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Introduction Surgical removal of an impacted third molar is one of the most common oral surgical procedures performed in dental offices. The postoperative phase is often associated with severe inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) are usually prescribed to manage postoperative discomfort. NSAIDs have been associated with gastrointestinal bleeding, renal function disturbances, and platelet count reductions. Thus, the present study demonstrates the utility of aescin in managing postoperative discomfort after the surgical removal of impacted mandibular third molars. This study aimed to correlate and compare the impact of aescin and diclofenac on salivary PGE2 levels and serum C-reactive protein levels after surgical extraction of the mandibular third molar. The study will also evaluate and compare the effectiveness of individual drug therapy in managing postoperative pain, swelling and mouth opening. Methods The planned study is a single-center, double-blind, randomized, parallel, prospective clinical trial. Each patient will be prescribed either diclofenac sodium 150 mg/day or aescin (escin) 120 mg/day to be taken orally in divided doses for five days after surgically removing the impacted mandibular third molar. Pain will be assessed using a visual analog scale. Facial swelling and mouth opening will be recorded using a metric scale with standardized reference points. ELISA (enzyme-linked immunosorbent assay (ELISA) will be employed to measure salivary Prostaglandin E2 and serum C–reactive protein levels. All parameters will be recorded preoperatively (T0) on the second postoperative day (T1) and fifth postoperative day (T2). Conclusion The proposed study is expected to show a clinically acceptable response to the administration of aescin for the management of postoperative discomfort compared to diclofenac sodium after third molar surgery. The proposed study is expected to positively manipulate the levels of salivary Prostaglandin E2 and serum C–reactive protein, which are reliable inflammatory markers. The outcome of this study may provide an efficacious and safe alternative to conventional nonsteroidal anti-inflammatory drugs for managing postoperative discomfort following third molar surgery.

Introduction Surgical removal of an impacted third molar is one of the most common oral surgical procedures performed in dental offices. The postoperative phase is often associated with severe inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) are usually prescribed to manage postoperative discomfort. NSAIDs have been associated with gastrointestinal bleeding, renal function disturbances, and platelet count reductions. Thus, the present study demonstrates the utility of aescin in managing postoperative discomfort after the surgical removal of impacted mandibular third molars. This study aimed to correlate and compare the impact of aescin and diclofenac on salivary PGE2 levels and serum C-reactive protein levels after surgical extraction of the mandibular third molar. The study will also evaluate and compare the effectiveness of individual drug therapy in managing postoperative pain, swelling and mouth opening. Methods The planned study is a single-center, double-blind, randomized, parallel, prospective clinical trial. Each patient will be prescribed either diclofenac sodium 150 mg/day or aescin (escin) 120 mg/day to be taken orally in divided doses for five days after surgically removing the impacted mandibular third molar. Pain will be assessed using a visual analog scale. Facial swelling and mouth opening will be recorded using a metric scale with standardized reference points. ELISA (enzyme-linked immunosorbent assay (ELISA) will be employed to measure salivary Prostaglandin E2 and serum C–reactive protein levels. All parameters will be recorded preoperatively (T0) on the second postoperative day (T1) and fifth postoperative day (T2). Conclusion The proposed study is expected to show a clinically acceptable response to the administration of aescin for the management of postoperative discomfort compared to diclofenac sodium after third molar surgery. The proposed study is expected to positively manipulate the levels of salivary Prostaglandin E2 and serum C–reactive protein, which are reliable inflammatory markers. The outcome of this study may provide an efficacious and safe alternative to conventional nonsteroidal anti-inflammatory drugs for managing postoperative discomfort following third molar surgery.

Introduction Surgical removal of an impacted third molar is one of the most common oral surgical procedures performed in dental offices. The postoperative phase is often associated with severe inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) are usually prescribed to manage postoperative discomfort. NSAIDs have been associated with gastrointestinal bleeding, renal function disturbances, and platelet count reductions. Thus, the present study demonstrates the utility of aescin in managing postoperative discomfort after the surgical removal of impacted mandibular third molars. This study aimed to correlate and compare the impact of aescin and diclofenac on salivary PGE2 levels and serum C-reactive protein levels after surgical extraction of the mandibular third molar. The study will also evaluate and compare the effectiveness of individual drug therapy in managing postoperative pain, swelling and mouth opening. Methods The planned study is a single-center, double-blind, randomized, parallel, prospective clinical trial. Each patient will be prescribed either diclofenac sodium 150 mg/day or aescin (escin) 120 mg/day to be taken orally in divided doses for five days after surgically removing the impacted mandibular third molar. Pain will be assessed using a visual analog scale. Facial swelling and mouth opening will be recorded using a metric scale with standardized reference points. ELISA (enzyme-linked immunosorbent assay (ELISA) will be employed to measure salivary Prostaglandin E2 and serum C–reactive protein levels. All parameters will be recorded preoperatively (T0) on the second postoperative day (T1) and fifth postoperative day (T2). Conclusion The proposed study is expected to show a clinically acceptable response to the administration of aescin for the management of postoperative discomfort compared to diclofenac sodium after third molar surgery. The proposed study is expected to positively manipulate the levels of salivary Prostaglandin E2 and serum C–reactive protein, which are reliable inflammatory markers. The outcome of this study may provide an efficacious and safe alternative to conventional nonsteroidal anti-inflammatory drugs for managing postoperative discomfort following third molar surgery.

Copyright of Al-Mustansiriyah Journal for Pharmaceutical Sciences is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Aesculus indica, the Indian Horse Chestnut (IHCN), is a wild tree species indigenous to the temperate forests of the Himalayas. The seeds of this tree are abundant in carbohydrates but are not edible because they contain a very significant quantity of bitter saponins. Indigenous tribes in the Chamba district of Himachal Pradesh possess a unique traditional knowledge of separating saponins and other impurities from starch. Once this process is over, the resultant product is used as food and medicine. The starch complex, locally known as Seek, is used to prepare several dishes for auspicious occasions. Seek is used as a noncereal diet during fasting, and to keep young children and the elderly warm during the chilly winter months. The local population utilizes the seeds to treat ailments like joint pain, fatigue, diabetes, venous insufficiency, phlebitis, hemorrhoids, ulcers, thrombosis, colic, etc. IHCN has a high energy value, superior starch quality, and a variety of secondary metabolites. These qualities make it a promising raw material for the nutraceutical, functional food, cosmetic, and pharmaceutical industries. The utilization of plant components through local indigenous knowledge, as well as their distribution, botany, and ecology, have been described in the present study. Inventorization of the production and productivity of the tree, selection of better and high-yielding germplasm, mechanized processing, value addition, and popularization would be helpful to develop sustainable management practices for IHCN and improve the livelihood and nutritional security of the tribal population residing in the remote localities of Western Himalayas. [ABSTRACT FROM AUTHOR]

Introduction Surgical removal of an impacted third molar is one of the most common oral surgical procedures performed in dental offices. The postoperative phase is often associated with severe inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) are usually prescribed to manage postoperative discomfort. NSAIDs have been associated with gastrointestinal bleeding, renal function disturbances, and platelet count reductions. Thus, the present study demonstrates the utility of aescin in managing postoperative discomfort after the surgical removal of impacted mandibular third molars. This study aimed to correlate salivary PGE2 levels and serum C-reactive protein levels with subjective and objective symptoms after surgical extraction of the mandibular third molar and their relationship with drug therapy. Methods The planned study is a single-center, double-blind, randomized, parallel, prospective clinical trial. Each patient will be prescribed either diclofenac sodium 150 mg/day or aescin (escin) 120 mg/day to be taken orally in divided doses for five days after surgically removing the impacted mandibular third molar. Pain will be assessed using a visual analog scale. Facial swelling and mouth opening will be recorded using a metric scale with standardized reference points. ELISA (enzyme-linked immunosorbent assay (ELISA) will be employed to measure salivary Prostaglandin E2 and serum C–reactive protein levels. All parameters will be recorded preoperatively (T0) on the second postoperative day (T1) and fifth postoperative day (T2). Conclusion The proposed study is expected to show a favorable response to the administration of aescin for the management of postoperative discomfort compared to diclofenac sodium after third molar surgery. The proposed study is expected to positively manipulate the levels of salivary Prostaglandin E2 and serum C–reactive protein, which are reliable inflammatory markers. The outcome of this study may provide an efficacious and safe alternative to conventional nonsteroidal anti-inflammatory drugs for managing postoperative discomfort following third molar surgery.

Background: Aescin is a mixture of the triterpene saponins extracted from the seeds of the horse chestnut tree Aesculus hippocastanum. Aescin has a venotonic, anti-inflammatory, antioxidant and anti-edematous characteristics that are mostly connected to the agent molecular mechanism. Objective: The present study aim to investigate the potential effects of Aescin on psoriasis induced by Imiquimod in male rats, ncluding its effect on the level of tumor necrosis factor alpha, Ki-67 and the histopathologic features of the psoriatic skin. Methods: Thirty-six albino male rats were divided into six groups each group containing 6 animals, psoriasis was induced by Imiquimod to five of the groups, while for the last group vasaline was applied and the group served as a control group. The animals were then treated with topical Aescin, topical clobetasol, combination of topical Aescin and clobetasol and oral Aescin, finally all animals were sacrificed and the dorsal back skin was taken to perform histopathological and immunohistochemical analysis. Results: regarding the level of Ki-67, Strong expression of Ki-67 was seen in the group who received Imiquimod only, where the scoring of Ki-67 was notably lowered among the other groups. However, the lowest expression was noticed in the group that were treated with the combination of topical Aescin and clobetasol. While the number of TNF-α positive cells and the intensity of immunostaining were higher in the induction group who received Imiquimod only and the lowest among the group who received the combination of topical Aescin and Clobetasol. Lastly the histopathologic analysis shows that the histopathologic features of psoriasis was markedly affected by the anti-inflammatory effect of Aescin and clobetasol, which was noticed through inhibition of proinflammatory markers, and the decrease in capillary permeability. Conclusion: Topical Aescin alone or in combination with clobetasol reduced Ki-67 expression successfully; furthermore, the combination of topical Aescin and Clobetasol decreased TNF- score and had the strongest anti-inflammatory activity more than the other groups. Lastly Aescin was able to alter the histopathologic features of the psoriatic skin through its anti-inflammatory, venotonic and anti-edematous activity.

The saponin β -aescin is well known for its self-aggregation above the critical micelle concentration (cmc) and its interaction with model membranes made of zwitterionic phospholipids including the formation of mixed bicelle systems. In this study, we investigate the interaction of β -aescin with small unilamellar vesicles (SUVs) made of the negatively charged lipid 1,2-dioleoyl-sn-glycero-3-phosphoglycerol (DOPG). The study is conducted at a pH value at which aescin is negatively charged as well, and mixtures up to an aescin content of 50 mol% (equivalent to a molecular ratio of 1:1) were investigated, so that the cmc of aescin is exceeded by far. Analysis of the system by scattering and NMR methods was performed with respect to two reference systems made of the bare components: DOPG SUVs and aescin micelles. Wide-angle X-ray scattering (WAXS) was used to determine molecular correlation distances for both kinds of molecules, and small-angle neutron and X-ray scattering (SANS and SAXS) revealed a structural picture of the system, which was further confirmed by diffusion-ordered nuclear magnetic resonance spectroscopy (DOSY-NMR). Contrary to the expected solubilization of the DOPG membrane, most probably none- or only weakly-interacting, separated DOPG SUVs and aescin micelles were found. The study additionally highlights the importance of using independent methods to characterize a rather complex colloidal system in order to obtain a complete picture of the structures formed. [ABSTRACT FROM AUTHOR]

The diabetic peripheral neuropathy pain model was constructed after 95 Sprague Dawley rats had been randomly divided among blank reference and model groups. Aescin low-dose group (0.5 mg/kg), aescin medium-dose group (1.0 mg/kg), aescin high-dose group (1.5 mg/kg), and positive control group (0.25 mg/ kg mecobalamin) were then randomly assigned to the simulation group following successful modeling. At the conclusion of the study, the mean sciatic nerve conduction velocity was determined, blood glucose in addition to the amount of inflammatory factors tumor necrosis factor-alpha, interleukin-6, and interleukin-1 were determined, and sciatic nerve cells from mice in all groups were collected for Western blot to identify the protein levels of high mobility group box 1 and receptor for advanced glycation end products. The mean sciatic nerve conduction velocity of the medium and high-dose groups of aescin was higher than those of the model control (p<0.05); rat blood glucose content, the contents of inflammatory factors interleukin-1 beta, interleukin-6 and tumor necrosis factor-alpha as well as the protein expression of high mobility group box 1 and receptor for advanced glycation end products in sciatic nerve tissue were lower and the body mass was higher than that of the model control group (p<0.05). Comparing the high-dose aescin group as well as the positive control group, there had been no discernible change in the aforementioned indices (p>0.05). Aescin is able to effectively improve the inflammatory response in the body by regulating high mobility group box 1-receptor for advanced glycation end products levels and slow down diabetic peripheral neuropathy caused by the inflammatory response. [ABSTRACT FROM AUTHOR]

Background and Purpose: Intravenous infusion of chemotherapy drugs can cause severe chemotherapy‐induced phlebitis (CIP) in patients. However, the underlying mechanism of CIP development remains unclear. Experimental Approach: RNA‐sequencing analysis was used to identify potential disease targets in CIP. Guanylate binding protein‐5 (GBP5) genetic deletion approaches also were used to investigate the role of GBP5 in NLR family pyrin domain containing 3 (NLRP3) inflammasome activation in lipopolysaccharide (LPS) primed murine bone‐marrow‐derived macrophages (BMDMs) induced by vinorelbine (VIN) in vitro and in mouse models of VIN‐induced CIP in vivo. The anti‐CIP effect of aescin was evaluated, both in vivo and in vivo. Key Results: Here, we show that the expression of GBP5 was upregulated in human peripheral blood mononuclear cells from CIP patients. Genetic ablation of GBP5 in murine macrophages significantly alleviated VIN‐induced CIP in the experimental mouse model. Mechanistically, GBP5 contributed to the inflammatory responses through activating NLRP3 inflammasome and driving the production of the inflammatory cytokine IL‐1β. Moreover, aescin, a mixture of triterpene saponins extracted from horse chestnut seed, can alleviate CIP by inhibiting the GBP5/NLRP3 axis. Conclusion and Implications: These findings suggest that GBP5 is an important regulator of NLRP3 inflammasome in CIP mouse model. Our work further reveals that aescin may serve as a promising candidate in the clinical treatment of CIP. [ABSTRACT FROM AUTHOR]

Introduction: Harmonization of methodological approaches to the analysis of herbal substances containing triterpenoid saponins, considered the largest group of phytochemicals, is essential for the pharmaceutical industry worldwide., Objectives: This review aimed to perform a comparative analysis of the requirements for the standardization of herbal substances, herbal medicinal products (HMPs), and other herbal materials containing triterpenoid saponins in the pharmacopeial texts of the Russian Federation and the world's leading pharmacopeias., Materials and Methods: The review covers the data on the quantitative and qualitative analysis of herbal substances containing triterpenoid saponins, as presented in the State Register of Medicinal Products of Russia and the monographs of the world's leading pharmacopeias: the European Pharmacopeia, United States Pharmacopeia, British Pharmacopeia, Japanese Pharmacopeia, and the national pharmacopeias of the Eurasian Economic Union (EEU) Member States., Results: This review compares and discusses the analytical methods used for the standardization of Aesculus hippocastanum L. seeds, Aralia elata (Miq.) Seem roots, Glycyrrhiza spp. roots, Orthosiphon aristatus (Blume) Miq. leaves, and Polemonium caeruleum L. rhizomes with roots. The most common analytical methods used are (HP)TLC and (U)HPLC. The Russian Pharmacopeia also includes titrimetry and spectrophotometry., Conclusions: The appropriate selection of a group of biologically active compounds for HMP standardization is still challenging. We believe that a rational approach to the standardization of herbal substances and HMPs should be based on the use of herbal substances with maximum extractability and specific pharmacological activity. The harmonized procedures and reference substances for the identification and assay of active metabolites in HMPs must be implemented at all stages of production control from herbal substances to finished dosage forms., (© 2025 John Wiley & Sons Ltd.)

Horse chestnut is known as a venotonizing agent of plant origin. The main active ingredient of chestnut common extract is aescin. It has anti-edema, anti-inflammatory and venotonizing properties. The aescin medicinal agent should be used for chronic vein disease, hemorrhoidal disease and post-traumatic edema. The pharmacological properties of chestnut horse extract allow the inclusion of medications based on it in the rehabilitation program of patients who have suffered a new coronavirus infection (COVID-19).

Recent studies of self-assembly in binary systems of bio-surfactants, either of microbial origin or saponins extracted from plants, are reviewed. Saponins in water reported in the first section include aescin, glycyrrhizin, and quillaja saponins, while rhamnolipids are discussed in the second section on microbial surfactants. Studies of surface activities are a natural starting point of the characterization of surfactants, but here we focus mainly on physico-chemical and structural properties of self-assembled bulk structures in solution, often characterized by scattering techniques. When quantitative modelling is performed, self-assembly parameters like aggregation numbers, head group areas, and resulting shapes can be followed as a function of physical-chemical parameters like concentration, composition, temperature, or pH. Morphologies include micelles and their structural evolution with addition of other bio- or synthetic surfactants, co-surfactants, proteins or phospholipids.

Abstract Objective This study evaluated hepatoprotective effect of aescin (AES) and diosmin (DIO), individually or in low-dose combination in chemically induced liver injury in rats. Rats were divided into 6 groups; Group 1, control, Group 2, injected with a single dose of a mixture of corn oil and carbon tetrachloride (CCl4) to induce hepatic toxicity. Before CCl4 injection, Groups 3–6 were treated daily for 14 days with silymarin (SIL) (200 mg/kg), aescin (AES; 3.6 & 1.75 mg/kg), Diosmin (DIO; 100 & 50 mg/kg). Serum samples were analyzed for different liver function, oxidative stress and antioxidant markers. Moreover, inflammation and tissue damage were confirmed by histological staining of liver tissue sections. Results Results indicated that CCl4 elevated serum levels of all assessed liver function markers and decreased levels of key antioxidants. Administration of AES and/or DIO significantly reversed all those CCl4-induced effects. Histopathological study showed disruption of the hepatic architecture, necrosis and inflammatory cells and depositions of glycogen and protein in the tissues of CCl4-treated group. Pretreatment with DIO and/or AES significantly improved histopathological structure of liver tissue. In conclusion, low-dose combination of AES and DIO exhibited significant and preferential hepatoprotective activity compared to individual treatment with AES or DIO.

Target. Comparative assessment of the clinical efficacy of Aescusan I generation phlebotonics application in the complex treatment of patients with CVD.Material and methods. Analysis of treatment of 380 patients who applied for a phlebological appointment at the polyclinic department of SamSMU Clinics for the period from September 2017 to March 2019 was conducted. Group I (n = 104) included patients with even outpatient card numbers who were prescribed Troxevasin as a first-generation phlebotonic according to the scheme recommended by manufacturers Group II (n = 276) included patients with odd outpatient card numbers who were prescribed Aescusan (an extract of horse chestnut seeds Aesculus hippocastanum, active ingredient of which is aescin) as phlebotonics of the first generation according to the scheme recommended by the manufacturers. All patients were examined by a phlebologist before and after 1 course of treatment. Clinical efficacy of the therapy was assessed by the severity of the pain syndrome, feeling of heaviness, swelling and seizures using visual analogue scale (VAS). In addition, the effectiveness of conservative therapy was assessed through interviews and questionnaires. For a comparative assessment of the severity of edema syndrome, the lower limb circumference was measured at ankle level using a graduated tape.Results. No side effects were detected during clinical observation of the use of drugs. After the course of treatment, most of the observations showed positive dynamics. Changes in clinical symptoms (pain, seizures, heavy legs) in Group I were statistically unreliable (p>0.05). In the second group there was a decrease of pain syndrome intensity by 73,2%, a decrease of convulsions - by 63,5%, a decreaseof heaviness feeling – by 73,7%. In the course of the survey, 272 patients (98.5%) of Group II evaluated the treatment results as good, 4 patients (1.5%) did not notice any treatment results.In the course of repeated examination after the treatment 96,5% of doctors noted the result in Group II as good, 3,5% - as satisfactory. Conclusion. Thus, the results of complex treatment of patients with CVD showed that the use of 1st generation phlebotonics should be considered not only as pathogenetically justified, but also effective from the clinical point of view. Application of Aescusan drug leads to statistically significant reduction of clinical symptoms (subjective and objective) of lower limbs CVD.

RETRACTED ARTICLEThe article is devoted to Aescusan, a well-studied preparation that is traditionally used in clinical practice for the treatment of chronic diseases of veins, hemorrhoids, postoperative and post-traumatic edema. The main active substance is aescin that is contained in horse chestnut seed extract - Aesculus hippocastanum. The paper presents data of a randomized controlled study demonstrating the efficacy of Aescusan in the treatment of chronic venous diseases and chronic venous edema along with the compression therapy. A number of in vitro and in vivo experimental studies provided convincing proof of efficacy of Aescusan. In particular, they proved the anti-edema, anti-inflammatory and venotonic effect of the preparation. Aescusan improves calcium ions entry into the smooth muscle cell channels in the vascular wall, which increases the venous vascular tone. The anti-inflammatory effect of Aescusan is associated with blockade of prostaglandin F2 (PGF2) release from the venous wall, 5-hydroxytryptamine (5-HT) and histamine antagonism, decreased catabolism of tissue mucopolysaccharides. Conclusion: Aescusan has a pluripotent effect on various pathogenetic mechanisms of chronic venous diseases. It is known for its good tolerability and ease of use, which makes it possible to use the preparation in patients with chronic venous diseases, hemorrhoids, and peripheral post-traumatic edema.

Medical treatment is very important in the relief of symptoms and pain related to hemorrhoidal disease, even in advanced cases with absolute surgical indication. Medical remedies containing components such as flavonoids, diosmin, calcium dobesilate, oxerutin, and horse chestnut (Aesculus hippocastanum, Hippocastanaceae family) are commonly used in the medical management of hemorrhoidal disease. The primary active constituent found in horse chestnut seed extract, aescin, is a mixture of triterpene saponins present in two forms, alpha and beta, which are distinguished by their water solubility and melting points; other constituents include bioflavonoids (quercetin and kaempferol), proanthocyanidin A2 (an antioxidant), and the coumarins fraxin and aesculin. The antiedematous, antiinflammatory and venotonic properties observed are due exclusively to aescin. Its venotonic effect was shown to be mediated by its sensitizing activity on ion channels in the vessel wall, especially to calcium, which results in an increase in contractility. It has also been proposed that enhanced release of prostaglandin F2 antagonizes the vasodilatory effects of histamine and serotonin, and venous wall damage is reduced by antagonizing proteoglycan degradation, which aids in the preservation of connective tissue integrity. Horse chestnut extract, which owes its antiseptic, venotonic, vasoprotective, and antiinflammatory properties to its aescin content, has emerged as an important agent that can facilitate the treatment of every stage of hemorrhoidal disease. In this review, we investigated these effects as well as its more recently studied apoptotic and antioxidant effects in light of experimental and clinical studies published in the literature.

In the present study, we show how acrylamide-based microgels can be employed for the uptake and release of the drug β-aescin, a widely used natural product with a variety of pharmacological effects. We show how aescin is incorporated into the microgel particles. It has an important influence on the structure of the microgels, by reducing their natural network-density gradient in the swollen state. Moreover, temperature-dependent measurements reveal how the incorporation of aescin stabilizes the microgel particles, while the volume phase transition temperature (VPTT) is almost constant, which is very important for the intended drug release. Finally, it is shown that upon increase of the temperature above the VPTT the particles are able to release aescin from their network, encouraging the use of this particular drug delivery system for hypothermia treatments. [ABSTRACT FROM AUTHOR]

Objective: This study evaluated hepatoprotective effect of aescin (AES) and diosmin (DIO), individually or in low-dose combination in chemically induced liver injury in rats. Rats were divided into 6 groups; Group 1, control, Group 2, injected with a single dose of a mixture of corn oil and carbon tetrachloride (CCl4) to induce hepatic toxicity. Before CCl4 injection, Groups 3–6 were treated daily for 14 days with silymarin (SIL) (200 mg/kg), aescin (AES; 3.6 & 1.75 mg/kg), Diosmin (DIO; 100 & 50 mg/kg). Serum samples were analyzed for different liver function, oxidative stress and antioxidant markers. Moreover, inflammation and tissue damage were confirmed by histological staining of liver tissue sections. Results: Results indicated that CCl4 elevated serum levels of all assessed liver function markers and decreased levels of key antioxidants. Administration of AES and/or DIO significantly reversed all those CCl4-induced effects. Histopathological study showed disruption of the hepatic architecture, necrosis and inflammatory cells and depositions of glycogen and protein in the tissues of CCl4-treated group. Pretreatment with DIO and/or AES significantly improved histopathological structure of liver tissue. In conclusion, low-dose combination of AES and DIO exhibited significant and preferential hepatoprotective activity compared to individual treatment with AES or DIO. [ABSTRACT FROM AUTHOR]

Species of the genus Aesculus are very attractive woody ornamentals. Their organs contain numerous health-promoting phytochemicals. The most valuable of them—aescin—is used in commercial preparations for the treatment of venous insufficiency. The industrial source of aescin is horse chestnut seeds because the zygotic embryos are the main site of its accumulation. Horse chestnut somatic and zygotic embryos contain similar amount of aescin, hence somatic embryos could be exploited as an alternative source of aescin. Somatic embryogenesis, androgenesis and de novo shoot organogenesis were successfully achieved in several Aesculus species, as well as secondary somatic embryogenesis and shoot organogenesis, which enables mass production of embryos and shoots. In addition, an efficient method for cryopreservation of embryogenic tissue was established, assuring constant availability of the plant material. The developed methods are suitable for clonal propagation of elite specimens selected as the best aescin producers, the most attractive ornamentals or plants resistant to pests and diseases. These methods are also useful for molecular breeding purposes. Thus, in this review, the medicinal uses and a comprehensive survey of in vitro propagation methods established for Aesculus species, as well as the feasibility of in vitro production of aescin, are presented and discussed.

Background: Benign prostatic hyperplasia (BPH) is the most common urogenital condition in aging males, while inflammation and tissue proliferation constitute the main pathophysiological factors. The adverse effects of currently available BPH medications limit patient compliance. We tested the protective effect of aescin against the development of BPH in rats. Methods: A total of 18 male Wistar rats were divided into 3 groups: control (sesame oil 1 mL/kg, s.c.); BPH (testosterone oenanthate 3 mg/kg, s.c., in sesame oil), and BPH-aescin rats (testosterone oenanthate 3 mg/kg, s.c. + aescin 10 mg/kg/day, p.o.). All treatments continued for 4 weeks. Serum and prostatic samples were harvested for biochemical and histopathological examination. Results: Induction of BPH by testosterone increased the prostate weight and prostate weight index, serum testosterone, prostate expression of inflammatory (IL-1β, TNF-α, and COX-2), and proliferative markers (PCNA and TGF-β1). Concurrent treatment with aescin decreased the testosterone-induced increase in prostatic IL-1β, TNF-α, and COX-2 expression by 47.9%, 71.2%, and 64.4%, respectively. Moreover, aescin reduced the prostatic proliferation markers TGF-β1 and PCNA by 58.3% and 71.9%, respectively, and normalized the prostate weight. Conclusion: The results of this study showed, for the first time, that aescin protected against the development of experimental BPH in rats via its anti-inflammatory and antiproliferative effects. These findings warrant further studies to clinically repurpose aescin in the management of BPH.

The saponin escin, extracted from horse chestnut seeds, forms adsorption layers with high viscoelasticity and low gas permeability. Upon deformation, escin adsorption layers often feature surface wrinkles with characteristic wavelength. In previous studies, we investigated the origin of this behavior and found that the substantial surface elasticity of escin layers may be related to a specific combination of short-, medium-, and long-range attractive forces, leading to tight molecular packing in the layers. In the current study, we performed atomistic molecular dynamics simulations of 441 escin molecules in a dense adsorption layer with an area per molecule of 0.49 nm2. We found that the surfactant molecules are less submerged in water and adopt a more upright position when compared to the characteristics determined in our previous simulations with much smaller molecular models. The number of neighbouring molecules and their local orientation, however, remain similar in the different-size models. To maintain their preferred mutual orientation, the escin molecules segregate into well-ordered domains and spontaneously form wrinkled layers. The same specific interactions (H-bonds, dipole–dipole attraction, and intermediate strong attraction) define the complex internal structure and the undulations of the layers. The analysis of the layer properties reveals a characteristic wrinkle wavelength related to the surface lateral dimensions, in qualitative agreement with the phenomenological description of thin elastic sheets.

Osteoarthritis (OA) stands as a prevalent and progressively debilitating clinical condition globally, impacting joint structures and leading to their gradual deterioration through inflammatory mechanisms. While both non-modifiable and modifiable factors contribute to its onset, numerous aspects of OA pathophysiology remain elusive despite considerable research strides. Presently, diagnosis heavily relies on clinician expertise and meticulous differential diagnosis to exclude other joint-affecting conditions. Therapeutic approaches for OA predominantly focus on patient education for self-management alongside tailored exercise regimens, often complemented by various pharmacological interventions primarily targeting pain alleviation. However, pharmacological treatments typically exhibit short-term efficacy and local and/or systemic side effects, with prosthetic surgery being the ultimate resolution in severe cases. Thus, exploring the potential integration or substitution of conventional drug therapies with natural compounds and extracts emerges as a promising frontier in enhancing OA management. These alternatives offer improved safety profiles and possess the potential to target specific dysregulated pathways implicated in OA pathogenesis, thereby presenting a holistic approach to address the condition's complexities.

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Abstract The plant-derived biosurfactant aescin is naturally present in many plants and is used for treatment of disorders such as varicose veins and inflammation of veins. The hemolytic activity of this saponin is attributed to its interaction with cholesterol in the red blood cell membrane. This work investigates the phase and aggregation behavior of saponin-containing model membranes consisting of the phospholipid 1,2-dimyristoyl- sn -glycero-3-phosphocholine (DMPC). The aescin concentrations studied range from 1 mol% to 7 mol% with respect to the total lipid content. The methods of choice to elucidate the structural picture are small-angle scattering of X-rays (SAXS) and neutrons (SANS) and cryogenic transmission electron microscopy (cryo-TEM). SANS and SAXS revealed that at lower aescin contents vesicular structures are conserved and vesicles tend to aggregate already at aescin contents of around 1 mol%. Aggregation and vesicle deformation effects are found to be stronger when the phospholipids are in the L β ′ phase. With increasing aescin content, mixed structures, i.e. aggregated and deformed vesicles and solubilized bilayer fragments, are present. This was proven for a sample with 4 mol% aescin by cryo-TEM. An increasing aescin amount leads to membrane decomposition and free standing bilayers which tend to build stacks at high temperature. These stacks are characterized by SAXS using the modified Caillé theory. Analyses and model dependent fitting reveal formation of well-defined structures beginning at 7 mol% aescin. Graphical Abstract Highlights • High quality small angle scattering data are presented. • DMPC/aescin mixtures show a pronounced concentration and temperature dependent phase behavior. • Coexistence of different structures is revealed. • A first step in understanding the molecular action of saponins on biomembranes is provided. [ABSTRACT FROM AUTHOR]

The liver plays a crucial role in biotransformation but it is susceptible to chemical-induced damage, known as hepatotoxicity. Traditional therapies for protecting the liver face significant challenges, including poor bioavailability, off-target effects, adverse reactions, drug breakdown, and inadequate uptake. These issues emphasize the need for precise, targeted therapeutic approaches against hepatotoxicity. The objective of our research was to develop a customized, biocompatible, and biodegradable nanodrug delivery system for hepatoprotection. We chose collagen hydrolyzed protein, or gelatin, as the base material and utilized solvent evaporation and nanoprecipitation methods to create nanoparticles with size ranging from 130 to 155 nm. The resulting nanoparticles exhibited a spherical and smooth surface, as confirmed by scanning and transmission electron microscopy. Bioactive aescin (AES), into these gelatin nanoparticles (AES-loaded gel NPs), we tested these nanoparticles using a hepatotoxicity model. The results were indicating a significant reduction in the levels of key biomolecules, including NF-κB, iNOS, BAX, and COX-2 and decreased serum levels of enzymes ALT and AST. This reduction correlated with a notable alleviation in the severity of hepatotoxicity. Furthermore, the treatment with AES-loaded gel NPs resulted in the downregulation of several inflammatory and liver-specific biomarkers, including nitrite, MPO, TNF-α, and IL-6. In summary, our study demonstrates that the AES-loaded gel NPs were markedly more effective in mitigating experimental hepatotoxicity when compared to the free aescin. The nanoparticles exhibited a propensity for suppressing liver damage, showcasing the potential of this targeted therapeutic approach for safeguarding the liver from harmful chemical insults. • Aescin loaded gelatin NPs were synthesized successfully. • NPs significantly decreased hepatic damage. • Overall aescin loaded gelatin nanoparticles showed enhanced hepatoprotection than free drugs [ABSTRACT FROM AUTHOR]

Background: Aescin, a natural mixture of saponins occurring in Aesculus hippocastanum, exhibits important flebotonic properties, being used in the treatment of chronic venous insufficiency in legs. The inclusion of aescin into cyclodextrins (CDs) is a technical solution for its incorporation into the textile of stockings, but details of the physicochemistry of these host–guest systems are lacking. This work investigates the inclusion of aescin into the cavities of two native cyclodextrins, β-CD and γ-CD.Results: The continuous variation method applied to aqueous-phase 1H nuclear magnetic resonance (1H NMR) has demonstrated that the preferred CD/aescin inclusion stoichiometries are 2:1 with β-CD and 1:1 with γ-CD. The affinity constant calculated for γ-CD·aescin was 894 M−1, while for 2β-CD·aescin it was estimated to be 715 M−1. Density functional theory (DFT) calculations on the interaction of aescin Ib with CDs show that an inclusion can indeed occur and it is further demonstrated that the wider cavity of γ-CD is more adequate to accommodate this large guest. ROESY spectroscopy is consistent with the formation of a complex in which the triterpenic moiety of aescin is included into the cavity of γ-CD. The higher stability of this geometry was confirmed by DFT. Furthermore, DFT calculations were applied to determine the chemical shifts of the protons H3 and H5 of the CDs in the optimised structures of the inclusion complexes. The calculated values are very similar to the experimental data, validating the approach made in this study by NMR.Conclusion: The combination of experimental data from aqueous-state NMR measurements and theoretical calculations has demonstrated that γ-CD is the most suitable host for aescin, although the inclusion also occurs with β-CD. The geometry of the γ-CD·aescin complex is characterised by the inclusion of the triterpene segment of aescin into the host cavity.

Lung cancer is the most common and lethal cancer worldwide, yet there are no adequate and novel medications to control this illness. Previous reports suggested the potential of protein kinases to target lung cancer by regulating autophagy. This study establishes the role of aescin, a triterpenoid saponin, in targeting protein kinases responsible for lung cancer proliferation and mobility. The experimental data revealed that aescin significantly impedes lung cancer cell proliferation by downregulating protein kinases such as AKT, mTOR, MEK, and ERK. Downregulation of AKT-mTOR may promote a string of events inducing cytotoxic autophagy-mediated apoptosis in the presence of aescin. Besides, aescin decreases mobility and invasion by downregulating HIF-1α and VEGF gene expressions. Moreover, it successfully monitors EGFR gene expression, improves lung histology, and regulates biochemical parameters in a pre-clinical DEN-induced lung cancer model. Aescin was observed to be safe and non-toxic in both in silico toxicity predictions and ex vivo erythrocyte fragility assays. Hence, this study elucidates the molecular mechanism of aescin in targeting protein kinases and suggests that it could be a safer and more viable therapeutic agent for lung cancer treatment. [Display omitted] [ABSTRACT FROM AUTHOR]

This work investigates the temperature-dependent micelle formation as well as the micellar structure of the saponin aescin. The critical micelle concentration ( c m c ) of aescin is determined from the concentration-dependent autofluorescence (AF) of aescin. Values between c m c aescin , AF (10 ∘ C) = 0.38 ± 0.09 mM and c m c aescin , AF (50 ∘ C) = 0.32 ± 0.13 mM were obtained. The significance of this method is verified by tensiometry measurements. The value determined from this method is within the experimental error identical with values obtained from autofluorescence ( c m c aescin , T ( WP ) (23 ∘ C) = 0.33 ± 0.02 mM). The structure of the aescin micelles was investigated by small-angle X-ray scattering (SAXS) at 10 and 40 ∘ C. At low temperature, the aescin micelles are rod-like, whereas at high temperature the structure is ellipsoidal. The radii of gyration were determined to ≈31 Å (rods) and ≈21 Å (ellipsoid). The rod-like shape of the aescin micelles at low temperature was confirmed by transmission electron microscopy (TEM). All investigations were performed at a constant pH of 7.4, because the acidic aescin has the ability to lower the pH value in aqueous solution.

Aescin nanoparticles (ANPs) were prepared using solution-enhanced dispersion by supercritical fluids (SEDS) in order to improve the dissolution properties of aescin and avoid complicated salt-forming procedures. Because aescin is a mixture, the effects of the operating conditions on the composition of the ANPs were first investigated. The compositional ratio of the four dominant active components in aescin changed with the pressure at low solution concentrations (5 mg/mL), but remained constant at higher concentrations (>10 mg/mL). Spherical ANPs with an average diameter below 50 nm was obtained at 12 MPa with solution concentration between 10 to 15 mg/mL. The morphology of ANPs was primarily influenced by the concentration and pressure but not affected by the nozzle diameter. The dissolution of aescin was increased by near 5.5 times from raw aescin to ANPs. Compared with the sodium aescinate, the ANPs exhibited the similar dissolution, but had a moderate initial dissolution burst. [ABSTRACT FROM AUTHOR]

The colorimetric assay used for saponin quantification in plant extracts is subject to interference by common solvents used to extract the saponins from plant materials. Therefore, the degree of interference of ten common solvents was investigated. It was found that the presence of acetone, methanol and n-butanol in the reaction solution caused an intense darkening of the reaction solution in the absence of saponins, which likely could lead to erroneous saponin content values. Using aescin to construct standard curves with different solvents—such as water, ethanol, and methanol— also showed significant differences in the standard curves obtained, which led to different values when they were applied to quantify the saponin content of an ethanol extract from dried and powdered Gac (Momordica cochinchinensis Spreng) seed kernels. To improve the method, a solvent evaporation step was added prior to the colorisation reaction to prevent undesired solvent interference during the reaction step. Using this modified protocol for the aescin standard curve and the Gac seed kernel extract eliminated any solvent interference. Thus, this improved protocol is recommended for the quantification of the saponin content of plant extracts irrespective of which extraction solvent is used.

Non-alcoholic fatty liver disease (NAFLD) is a common metabolic liver disease worldwide. It has been proven that aescin (Aes), a bioactive compound derived from the ripe dried fruit of Aesculus chinensis Bunge , has a number of physiologically active properties like anti-inflammatory and anti-edema, however it has not been investigated as a potential solution for NAFLD. This study's major goal was to determine whether Aes can treat NAFLD and the mechanism underlying its therapeutic benefits. We constructed HepG2 cell models in vitro that were affected by oleic and palmitic acids, as well as in vivo models for acute lipid metabolism disorder caused by tyloxapol and chronic NAFLD caused by high-fat diet. We discovered that Aes could promote autophagy, activate the Nrf2 pathway, and ameliorate lipid accumulation and oxidative stress both in vitro and in vivo. Nevertheless, in Autophagy-related proteins 5 (Atg5) and Nrf2 knockout mice, Aes lost its curative impact on NAFLD. Computer simulations show that Aes might interact with Keap1, which might allow Aes to increase Nrf2 transfer into the nucleus and perform its function. Importantly, Aes's stimulation of autophagy in the liver was hampered in Nrf2 knockout mice. This suggested that the impact of Aes in inducing autophagy may be connected to the Nrf2 pathway. We first discovered Aes's regulating effects on liver autophagy and oxidative stress in NAFLD. And we found Aes may combine the Keap1 and regulate autophagy in the liver by affecting Nrf2 activation to exert its protective effect. [Display omitted] [ABSTRACT FROM AUTHOR]

OBJECTIVE: Impairment of the peripheral microcirculation in diabetic patients often leads to severe complications in the lower extremities, such as foot infections and ulcerations. In this study, a novel aescin-based formulation has been evaluated as a potential approach to prevent skin breaks and ulcerations by improving the peripheral microcirculation and skin hydration. PATIENTS AND METHODS: In this registry study, 63 patients with moderate diabetic microangiopathy were recruited. Informed participants freely decided to follow either a standard management (SM) to prevent diabetic foot diseases (n = 31) or SM associated with topical application of the aescin-based cream (n = 32). Peripheral microcirculatory parameters such as resting skin flux, venoarteriolar response and transcutaneous gas tension were evaluated at inclusion and after 8 weeks. In addition, several skin parameters of the foot area, such as integrity (as number of skin breaks/patients), hydration and content of dead cells were assessed at the defined observational study periods. RESULTS: Improvements in cutaneous peripheral microcirculation parameters were observed at 8 weeks in both groups; however, a remarkable and significant beneficial effect resulted to be exerted by the aescin-based cream treatment. In fact, the microcirculatory parameters evaluated significantly improved in the standard management + aescin-based cream group, compared with baseline and with the standard management group. Similar findings were reported for skin parameters of the foot area. CONCLUSIONS: The topical formulation containing aescin could represent a valid approach to manage skin wounds and prevent skin ulcerations in patients affected by moderate diabetic microangiopathy. [ABSTRACT FROM AUTHOR]

Aescin has many physiological functions that are highly relevant to spinal cord injury (SCI), including anti-inflammation, anti-oxidation, anti-oedema, and enhancing vascular tone. The present study investigated the putative therapeutic value of aescin in SCI, with a focus on its neuroprotective, anti-inflammatory, and anti-oxidative properties. Sodium aescinate (1.0 mg/kg body weight) or equivalent volume of saline was administered 30 min after injury by intravenous injection, with an additional dose daily for seven consecutive days after moderate SCI in rats. After contusion injury of the 8th thoracic (T8) spinal cord, aescin-treated rats developed less severe hind limb weakness than saline controls, as assayed by the Basso-Beattie-Bresnahan scale, the beam walking test, and a footprint analysis. The improved locomotor outcomes in aescin-treated rats corresponded to markedly decreased immune response, oxidative stress, neuronal loss, axon demyelination, spinal cord swelling, and cell apoptosis, measured around T8 after impact. Our data suggest aescin treatment as a novel, early, neuroprotective approach in SCI. Given the known safety of aescin in clinical applications, the results of this study suggest that it is a good candidate for SCI treatment in humans. [ABSTRACT FROM AUTHOR]

From the seed of Aesculus hippocastanum L., a complex mixture of triterpene saponin glycosides known as aescin was isolated, purified and characterized to be an active pharmaceutical ingredient for preparing of drug products. A reversed phase high performance liquid chromatographic method with UV detection was developed for the determination of total triterpene glycosides in enteric coated tablets containing aescin in a pattern-oriented manner. The mobile phase consisted of a mixture of acetonitrile and 0.1 % phosphoric acid solution (40: 60). UV detection was performed at 220 nm. The chromatographic column was Gemini C18 column, 5 µm 250 mm × 4.6 mm, which was maintained at 25 ◦C, connected with a precolumn (C18, 4.0 × 3.0 mm, 5 µm). The linear range was from 53.4 to 160.1 μg·mL−1. The RSD of intra-and inter-day precision variations were less than 1 % and the mean recovery was (100.66 ± 0.49) % (RSD = 0.64 %). The method showed its suitability, simplicity, rapidity and precision. Accordingly, it was proven adequate for quality control of this herbal drug product either for registration with the regulartory authority or routine analysis. • HPLC pattern-oriented approach. • Aescin from Aesculus hippocastanum L. in tablets determining. • Quality control and drug registration. [ABSTRACT FROM AUTHOR]

Aescin (escin) derived from the seeds of horse chestnut (Aesculus hippocastanum L.) is a natural mixture of triterpene saponins exhibiting a wide variety of pharmacological properties, including antiinflammatory, analgesic, and antipyretic activities. However, data concerning antifungal activities of these compounds are limited. This study aims to evaluate the in vitro antifungal susceptibility of Candida glabrata clinical isolates to #&945;- aescin sodium, #&946;-aescin crystalline and #&946;-aescin sodium using the disk diffusion (DD) and broth microdilution (BMD) methods. Moreover, the influence of subinhibitory concentration (0.5×MIC) of #&946;-aescins on the nystatin MIC was also studied. In general, the results obtained by the DD assay correlated well with those obtained by the BMD method. Both #&946;-aescins effectively inhibited the growth of all 24 strains tested. The minimum inhibitory concentration (MIC) values ranging from 8 to 32µg/ml for #&946;-aescin crystalline, whereas those of #&946;-aescin sodium were slightly lower and ranged from 4 to 16µg/ml. In contrast, #&945;-aescin sodium was found to be completely ineffective against the strains studied. MIC values of nystatin were reduced 2-16-fold and 2-4-fold in the presence of subinhibitory concentration of #&946;-aescin crystalline and #&946;-aescin sodium, respectively. Results of the present study may suggest the additive interaction between #&946;-aescin and nystatin. [ABSTRACT FROM AUTHOR]

The sustained release of alprenolol, a β-adrenergic antagonist, could be beneficial for the treatment of various heart diseases while reducing the side effects resulting from its continuous use. The novel and branched copolymers uniquely composed of biodegradable components (lactide and glycolide) have been synthesized using natural and therapeutically-efficient aescin-initiator, and consequently characterized to determine their structures and physicochemical properties. The obtained matrices were not cyto- and genotoxic towards bacterial luminescence, protozoan, and Salmonella typhimurium TA1535. The copolymers release the drug in vitro in a sustained manner and without burst release. The value of the drug released was strongly dependent on the copolymer composition and highly correlated with the hydrolytic matrices' degradation results. [ABSTRACT FROM AUTHOR]