. • Aloe species have therapeutic benefits such as antioxidants, antidiabetic and anticancer. • The west African aloe species are underutilized but can be harnessed as medicines. • Modern technologies are needed to decipher their detailed chemical entities. The genus Aloe belongs to the family Xanthorrhoeaceae with over 560 species ranging from small shrub-like plants to large trees. Despite their pharmacological applications against ailments such as arthritis, cancer, type 2 diabetes mellitus, digestive disorders, cancer, microbial infections, and skin diseases, only Aloe vera, Aloe ferox, Aloe perryi , and Aloe arborecens have received superior research attention over the years with some members of the genus such as Aloe buettneri, Aloe macrocarpa , and Aloe schweinfurthii being either neglected or underutilized. Here, we reviewed the ethnobotanical, phytochemistry, toxicological and pharmacological importance of the three indigenous and underutilized West African Aloe species- A. buettneri, A. macrocarpa , and A. schweinfurthii. Scientific databases such as Google Scholar, PubMed, JSTOR, Science Direct, and Scopus were used in retrieving the data presented in this study. The information gathered revealed that, the three species are generally underutilized with some ethnopharmacological uses against dysmenorrhea, skin diseases, female infertility, chronic gonorrhea, facilitation of childbirth, hemorrhoids, and impotency in men, being documented. Majorly, their leaves and gel are rich in alkaloids, phenolics, sterols, saponins, glycosides, anthraquinones, and anthraquinoic derivatives and the species exhibited a broad spectrum of biological activities including antidiabetic, aphrodisiac, anti-ulcer, anti-inflammatory, antimicrobial, antioxidant, analgesia, antipyretic, antileishmanial, and antimalarial. Despite their numerous therapeutic applications, Aloe species generally potentiate toxicological concerns at high doses, necessitating further research to standardize and establish their optimum therapeutic doses including those of the West African species. Furthermore, while the medicinal uses of Aloe species have been well documented in Africa, there is still paucity of information on the pharmacological and phytochemistry of the West African species. Therefore, further advanced and in-depth investigations are imperative to isolate and characterize their active compounds, as well as to understand the molecular mechanism of action of the species against human ailments with the hope of developing commercially valuable products of high economic importance. [ABSTRACT FROM AUTHOR]

Aloe vera (Aloe barbadensis Miller) is a perennial drought tolerant medicinal species. This research study investigates the influence of biofertilizers on mycorrhizal fungi colonization, leaf number and width, plant height, offset number, leaf relative elongation rate (RER), leaf dry weight and leaf gel weight, water productivity (WP) for the gel, and aloin content in Aloe vera plants. The experiments were carried out in the warm and dry climate of Bushehr Province, Iran during 2016–2018. Treatments are reported to include irrigation regimes and biofertilizers at four levels. In terms of irrigation regimes, 25%, 50%, 75%, and 100% of water requirement accompanied the following treatments for biofertilizers, phosphorus-solubilizing bacteria (PSB), mycorrhizal fungi (MF), PSB+MF , and control (without any biofertilizers). The PSB includes Pseudomonas putida strain P 13 and Pantoea agglomerans strain P 5, in addition to Glomus mosseae as MF. The biofertilizer benefits (remarkably PSB+MF) on investigated traits were observed in three harvests. The results confirm the positive impacts of biofertilizers on important traits such as offset number (an economical part of Aloe vera planting), water productivity with less water consumption, and root colonization, which is the main reason of increasing the mentioned traits. Considering the minimal difference between 100%, 75% and 50% of water requirement in terms of gel fresh weight and more aloin content in 50% of our experiments, Aloe vera is reported as a high drought tolerant plant which merely requires an acceptable gel yield and aloin content. Moreover, better water productivity and consumption is possible in warm and arid regions by applying 50% of Aloe vera water requirement as well as biofertilizers. [Display omitted] [ABSTRACT FROM AUTHOR]

The genus Aloe (family: Xanthorrhoeaceae) encompasses 490 shrubby-succulent-perennial species which are native to Africa. Among these, Aloe vera has grabbed the limelight in the arena of herbal medicine due to the presence of unique phytochemicals such as Aloin A and B, Homonataloin, Aloe emodin, acemannan etc. in its latex. Moreover, its leaf extract contains 99% water, and 75 active compounds including vitamins (A, B1, B2, B3, B6, B9, B12, C, and E), minerals (Zn, Se, Na, Mn, Mg, K, Cu, Cr, Ca), amino acids, and enzymes (peroxidase, lipase, cellulase, catalase, carboxypeptidase, bradykinase, amylase, alkaline phosphatase). Thus, Aloe vera is revered as a 'wonder plant' as it possesses multiple pharmaceutical properties such as anti-oxidant, anti-inflammatory, anti-tumor, anti-fungal, anti-diabetic, anti-ulcer, anti-hypertensive and its juice helps to cure gastrointestinal disorders, and dermal diseases, it also strengthens the immune system. Being a xerophyte, Aloe vera is commercially cultivated in many countries which include South Africa, America, Australia, India etc. The Aloe gel, is meticulously extracted, processed and stabilized before using it in preparation of various health care products. This review focuses on the explicit information on origin, botanical description, phytochemistry, nutritional and medicinal benefits, with special emphasis on value-added products of Aloe vera. The review revealed 46 value-added Aloe-products that are being manufactured by different companies worldwide. Thus, sustainable Aloe-cultivation must be ensured to meet the rising global demands for Aloe vera gel and allied products. [ABSTRACT FROM AUTHOR]

Aloe products are increasingly valued as ingredients in food supplements and as flavoring agents. The global Aloe vera market is varied, large, growing, and increasingly important in food, cosmetics, and medicines. Aloin, an anthraquinone glycoside, is one of the major components by weight of the anthraquinone derivatives of Aloe vera gel. Principal metabolites, aloe emodin and emodin, are a source of debate concerning toxic vs salutary effects, hence the accurate toxicological characterization of these compounds has become increasingly important. The purpose of this study was to determine the genotoxic profile of a stabilized Aloe vera juice product derived from the inner filet and marketed as a beverage currently sold in the European Union containing 8 to 10 ppm aloin and a mixture of purified aloin A and B. The present data confirm that a commercial stabilized Aloe vera gel intended for consumption as a juice beverage is not genotoxic. Furthermore, both aloin A and B were negative in the same assays and therefore are also not genotoxic. These results are consistent with the work of other groups and contrast with data obtained using products containing the Aloe vera latex hydroxyanthracene derivatives (HADs). [ABSTRACT FROM AUTHOR]

The present study explored the stability of extracted anthraquinones (aloin, aloe-emodin and rhein) from whole-leaf Aloe vera gel (WLAG), its freeze-dried powder (FDP) and spray-dried powder (SDP) under varying pH and temperature conditions during storage. Each anthraquinone behaved differently under different processing parameters. The amount of anthraquinones present in the gel was higher than in FDP and SDP. The aloin contents decreased by more than 50% at 50 °C and 70 °C, while at 25 °C and 4 °C, the decrease was moderate. A substantial reduction in aloin concentration was noticed at pH 6.7, whereas it remained unaffected at pH 3.5. The temperature and pH had no significant effect on the stability of aloe-emodin. Interestingly, a small quantity of rhein was detected during storage due to the oxidative degradation of aloin into aloe-emodin and rhein. These findings can provide significant insight into retaining anthraquinones during processing while developing functional foods and nutraceuticals to obtain maximum health benefits. [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of aloin against chronic constriction injury (CCI)-induced neuropathic pain in rats. Methods: Rats were randomly divided into 7 groups: Group I (normal control), Group II (sham-operated), Group III (CCI control) and Group IV, V, VI, and VII, which underwent CCI surgery and then were administered with aloin (5 mg/kg, p.o.; 25 mg/kg, p.o.; 125 mg/kg, p.o.) and gabapentin (50 mg/kg, p.o.), respectively for 14 days. Peripheral neuropathy was induced by silk ligatures (4-0) loosely placed around the sciatic nerve. Nociceptive thresholds against mechanical stimuli (Von-Frey filaments) and thermal stimuli (12 °C and 40 °C) were measured at mid-plantar paw region ipsilateral to the compressed nerve on day-3, 7, 11, and 14. The concentration of cytokines including tumor necrosis factor-α (TNF-α), interleukin-6, and interleukin-1β was estimated at day-7. At day 14, motor nerve conduction velocity was determined under urethane anesthesia (1.25 g/kg). Oxidative stress parameters (malondiadehyde, glutathione, catalase, and superoxide dismutase) were estimated in sciatic nerve homogenates at day 14. Representative nerve samples were processed for histological investigations. Results: Aloin significantly reduced CCI-induced mechanical and thermal allodynia. It also improved motor nerve conduction velocity and decreased oxidative stress in nerve tissues. In addition, it decreased pro-inflammatory cytokine levels and restored the histoarchitecture of compressed sciatic nerve. Conclusions: Aloin mitigates CCI-induced neuropathic pain in rats by inhibiting oxidative stress and pro-inflammatory cytokines in the afflicted sciatic nerve.

Plants contain underutilized resources of compounds that can be employed to combat viral diseases. Aloe vera (L.) Burm. f. (syn. Aloe barbadensis Mill.) has a long history of use in traditional medicine, and A. vera extracts have been reported to possess a huge breadth of pharmacological activities. Here, we discuss the potential of A. vera compounds as antivirals and immunomodulators for the treatment of viral diseases. In particular, we highlight the use of aloe emodin and acemannan as lead compounds that should be considered for further development in the management and prevention of viral diseases. Given the immunomodulatory capacity of A. vera compounds, especially those found in Aloe gel, we also put forward the idea that these compounds should be considered as adjuvants for viral vaccines. Lastly, we present some of the current limitations to the clinical applications of compounds from Aloe, especially from A. vera. [ABSTRACT FROM AUTHOR]

The shift in food consumption pattern to accommodate an array of bioactive compounds in foods with minimum calorie intake has resulted in the development of many novel beverages in the last decade. In the present study, optimization of apricot (AP; 0–50%) blended Aloe vera (AV; 50–100%) based low-calorie beverage functionally enriched with aonla juice (AJ; 3,5,7,10%) using steviol glycoside (SG; 0–100%) was performed. The preliminary screening suggested that 40% addition of AP (AV-AP; 60:40) had an acceptable taste. While, for functional enrichment of squash, incorporation of 7% AJ with 40ºB TSS was optimized based on color, consistency, taste, and overall acceptability scores. The developed squash had higher ascorbic acid (26.83 mg/100 g), total phenols (68.77 mg/100 g), antioxidant potential (36.50%) and antimicrobial activity against Staphylococcus aureus (18.00 mm). The aloin content was recorded 0.9 ppm, well within the maximum permissible limits. Additionally, replacement of sucrose with stevioside up to 50 per cent resulted in equi-sweetness level without characteristic bitter aftertaste and a significant reduction in energy value from 142 kcal/100 g to 85.26 kcal/100 g. The developed beverage recorded a high amount of functional compounds with reduced energy values. The beverage can be a recommendation for general consumption for health- conscious people to cover their functional food desires. [ABSTRACT FROM AUTHOR]

Traumatic brain injury (TBI) is a subset of brain injury induced by external mechanical forces to the head or neck. TBI has been reported to be one of the leading causes of disability, and it causes a huge financial burden around the world. Aloin is the major anthraquinone glycoside extracted from Aloe species, and has presented anti-tumour, anti-oxidative and anti-inflammatory activities. However, few studies have focused the effect of aloin in treatment of TBI. Nicotinamide adenine dinucleotide phosphate oxidase (NOX) is the only subset of enzymes which produces solely the reactive oxygen species (ROS). A recent study showed that activation of NOX might aggravate the primary TBI, and among these members, NOX2 is the key member in regulation of uncontrolled ROS expression, and thus plays a critical role in development of inflammatory diseases. Here, we noticed that inhibition of NOX2 combined with aloin treatment promoted the recovery of brain function in a mice model as well as the viability rate in a cell model. A further study found that the inflammation response process was also inhibited after treatment. Then, we found that these effects might be mediated by the PI3K/AKT/mTOR signalling pathway and NOX2 might be a therapeutic target for TBI.

The Aloe species is known for its medicinal and cosmetic properties. Aloin is an active ingredient found in the leaves of medicinal plants of the genus Aloe. Aloin has attracted considerable interest for its antiinflammatory, anticancer, antibacterial, and antioxidant activities. However, since its clinical application is restricted by its unclear mechanism of action, a deeper understanding of its pharmacological activity is required. This review provides an overview of current pharmacological and toxicological studies published in English from February 2000 to August 2021. Herein, we summarized the sources and potential health benefits of aloin from a clinical application perspective to guide for further studies on the sources of aloin, aimed at efficiently increasing aloin production. Importantly, the function and mechanism of action of aloin remain unclarified. In future research, it is necessary to develop new approaches for studying the pharmacological molecular mechanisms underlying the activity of this compound against various diseases. [ABSTRACT FROM AUTHOR]

CircRNA/miRNA/mRNA axis has been reported to play crucial regulatory roles in multiple cancers, including hepatocellular carcinoma (HCC). In addition, recent investigations revealed that aloin exerted anti-tumor functions in HCC. However, the underlying mechanism of aloin on anti-tumor functions in HCC remained elusive. Therefore, this study aimed to investigate whether circRNA/miRNA/mRNA axis medicated the anti-tumor effect of aloin in HCC. Cell viability, invasion, apoptosis and autophagy were accessed by cell counting kit-8 (CCK-8), transwell invasion assay, flow cytometry, Western blot and immunofluorescence analysis, respectively. Expression levels of circ_0011385, miR-149-5p and WT1 mRNA were determined using qRT-PCR assay. Binding sites between miR-149-5p and circ_0011385 or WT1 were predicted in starBase database. The binding relationship among circ_0011385, miR-149-5p and WT1 were verified by dual-luciferase reporter assay and RNA immunoprecipitation. Besides, the rescue experiments were performed by co-transfection with cric_0011385 overexpression plasmid, si-cric_0011385, miR-149-5p mimic and inhibitor, WT1 pDNA and si-WT1 in HCC cells. Furthermore, tumor growth was also investigated in the xenograft mouse model. Aloin inhibited HCC proliferation and invasion as well as promoted apoptosis and autophagy both in vitro and in vivo. Besides, aloin suppressed circ_0011385 expression. Overexpressed circ_0011385 partially reversed the anti-tumor effect of aloin on HCC. In addition, it was revealed that the circ_0011385, miR-149-5p and WT1 genes were abnormally expressed in HCC. Furthermore, the binding interactions between circ_0011385, miR-149-5p and WT1 were predicted and confirmed. Moreover, the effect of circ_0011385 on the anti-tumor role of aloin in HCC was rescued by miR-149-5p mimics. MiR-149-5p regulated HCC progression via modulating WT1. Aloin suppressed cell proliferation, invasion and tumor growth and promoted apoptosis and autophagy in HCC through regulating circ_0011385/miR-149-5p/WT1 axis. Aloin may be a potential candidate drug for HCC treatment.Abbrevations: HCC: Hepatocellular carcinoma; ceRNA: competing endogenous RNA; miRNA: microRNA; MREs: miRNA response elements; WT1: Wilms' tumor 1; MMP-2: Matrix metalloproteinase; EMT: epithelial-mesenchymal transition; GADPH: glyceraldehyde 3-phosphate dehydrogenase; WT: wild type; MUT: mutant type; DMEM: dulbecco's modified eagle medium. [ABSTRACT FROM AUTHOR]

Background: Osteosarcoma is a malignant tumor of bone and soft tissue in adolescents. Due to its tumor biological behavior pattern, osteosarcoma usually generates poor prognosis. Autophagy is an important self-defense mechanism in osteosarcoma. Methods: Cell viability in IC50 testing and reverse assays was examined by the MTT assay. Cell apoptosis conditions were examined by flow cytometry, Hoechst 33,342 staining and apoptosis-related protein immunoblotting. Autophagy conditions were tested by autophagy-related protein immunoblotting, transmission electron microscopic observation and dual fluorescence autophagy flux detection. The possible targets of aloin were screened out by network pharmacology and bioinformatic methods. Osteosarcoma xenografts in nude BALB/c mice were the model for in vivo research on tumor suppression, autophagy induction, pathway signaling and toxicity tests. In vivo bioluminescence imaging systems, immunohistochemical assays, and gross tumor volume comparisons were applied as the main research methods in vivo. Results: Aloin induced osteosarcoma apoptosis in a dose-dependent manner. Its possible effects on the PI3K/AKT pathway were screened out by network pharmacology methods. Aloin increased autophagic flux in osteosarcoma by downregulating the PI3K/AKT pathway. Aloin promoted autophagic flux in the osteosarcoma cell lines HOS and MG63 in a dose-dependent manner by promoting autophagosome formation. Chloroquine reversed the apoptosis-promoting and autophagy-enhancing effects of aloin. Autophagy induced by starvation and rapamycin significantly enhanced the autophagic flux and apoptosis induced by aloin, which verified the role of the PI3K/AKT axis in the pharmacological action of aloin. Therapeutic effects, autophagy enhancement and regulatory effects on the PI3K/AKT/mTOR pathway were demonstrated in a nude mouse xenogeneic osteosarcoma transplantation model. Conclusions: Aloin inhibited the proliferation of osteosarcoma by inhibiting the PI3K/AKT/mTOR pathway, increasing autophagic flux and promoting the apoptosis of osteosarcoma cells. [ABSTRACT FROM AUTHOR]

Abstract Hepatocellular carcinoma (HCC) is a devastating and highly metastatic cancer worldwide. Metformin (MET) is the priority drug for treatment of type 2 diabetes; however, it possesses multiple biological effects like anticancer and hepatoprotective activity. Herein, we examined the effects of aloin (barbaloin) and MET as well as combination treatment in HCC cell line in vitro and in vivo. As a result, aloin and MET alone exhibited inhibitory effects on proliferation and invasion of HepG2 and Bel‐7402 cells. Specially, combination treatment of aloin and MET showed enhanced inhibitory effects in vitro. Aloin and MET alone induced apoptosis and autophagy in vitro. Similarly, aloin and MET cooperated to promote apoptosis and autophagy in HepG2 and Bel‐7402 cells. In the HepG2 xenograft models, aloin in combination with MET confine tumor growth and facilitate apoptosis and autophagy. Both the in vitro and in vivo results showed that aloin and MET alone as well as combination treatment activated the PI3K/AKT/mTOR pathway. Overall, our research demonstrated that the concomitant treatment with aloin and MET enhances the antitumor effect by inhibiting the growth and invasion as well as inducing apoptosis and autophagy in HCC through PI3K/AKT/mTOR pathway.

Ziqian Wang, 1, 2 Tuo Tang, 1, 2 Shengnan Wang, 1, 2 Tianyu Cai, 1, 2 Hong Tao, 1, 2 Qing Zhang, 1, 2 Shimei Qi, 1, 2 Zhilin Qi 1, 2 1Department of Biochemistry and Molecular Biology, Wannan Medical College, Wuhu, Anhui 241002, People’s Republic of China; 2Anhui Province Key Laboratory of Active Biological Macro-Molecules, Wannan Medical College, Wuhu, Anhui 241002, People’s Republic of ChinaCorrespondence: Zhilin QiDepartment of Biochemistry and Molecular Biology, Wannan Medical College, 22 Wenchang West Road, Wuhu, Anhui 241002, People’s Republic of ChinaEmail 422627721@qq.comBackground: Aloin has been reported to have many pharmacological effects including anti-inflammatory, anti-oxidant and anti-tumour activities. However, the precise molecular mechanisms underlying the anti-tumour properties of aloin are yet to be elucidated.Methods: HGC-27 and BGC-823 gastric cancer cells were treated with aloin. EdU and colony formation assays were used to detect the proliferation ability of cells. The migration of cells was detected using wound healing and transwell assays. Western blotting was used to detect the levels of cyclinD1, cyclin E1, MMPs, N-cadherin, E-cadherin and NOX2. The phosphorylation of Akt, mTOR, P70S6K, S6, Src, stat3 and IκBα were also detected by Western blotting. Flow cytometry was used to detect the cell cycle distribution.The location of p65 in cells was determined by using a confocal microscopy assay. The total amounts of ROS present in cells were measured using an ROS assay kit.Results: Here, we found that aloin inhibited the proliferation and migration of HGC-27 and BGC-823 gastric cancer cells using a combination of EdU, colony formation, wound healing and transwell assays. Further investigations revealed that aloin decreased the protein expression levels of cyclin D1, N-cadherin, and the matrix metalloproteinases (MMP)-2 and MMP-9; increased E-cadherin expression in a dose-dependent manner; inhibited reactive oxygen species (ROS) generation; and mediated the activation of Akt-mTOR, signal transducer and activator of transcription-3 (Stat3), and NF-κB signalling pathways. Our results also indicated that aloin is able to attenuate the expression levels of the two regulatory proteins of nicotinamide adenine dinucleotide phosphate oxidase 2 (NOX2), p47phox and p22phox, but had no effect on the level of gp91phox. N-acetylcysteine treatment of gastric cancer cells inhibited ROS production and Akt-mTOR, Stat3, and IκBα phosphorylation. Taken together, our data suggest that aloin inhibits the proliferation and migration of gastric cancer cells by downregulating NOX2–ROS-mediated activation of the Akt-mTOR, Stat3, and NF-κB signalling pathways.Conclusion: Our findings suggest a potential role for aloin in the prevention of gastric cancer cell proliferation and migration and provide novel insights into the anti-cancer properties of aloin.Keywords: aloin, gastric cancer, proliferation, migration, nicotinamide adenine dinucleotide phosphate oxidase 2, reactive oxygen species

Myocardial ischemia/reperfusion injury (I/RI) frequently incurs in acute myocardial infarction with high morbidity and mortality worldwide and is characterized with cardiomyocyte apoptosis and inflammatory response. Aloin is a major anthraquinone from Aloe species and fulfills pleiotropic protective functions in several disease models including hepatic injury. Nevertheless, the potential of aloin in MI/RI remains elusive. Intriguingly, aloin had modest cytotoxicity in H9c2 cardiomyocytes. Importantly, aloin dose-dependently ameliorated cell viability that was inhibited in response to simulated ischemia/reperfusion (SI/R) stimulation. Moreover, the enhanced apoptosis in cells under SI/R conditions were reduced after aloin treatment, concomitant with the decrease in pro-apoptotic Bax protein levels and increase in anti-apoptotic Bcl-2 protein expression. Of interest, aloin administration attenuated SI/R-induced oxidant stress by decreasing reactive oxygen species (ROS) production, lactate dehydrogenase (LDH), and malondialdehyde (MDA) release and increasing activity of anti-oxidant stress enzyme superoxide dismutase (SOD). Additionally, the elevated pro-inflammatory cytokine levels were counteracted after aloin treatment in cells under SI/R conditions, including TNF-α, IL-6, and IL-1β. Mechanically, aloin further enforced the activation of the NF-E2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) signaling. Noticeably, blockage of this pathway by si-Nrf2 transfection blunted aloin-mediated cardioprotective efficacy against SI/R-evoked oxidative stress injury and inflammatory response. Thus, these findings corroborate that aloin may antagonize SI/R-induced cardiomyocyte injury by attenuating excessive oxidative stress and inflammation, thereby endorsing its potential as a promising therapeutic agent against myocardial infarction. [ABSTRACT FROM AUTHOR]

Through ring-opening polymerization of L-lactide, aloin, a natural compound, was bonded to the polymeric chains and the molecular structures of obtained PLA-An were characterized by FT-IR and NMR. Measurements on the UV-Vis absorption and fluorescence emission spectroscopy show that PLA-An has a characteristic absorption of aloin and a large Stokes shift at the state of solution in the PL, being capable of absorbing UV light and dissipating some of UV energy. Additionally, due to chemical bonds, aloin groups aren't easy to be extracted by solvent, which allows aloin to play the role of ultraviolet absorption for a long time. [ABSTRACT FROM AUTHOR]

The present study explored the stability of extracted anthraquinones (aloin, aloe-emodin and rhein) from whole-leaf Aloe vera gel (WLAG), its freeze-dried powder (FDP) and spray-dried powder (SDP) under varying pH and temperature conditions during storage. Each anthraquinone behaved differently under different processing parameters. The amount of anthraquinones present in the gel was higher than in FDP and SDP. The aloin contents decreased by more than 50% at 50 °C and 70 °C, while at 25 °C and 4 °C, the decrease was moderate. A substantial reduction in aloin concentration was noticed at pH 6.7, whereas it remained unaffected at pH 3.5. The temperature and pH had no significant effect on the stability of aloe-emodin. Interestingly, a small quantity of rhein was detected during storage due to the oxidative degradation of aloin into aloe-emodin and rhein. These findings can provide significant insight into retaining anthraquinones during processing while developing functional foods and nutraceuticals to obtain maximum health benefits.

Objective To explore the effect of aloin on the proliferation, apoptosis and invasion of esophageal cancer KESY70 cell line. Methods Different concentrations of aloin were added into KESY70 cells which were randomly divided into five groups: untreated group (KESY70), control group (DMSO) and Aloin groups (10, 40, 80 μmol/L). CCK-8 assay was used to test the viability and proliferation of KESY70 cells. The apoptosis was detected by flow cytometry. Transwell assay was performed to analyze the invasion of KESY70 cells. The expression levels of PCNA, cleaved caspase-3 and MMP-9 were checked by Western blot. Results Cell viabilities of 40, 80 and 120 μmol/L Aloin groups were remarkably decreased, compared with DMSO group(P < 0.01). The proliferation rates of KESY70 cells treated with 40 and 80 μmol/L aloin for three days were attenuated, compared with the DMSO group (P < 0.05). Compared with DMSO group, the apoptosis rates were increased (P < 0.05), the invasion abilities were inhibited (P < 0.05), the expression levels of PCNA and MMP-9 were reduced (P < 0.05), and the expressions of cleaved caspase-3 were increased (P < 0.05) in Aloin groups. Conclusion Aloin may suppress the proliferation, invasion and induce the apoptosis of KESY70 cells.