Ethnopharmacological Use Research Articles

Tubiechong patching promotes tibia fracture healing in rats by regulating angiogenesis through the VEGF/ERK1/2 signaling pathway

Ethnopharmacological relevanceThe external use of traditional Chinese medicine (TCM) to treat fractures has a long history of clinical application and theoretical basis, and is also one of the characteristic treatment methods of TCM with significant efficacy and many advantages. Among the commonly used external Chinese medicines, Tubiechong is noteworthy. Aim of the studyTo elucidate whether local patching of Tubiechong can promote fracture healing and explore its mechanism of action. Materials and methodsA rat tibia fracture model was constructed by the modified Einhorn modeling method. X-ray films were taken to evaluate the progress of fracture healing. Serum bone alkaline phosphatase (BALP), osteocalcin (BGP) and the C-terminal content of collagen type I (CTX-I) were analyzed by ELISA. CD31 immunohistochemistry was used to evaluate angiogenesis in the tibia segment. The effects of Tubiechong decoction (TD) on HUVEC proliferation, migration and invasion were detected by MTT assay, wound healing assay and Transwell migration assay, respectively. RNA-seq was performed to identify differentially expressed genes (DEGs). Enrichment of functions and signaling pathway analysis were performed based on the Gene Ontology (GO) and the Kyoto Encyclopedia of Genes and Genomes (KEGG) database. Quantitative real time polymerase chain reaction (qRT-PCR) was used to study gene expression levels. Western blotting (WB) was used to detect the expression of relevant regulatory proteins. ResultsThe healing time of rat tibia fractures in the three TD dose groups was shortened. The serum levels of BALP, BGP and CTX- I in the TD-treated group were higher than those in the NC group. The X-ray results showed that on the 7th day after surgery, the fracture healing degree of the high-dose TD group was significantly better than that of the NC group, and the fracture healing degrees of each TD treatment group were significantly higher than those of the NC group on the 14th, 17th, and 21st days after the operation. The CD31 immunohistochemistry results showed that the number of blood vessels and the vascular area in the TD treatment group were higher than those in the NC group. In vitro, TD promoted the proliferation, wound healing and migration of HUVECs. GO analysis of transcriptome sequencing results showed that TD significantly altered the expression of genes related to cell growth, metabolism, and motility. According to KEGG annotations, VEGFA was upregulated. Eight DEGs were enriched in the VEGFA-VEGFR2 signaling pathway, of which six were upregulated. KEGG signaling pathway analysis showed that the most abundant DEGs were in mitogen-activated protein kinase (MAPK) signaling pathway. qRT-PCR showed that VEGFA gene expression in HUVECs was 7.8 times that of the control group after 1 mg/mL TD treatment for 24 h, and WB experiments showed that its protein expression was 3 times that of the control group. WB results showed that the phosphorylated ERK gene was highly expressed, while the expression levels of phosphorylated P38 and phosphorylated JNK protein remained unchanged. ConclusionTubechong patching therapy promotes tibia fracture healing in rats by regulating angiogenesis through the VEGF/ERK1/2 signaling pathway.

Efficacy of Trevesia palmata (Roxb. ex Lindl.) Vis. Extract on MG 63 cell lines and arthritis-induced animal models

Ethnopharmacological relevanceDespite widespread use of herbal remedies for treating arthritis and osteosarcoma, many plants are still not pharmacologically evaluated for their efficacy. Contrary to many non-steroidal, immunosuppressants, antibiotics, and antineoplastic drugs that have adverse effects, phytotherapeutic compounds have promising benefits with fewer complications. In this study the unexplored Northeastern India indigenous plant Trevesia palmata (Roxb. ex Lindl.) Vis. used in traditional medicine to cure bone fractures is chosen for studying anti-proliferative and anti-rheumatic properties. Aim of the studyThis study designed to explore the polyphenolic composition, antioxidant, anti-inflammatory and anti-arthritic potential of T. palmata leaf extracts. Further, the cellular activity was studied using MG 63 osteoblast cell lines and pharmacologically evaluated using Complete Freund's Adjuvant (CFA) induced arthritic rat model. Materials and methodsIn vitro free radical scavenging activity, anti-inflammatory and anti-arthritic activities of extracts were analyzed using standardized methods. The polyphenolic profiling and apoptosis inducing ability of T. palmata ethyl acetate (TPEA) extract on MG 63 osteoblast cell lines were analyzed. The in vivo pharmacological studies were carried out with low dose 250 mg/kg and high dose of 500 mg/kg of T. palmata. The biochemical and haematological parameters and in vivo antioxidant activity were evaluated for the control and treated groups. Radiological and histological study were done to understand the impact and penetration of inflammatory arthritis from tissues to joint bones. ResultsTPEA showed highest free radical scavenging activity (DPPH - 4.72 IC50, ABTS - 242.33 ± 6.81 mM TE/g extract), anti-inflammatory (40.04% inhibition of RBC lysis) and anti-arthritic activity (32.4% inhibition of protein denaturation) with the presence of gallic acid, catechin, caffeic acid, rutin, quercetin and naringenin. The TPEA extract inhibited cell proliferation of MG 63 osteoblast cells and induced apoptosis by arresting cell cycle at different phases. After acute toxicity studies the doses 250 mg/kg and 500 mg/kg were fixed and showed better results in CFA-induced arthritic animals. Thus, the extract phytoconstituents may have immense potential against chronic inflammation, joint ailments, bone cancer and arthritis which serves as a phytomedicine contrary to synthetic medications. ConclusionsThe potential treatment of polyphenolic compounds in the T. palmata extract on osteosarcoma and arthritis was demonstrated from this study. Thus, cellular inflammatory infiltrates are significantly reduced in bone and joint tissues as well.

THE DEVELOPMENTAL AND BIOCHEMICAL FEATURES OF LEISHMANIA DONOVANI PROMASTIGOTE AND THEIR REPRESSION BY DATURA STRAMONIUM PLANT EXTRACT

Leishmania is an intracellular digenetic obligate parasite spread by insects and poses grave health issues throughout the world. Extensive use of antimony compounds as drugs poses high toxicity and cost and therefore, a position has been identied for herbal medicine. This study has been carried out to explore the developmental biochemical characteristics of Leishmania donovani promastigote. In addition, the mode of action of Datura stramonium (Solanaceae) plant extract on promastigote form of leishmania have been examined. Friedman's repeated measures analysis showed that 96hr of development is the junction point in promastigotes ontogeny. Post 96hr, it grows with a long stationary phase with higher enzymatic activities viz., acid phosphatase, superoxide dismutase and glutathione (oxidized and reduced). Total protein estimated, showed a linear relationship (R2 = 0.999). Phytochemical screening of extracts showed the presence of alkaloid, avonoid, xed oil and fats, saponin, tannin and phenolic compounds etc, and showed an effectual free radical scavenging in the DPPH assay with an IC50 value of extract of D. stramonium (55.63 µg/ml). A concentration of 250 µg/mL of the plant extract completely inhibited the L. donovani promastigotes in vitro while concentrations of 50 µg/mL and 100 µg/mL decreased the survival level by 25-50%. Our ndings corroborate the ethnopharmacological use of this plant for the treatment of Leishmaniasis. Also, our results are promoters as potential sources to search antileishmanial bioactive agents.

Chemical Composition and In Vitro Anti-Helicobacter pylori Activity of Campomanesia lineatifolia Ruiz & Pavón (Myrtaceae) Essential Oil.

Helicobacter pylori is the most common cause of gastritis and peptic ulcers, and the number of resistant strains to multiple conventional antimicrobial agents has been increasing in different parts of the world. Several studies have shown that some essential oils (EO) have bioactive compounds, which can be attributed to antimicrobial activity. Therefore, EOs have been proposed as a natural alternative to antibiotics, or for use in combination with conventional treatment for H. pylori infection. Campomanesia lineatifolia is an edible species found in the Brazilian forests, and their leaves are traditionally used for the treatment of gastrointestinal disorders. Anti-inflammatory, gastroprotective, and antioxidant properties are attributed to C. lineatifolia leaf extracts; however, studies related to the chemical constituents of the essential oil and anti-H. pylori activity is not described. This work aims to identify the chemical composition of the EO from C. lineatifolia leaves and evaluate the anti-H. pylori activity. The EO was obtained by hydrodistillation from C. lineatifolia leaves and characterized by gas chromatography–mass spectrometry analyses. To assess the in vitro anti-H. pylori activity of the C. lineatifolia leaf’s EO (6 μL/mL–25 μL/mL), we performed broth microdilution assays by using type cultures (ATCC 49503, NCTC 11638, both clarithromycin-sensitive) and clinical isolate strains (SSR359, clarithromycin-sensitive, and SSR366, clarithromycin-resistant). A total of eight new compounds were identified from the EO (3-hexen-1-ol (46.15%), α-cadinol (20.35%), 1,1-diethoxyethane (13.08%), 2,3-dicyano-7,7-dimethyl-5,6-benzonorbornadiene (10.78%), aromadendrene 2 (3.0%), [3-S-(3α, 3aα, 6α, 8aα)]-4,5,6,7,8,8a-hexahydro-3,7,7-trimethyl-8-methylene-3H-3a,6-methanoazulene (2.99%), α-bisabolol (0.94%), and β-curcumene (0.8%)), corresponding to 98.09% of the total oil composition. The EO inhibited the growth of all H. pylori strains tested (MIC 6 μL/mL). To our knowledge, the current study investigates the relation between the chemical composition and the anti-H. pylori activity of the C. lineatifolia EO for the first time. Our findings show the potential use of the C. lineatifolia leaf EO against sensitive and resistant clarithromycin H. pylori strains and suggest that this antimicrobial activity could be related to its ethnopharmacological use.

Antihypertensive Activity in High Salt-Induced Hypertensive Rats and LC-MS/MS-Based Phytochemical Profiling of Melia azedarach L. (Meliaceae) Leaves.

Melia azedarach L. leaves have been traditionally used but not scientifically evaluated for antihypertensive activity. The focus of the present work was to carry out the detailed phytochemical profiling and antihypertensive potential of methanolic extract and subsequent fractions of this plant. The tandem mass spectrometry-based phytochemical profiling of M. azedarach extract (Ma.Cr) and fractions was determined in negative ionization mode while molecular networking was executed using the Global Natural Product Social (GNPS) molecular networking platform. This study resulted in the identification of 29 compounds including flavonoid O-glycosides, simple flavonoids, triterpenoidal saponins, and cardenolides as the major constituents. Ma.Cr at the concentration of 300 mg/kg resulted in a fall in blood pressure (BP), i.e., 81.44 ± 2.1 mmHg in high salt-induced hypertensive rats in vivo, in comparison to normotensive group, i.e., 65.36 ± 1.8 mmHg at the same dose. A decrease in blood pressure was observed in anaesthetized normotensive and hypertensive rats treated with extract and various fractions of M. azedarach. A reasonable activity was observed for all fractions except the aqueous fraction. The highest efficacy was shown by the ethyl acetate fraction, i.e., 77.06 ± 3.77 mmHg in normotensive and 88.96 ± 1.3 mmHg in hypertensive anaesthetized rats. Ma.Cr and fractions showed comparatively better efficacy towards hypertensive rats as compared to rats with normal blood pressure. Blood pressure-lowering effects did not change upon prior incubation with atropine. In vitro testing of Ma.Cr and polarity-based fractions resulted in L-NAME sensitive, endothelium-dependent vasodilator effects on aortic tissues. Pretreatment of aorta preparations with Ma.Cr and its fractions also blocked K+-induced precontractions indicating Ca2+ channel blocking activity comparable to verapamil. The extract and polarity-based fractions did not reveal a vasoconstrictor response in spontaneously beating isolated rat aorta. Ma.Cr and fractions when used in atrial preparations resulted in negative inotropic and chronotropic effects. These effects in atrial preparations did not change in the presence of atropine. These effects of extract and fractions explained the antihypertensive potential of M. azedarach and thus provided a scientific basis for its ethnopharmacological use in the treatment of hypertension. Among the constituents observed, flavonoids and flavonoid O-glycosides were previously reported for antihypertensive potential.

Acute toxicity profile and gastroprotective potential of ethanolic leaf extract of Manihot esculenta Crantz

The leaves of Manihot esculenta Crantz are used widely in traditional medicine to treat gastric ulcers. However, the safety and ethnopharmacological use of the plant as an anti-ulcer agent has not been validated in experimental studies. The study investigated the toxicity profile and anti-ulcer properties of ethanolic leaf extract of Manihot esculenta (MELE) in rats. A high dose of MELE (2000 mg/kg, p.o.) did not cause death in any of the rats. Moreover, no behavioural, haematological, or biochemical abnormalities could be attributed to the extract. The administration of acidified alcohol reduced rats’ luminal pH from 4.47 ± 1.39 (naïve control) to 1.95 ± 0.31 in the negative control rats. However, pre-treatment of rats with MELE (30, 100, and 300 mg/kg, p.o.) or omeprazole (10 mg/kg, p.o.) significantly (p < 0.05) elevated the luminal pH to 2.24 ± 0.19, 3.21 ± 0.18, 3.12 ± 0.40 and 2.63 ± 0.10 respectively. MELE (100 and 300 mg/kg) and omeprazole (10 mg/kg) caused a significant (p < 0.05) reduction in rats’ gastric ulceration with percentage inhibition of 71.05, 76.31 and 78.94% respectively. The extensive ulceration and erosion of the stomachs of rats in the negative control group were reversed by treatment with various doses of the extract and omeprazole. Elevated Ki67 immunoreactivity in the negative control group was also reduced by the MELE (30, 100 and 300 mg/kg) and the standard reference drug, omeprazole (10 mg/kg). The present study suggests that MELE produced no observed adverse effects and offered protection against acidified ethanol-induced gastric ulceration. Further studies should aim at isolating the active compounds responsible for the anti-ulcer effect as well as their possible mechanisms of action.

Ethno Botanical, Pharmacology and Phytochemistry of widely used medicinal plants in Niger: A Review

The plants Cassia italica (Mill.) F.W. Anders, Limeum pterocarpum (L.), Strychnos innocua Del, Ipomoea asarifolia (DESR.) Roem. & Schult, Blepharis linariifolia Pers, Boscia senegalensis (Pers) Lam. Ex Poir, Neocarya macrophylla (Sabine) Prance, Phyllanthus pentandrus Schum & Tonn and Ximenia americanum L belong to different families and are used for the treatment of several pathologies. The aim of this review is to present the current state of research on the ethnopharmacological use of these medicinal plants and to give an overview of the significant results documented. Scientific information about these plants reported were used. Literature review was conducted using search engines and other scientific database websites for chemicals such as ChemSpider, PubChem. Phytochemical work on some of these plants has revealed the presence of several chemical groups and more than 100 compounds have been isolated from some of these plants. The isolated compounds belong to various chemicals classes such as stilbenes, flavonoids, terpenoids, Tannins. Some crude extracts showed a wide spectrum of biological activities, such as antiproliferative, analgesic, anti-inflammatory, antioxidant, antimicrobial and antiplasmodial activities. This review provides an overview of the use, pharmacology and phytochemistry of these plants.

Costus spiralis extract restores kidney function in cisplatin-induced nephrotoxicity model: Ethnopharmacological use, chemical and toxicological investigation

Ethnopharmacological relevanceCostus spiralis (Jacq.). Roscoe (Costaceae) is traditionally used in Brazil for the treatment of kidney diseases such as pyelonephritis, urethra inflammation, kidney stones, and inflammatory conditions. There are reports of its use by Brazilian Indians since the 17th century when it was known as “pacocatinga.” Currently, the use of the Costus species in Brazil is widespread, which was evidenced by the inclusion of the genus in the Brazilian National List of Medicinal Plants of Interest to the Unified Health System (RENISUS). Aim of the studyThis study aimed to confirm the ethnopharmacological use of Costus spiralis in the treatment of kidney diseases, toxicity study using animal models, and the phytochemistry of the species. Materials and methodsThe chemical profile of Costus spiralis leaves extract (CSLE) was obtained for the hydroethanolic extract by ultra-performance liquid chromatography coupled to a mass spectrometer and ultraviolet detector with diode array (UPLC-UV/DAD-ESI-MS). The acute oral toxicity of the extract was predicted using the neutral red uptake cytotoxicity assay. Wistar rats were used in a model in vivo for confirmation of acute oral toxicity (2000 mg/kg p.o. for 14 days.) and determination of the effect on a cisplatin-induced nephrotoxicity model. ResultsThe analysis by UPLC-UV/DAD-ESI-MS showed that the chemical composition of the extract is mostly di-glycosylated flavones of apigenin. In the extract were identified the flavones vicenin II and schaftoside. The quantification of total flavonoids by spectrometry showed 0.880%. CSLE proved to be safe for acute oral administration (2000 mg/kg) with an IC50 value of 222.9 μg/mL and predicted oral toxic dose of 523.82 μg/mL in a neutral red uptake cytotoxicity assay. The absence of death allows the classification of the extract in class 5 according to OECD 423 guidelines and therefore it can be considered as a high acute safety product, which is highly relevant, considering the wide popular use of the species. In the cisplatin-induced nephrotoxicity model, C. spiralis extract (5, 15, and 30 mg/kg) significantly improved renal function, reversing almost completely the effects on plasma creatinine levels and creatinine clearance (p < 0.001). ConclusionsThis study demonstrates that oral administration of Costus spiralis extract leaves is safe and effective in restoring the renal function in rats in a cisplatin-induced nephrotoxicity. It is suggested that the observed activity is related to the flavonoids present. This hypothesis should be confirmed, and the participation of other secondary metabolites should be investigated in the future.

Plants and intestinal parasitosis: a review on ethnopharmacological use by the Kantaruré-Batida indigenous community of Brazil

Indigenous knowledge is one of the most notable traditional sources about plants used to treat diseases. Thus, the aim of this study was to describe the botanical features and to investigate the pharmacological properties of plants used by the Kantaruré-Batida community to treat intestinal parasitosis. Botanical characterization was performed based on integrative review and on access to ‘Flora do Brasil’ platform, whereas plants’ pharmacological properties were investigated through systematic review. Among the 21 ethnospecies used, 48% were described as having activity against intestinal parasites. Although 52% had no such activity described, other properties can account for their use, that indicates that further studies are required. Therefore, this review reinforces the importance of valuing indigenous knowledge as tool to guide antiparasitic agent trials.

Central depressant effects of Piper tuberculatum Jacq essential oil in mice

This study aims to investigate the toxicity and possible effects and mechanism of action of the essential oil obtained from the Piper tuberculatum Jacq.‘s fruit (EOPT) on the central nervous system (CNS) of mice. In the Hippocratic test, it was observed ambulation reduction, sedation, piloerection and mortality of 25% at the dose of 1000 mg/kg and 50% at the dose of 5000 mg/kg. The results found demonstrate that the EOPT is endowed with a possible depressant effect, and is characterized by a likely sedative (open field test), anxiolytic-like (elevated plus maze test), anticonvulsant (pentylenetetrazole-induced seizure test) and hypnotic action (pentobarbital-induced sleeping time). These effects may possibly occur due to the interaction between the monoterpenes, present in its essential oil, and the GABAergic pathway confirmed by reversion of the effects by flumazenil. Then, these results demonstrate the therapeutic potential and the validation of the ethnopharmacological use of this species in the treatment of disorders affecting the central nervous system.

Ameliorative effect of methanolic extract of Tribulus terrestris L. on nicotine and lead-induced degeneration of sperm quality in male rats

Ethnopharmacological relevanceThe use of herbal and medicinal plants to treat male infertility is well known in history. Tribulus terrestris L. (TT) belongs to the Zygophyllaceae family and it is used in folk medicine to vitalize and also improve both physical performance and sexual function in men in addition to the protective effect of the gross saponins of TT against ischemic stroke and its clinical anti-inflammatory property.Aim of the study: This study aimed to investigate the effects of methanol extract of T. terrestris on nicotine hydrogen tartrate and lead-induced degeneration of sperm quality in male rats and to identify the volatile bioactive non-polar compounds thought to be responsible for its activity using gas chromatography-mass spectrometry (GC-MS). Materials and methodsThe effect of T. terrestris on nicotine hydrogen tartrate and lead-induced infertility was evaluated in male rats. Fifty-four mature male albino rats weighing 220–250 g body weight were used. The rats were randomly divided into 9 equal groups (n = 6). Infertility was induced by administering nicotine hydrogen tartrate (0.50 mg/kg) through peritoneal injection (i.p.) or lead acetate (1.5 g/L) orally with drinking water for sixty days. Two doses (50 and 100 mg/kg body weight of the animal) of T. terrestris were also used. At the end of the experimental period, the rats were anesthetized and sacrificed. Blood samples were collected. Hormonal analyses were carried out on the serum. The testicle, epididymis, and accessory sex organs (seminal vesical and prostates) were removed for histopathological analysis. Gas chromatography-mass spectrometry (GC-MS) analysis of the methanol extract was also carried out to identify major volatile compounds in T. terrestris methanol extract. ResultsNicotine and lead toxicity caused a significant (p < 0.05) decrease in the number of sperm, motility, and an increase in the sperm abnormalities such as the reduction in weight and size of sexual organs (testis, epididymis, and accessory sex glands), reduction of diameter and length of seminiferous tubules. The administration of T. terrestris methanol extract, however, improved the semen quantity and quality, sexual organ weights, and fertility of male rats and, thus, ameliorated the adverse effects of nicotine and lead. Ten major compounds were found from the GC-MS analysis of the extract of T. terrestris methanol extract. ConclusionFindings showed that T. terrestris plant methanolic extracts ameliorated nicotine hydrogen tartrate and lead-induced degeneration of sperm quality in male rats. The GC-MS analysis of the T. terrestris plant methanolic extracts revealed the presence of several important bioactive compounds which were thought to be responsible for the ameliorative effect. Further isolation and evaluation of the individual components would provide relevant lead to finding new drugs.

The potency of selected ethnomedicinal plants from East Kalimantan, Indonesia as antidiabetic agents and free-radical scavengers

Abstract. Ramadhan R, Phuwapraisirisan P, Amirta R, Darmawan MFB, Ul-Haq K, Kusuma IW, Suwito H, Abdulgani N, Mukhdlor A, Saparwadi. 2022. The potency of selected ethnomedicinal plants from East Kalimantan, Indonesia as antidiabetic agents and free-radical scavengers. Biodiversitas 23: 2225-2231. Ten ethnomedicinal plant extracts from East Kalimantan flora, traditionally used to treat blood sugar levels and other diabetes-related diseases, were examined in vitro for their antidiabetic and free radical scavenging activities by inhibiting rat alpha-glucosidase and several free radicals such as DPPH, ABTS, and Nitric oxide respectively. Out of the ten plant species investigated for their antidiabetic activity against maltase and sucrase rat alpha-glucosidase, three exhibited the strongest ?-glucosidaseinhibitory activity with maltose as a substrate, namely extracts of Garcinia nervosa, Syzygium caudatilimbum, and Shorea balangeran with IC50 values of 0.046; 0.037; 0.045 mg/mL. Meanwhile, quercetin as a positive control appeared to have a comparable IC50value. Furthermore, among the ten extracts, Syzygium caudatilimbum, Shorea balangeran, and Ixora javanica showed good inhibition against sucrase rat alpha-glucosidase. Moreover, the antioxidant test showed that the ten methanol extracts of plants from East Kalimantan have an antioxidant activity indicated by IC50values. The present study confirms that the ethnopharmacological use of selected plants from East Kalimantan might have potential as an antidiabetic and natural antioxidant.

Anti-adipogenic activity of maackiain and ononin is mediated via inhibition of PPARγ in human adipocytes

Obesity is a global health burden for which we do not yet have effective treatments for prevention or therapy. Plants are an invaluable source of bioactive leads possessing anti-adipogenic potential. Ethnopharmacological use of Ononis spinosa L. roots (OSR) for treatment of obesity and metabolic disorders requires а scientific rationale. The current study examined the anti-adipogenic capacity of OSR and its secondary metabolites ononin (ONON) and maackiain (MACK) in human adipocytes as an in vitro model of obesity. Both ONON and MACK diminished lipid accumulation during adipocyte differentiation. Molecular docking analysis exposed the potential interactions between MACK or ONON and target regulatory adipogenic proteins. Furthermore, results from an RT-qPCR analysis disclosed significant upregulation of AMPK by MACK and ONON treatment. In addition, ONON increased SIRT1, PI3K and ACC mRNA expression, while MACK notably downregulated CEBPA, AKT, SREBP1, ACC and ADIPOQ. The protein level of PI3K, C/EBPα, PPARγ and adiponectin was reduced upon MACK treatment in a concentration-dependent manner. Similarly, ONON suppressed PI3K, PPARγ and adiponectin protein abundance. Finally, our study provides evidence that ONON exerts anti-adipogenic effect by upregulation of SIRT1 and inhibition of PI3K, PPARγ and adiponectin, while MACK induced strong inhibitory effect on adipogenesis via hampering PI3K, PPARγ/C/EBPα signaling and anti-lipogenic effect through downregulation of SREBP1 and ACC. Even though OSR does not hamper adipogenic differentiation, it could be exploited as a source of natural leads with anti-adipogenic potential. The multidirectional mechanism of action of MACK warrant further validation in the context of in vivo obesity models.

Plectranthus zeylanicus: A Rich Source of Secondary Metabolites with Antimicrobial, Disinfectant and Anti-Inflammatory Activities.

Plectranthus zeylanicus Benth is used in Sri Lankan folk medicine as a remedy for inflammatory conditions and microbial infections. Our previous investigations revealed potent 5-lipoxygenase (5-LO) inhibitory activity in lipophilic extracts of this plant, supporting its anti-inflammatory potential. In-depth studies on the antimicrobial activity have not been conducted and the bioactive ingredients remained elusive. As a continuation of our previous work, the present investigation was undertaken to evaluate the antimicrobial activity of different extracts of P. zeylanicus and to isolate and characterize bioactive secondary metabolites. Different organic extracts of this plant were analyzed for their antibacterial activity, and the most active extract, i.e., dichloromethane extract, was subjected to bioactivity-guided fractionation, which led to the isolation of 7α-acetoxy-6β-hydroxyroyleanone. This compound displayed strong antibacterial activity against methicillin-resistant Staphylococcus aureus with a minimum inhibitory concentration of 62.5 µg/mL, and its disinfectant capacity was comparable to the potency of a commercial disinfectant. Moreover, 7α-acetoxy-6β-hydroxyroyleanone inhibits 5-LO with IC50 values of 1.3 and 5.1 µg/mL in cell-free and cell-based assays, respectively. These findings rationalize the ethnopharmacological use of P. zeylanicus as antimicrobial and anti-inflammatory remedy.

Variation in Population and Solvents as Factors Determining the Chemical Composition and Antioxidant Potential of Arctostaphylos uva-ursi (L.) Spreng. Leaf Extracts.

The bearberry Arctostaphylos uva-ursi (L.) Spreng. has a long history of ethnopharmacological use. This species has been used in folk medicine for centuries as a rich source of raw material abundant in secondary metabolites and is important for medicinal and pharmacological purposes. The plant is a source of herbal material—Uvae ursi folium, which is highly valued and sought by pharmaceutical and cosmetic industries. The studied bearberry leaves can be classified as a suitable herbal material for use in pharmacy; therefore, the investigated populations can be a potentially valuable source of plant material for cultivation and can be used in in vitro cultures and in biotechnological processes. The objective of this study was to characterize the variability of the phytochemical composition and antioxidant activity of water and ethanol bearberry extracts from raw material collected from different natural populations. In each of the twelve A. uva-ursi sites, three leaf samples were collected and analyzed. The water extracts from bearberry leaves were characterized by similar concentration of arbutin (77.64–105.56 mg g−1) and a significantly higher concentration of hydroquinone (6.96–13.08 mg g−1) and corilagin (0.83–2.12 mg g−1) in comparison with the ethanol extracts −77.21–103.38 mg g−1, 10.55–16.72 mg g−1, 0.20–1.54 mg g−1, respectively. The concentration of other metabolites in the water extracts was significantly lower in comparison with the ethanol extracts. In the case of the water extracts, a significant effect of not only total phenolic compounds, but also hydroquinone on the antioxidant parameters, was observed, which indicates the solvent-related activity of these metabolites. Therefore, it is suggested that special attention should be paid to the concentration of not only arbutin, but also hydroquinone in Uvae ursi folium. The latter metabolite serving a very important function as an active bearberry ingredient should be controlled not only in alcoholic extracts but also in water extracts, since bearberry leaves are applied as infusions and decoctions. The results presented in this paper can contribute to appropriate selection of plant material for pharmaceutical, cosmetic, and food industries, with special emphasis on the antioxidant activity of different types of extracts.

Gastroprotective effect of hydroalcoholic extract from Agaricus blazei Murill against ethanol-induced gastric ulcer in mice

Ethnopharmacological relevanceThe use of mushrooms in medicine is quite old and the first report about the use of genus Agaricus in treatment of ulcers occurred in Byzantine period. This mushroom is widely consumed as food, tea, food supplements, as well as nutraceutical and cosmeceutical applications, being cultivated and appreciated in several countries such as Brazil, Korea, Japan and China. Aim of the studyThis study aimed to characterize the chemical profile and the potential gastroprotective effect of hydroalcoholic extract from Agaricus blazei Murill (HEAb). Materials and methodsThe extract was chemically characterized by elemental analysis, UPLC-QTOF-MSE, Nuclear Magnetic Resonance (NMR) and high-performance liquid chromatography (HPLC) techniques to elucidate the metabolites present in the extract. The quantification of phenolic compounds and the in vitro antioxidant activities were performed and the gastroprotective effect of this extract was evaluated against ethanol-induced gastric ulcer model. HEAb was administered by gavage at 5, 25 and 50 mg kg−1 and N-acetylcysteine at 300 mg kg−1 (positive control). Furthermore, the pathways of nitric oxide (NO), Cyclic Guanylate Monophosphate (cGMP), prostaglandins (PGs) and the involvement of ATP-sensitive K+ Channels were modulated. ResultsMannitol, malic acid, pyroglutamic acid, L-agaritine and L-valine were putatively identified by UPLC-QTOF-MSE in HEAb. In addition, it was possible to identify mannitol by the intense signals in the NMR spectra, being still quantified as the main compound in the extract by HPLC. The contents of total phenols and flavonoids corroborated with the good antioxidant activity of HEAb. This study observed that HEAb at 25 and 50 mg kg−1 had gastroprotection effect demonstrated by the reduction of histopathological parameters and the reduction of mastocytosis in the stomach of mice. ConclusionsIn this study was possible to conclude that HEAb has gastroprotective effect related to the involvement of NO and PG pathways in the ethanol-induced gastric ulcer model in mice.

Persimmon (Diospyros Kaki) Leaves Extract (PLE): A Potential Drug for Eye-Related diseases

Persimmon (Diospyros kaki) leaves have been used as a traditional or local medicine for multiple diseases in different eastern countries (Japan, Korea, India, and China) for centuries. In the recent past, several studies have used persimmon leaves extract (PLE) against different eye-related diseases. In this review, we discussed the ethnopharmacological use, therapeutic potentials and future opportunities for research using PLE for different ocular disorders based on the latest research. The pieces of information regarding PLE were collected using Pubmed, ACS, Elsevier, EMBASE, Web of Science, CNKI and different books. It can be concluded from this review that PLE probably have therapeutic potential against inflammation and oxidative stress induced disorders like dry eye disease (DED), corneal neurovascularization (CoNV), glaucoma, age-related macular degeneration (AMD), diabetic retinopathy (DR), and edema. However, further investigations are required to discover exact biological compounds involved in the pharmacological effects against the aforementioned diseases. Furthermore, clinical trials are needed to be performed before integrating PLE for medicinal use

Anti-Alzheimer’s and Anti-inflammatory Activities of Compounds Isolated from Solanum Mauritianum

AbstractSolanum mauritianum, commonly known as “Tabaquillo”, was one of the most used plants by tribes from South America as a remedy for headaches. Based on this ethnopharmacological use, a bioguided isolation of compounds with anti-inflammatory and anti-Alzheimer’s activities from S. mauritianum was carried out by measuring the inhibition of NF-κB in C8D1A, Neuro-2a, and EOC 13.31 cells, and by measuring the inhibition of acetylcholinesterase and β-amyloid. This allowed the isolation and characterisation by nuclear magnetic resonance and mass spectrometry of four compounds (1–4). Compounds 1–4 showed NF-κB inhibitory activity with IC50 values of 9.13–9.96, 17.17–17.77, 2.41–2.79, and 1.59–1.93 µM, respectively, while celastrol (the positive control) had an IC50 value of 7.41 µM. Likewise, compounds 1–4 showed anti-Alzheimer’s activity, inhibiting the acetylcholinesterase by 40.33, 20.57, 61.26, and 83.32%, respectively, while galantamine (positive control) showed an inhibition of 90.38%. In addition, concerning the inhibition of β-amyloid aggregation, compounds 1–4 showed an inhibition of 47, 23, 65, and 93%, respectively, while curcumin (positive control) had an inhibition of 71.19%.

Antiviral Effects of Artemisinin and Its Derivatives against SARS-CoV-2 Main Protease: Computational Evidences and Interactions with ACE2 Allelic Variants.

Fighting against the emergent coronavirus disease (COVID-19) remains a big challenge at the front of the world communities. Recent research has outlined the potential of various medicinal herbs to counteract the infection. This study aimed to evaluate the interaction of artemisinin, a sesquiterpene lactone extracted from the Artemisia genus, and its derivatives with the SARS-CoV-2 main protease. To assess their potential use against COVID-19, the interactions of the main active principle of Artemisia with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro) was investigated through in silico probing. Our results showed that artemesinin and its derivatives manifested good oral absorption and bioavailability scores (0.55). They potently bound to the Mpro site of action—specifically, to its Cys145 residue. The selected compounds established two to three conventional hydrogen bonds with binding affinities ranging between −5.2 and −8.1 kcal/mol. Furthermore, artemisinin interactions with angiotensin converting enzyme 2 (ACE2) were dependent on the ACE2 allelic variants. The best score was recorded with rs961360700. A molecular dynamic simulation showed sufficient stability of the artemisinin–Mpro complex on the trajectory of 100 ns simulation frame. These binding interactions, together with drug-likeness and pharmacokinetic findings, confirmed that artemisinin might inhibit Mpro activity and explain the ethnopharmacological use of the herb and its possible antiviral activity against SARS-CoV-2 infection inducing COVID-19. Nevertheless, it interacted differently with the various ACE2 allelic variants reported to bind with the SARS-CoV-2 spike protein.

Etnofarmakološka upotreba čička ("Arctium lappa") u Pirotskom okrugu

The subject of this paper was the investigation of the ethnopharmacological use of burdock (Arctium lappa) in Pirot County (Southeastern Serbia). The research was conducted in the form of surveys among the rural population in four municipalities. It was noticed that fructus and radix were used in the folk medicine of the County for internal and external applications. Fructus was used internalyfor the treatment of diabetes (1 report), diarrhea (2 reports), cancer (1 report), and high blood pressure (1 report); externaly for strengthening hair roots (1 report), against skin diseases (1 report), and rheumatic pain (1 report). It was mentioned that radix was used for internal application for blood purification (1 report). The results showed that its application for the treatment of high blood pressure, and diarrhea were different and new in comparison with other ethnobotanical surveys in Serbia and the Balkan Peninsula.