RESUMO
The present study investigated the antioxidant potential of aqueous methanolic extracts of Hemidesmus indicus (L.) R.Br., followed by a pharmacoinformatics-based screening of novel Keap1 protein inhibitors. Initially, the antioxidant potential of this plant extract was assessed via antioxidant assays (DPPH, ABTS radical scavenging, and FRAP). Furthermore, 69 phytocompounds in total were derived from this plant using the IMPPAT database, and their three-dimensional structures were obtained from the PubChem database. The chosen 69 phytocompounds were docked against the Kelch-Neh2 complex protein (PDB entry ID: 2flu, resolution 1.50 Å) along with the standard drug (CPUY192018). H. indicus (L.) R.Br. extract (100 µg × mL-1) showed 85 ± 2.917%, 78.783 ± 0.24% of DPPH, ABTS radicals scavenging activity, and 161 ± 4 µg × mol (Fe (II)) g-1 ferric ion reducing power. The three top-scored hits, namely Hemidescine (-11.30 Kcal × mol-1), Beta-Amyrin (-10.00 Kcal × mol-1), and Quercetin (-9.80 Kcal × mol-1), were selected based on their binding affinities. MD simulation studies showed that all the protein-ligand complexes (Keap1-HEM, Keap1-BET, and Keap1-QUE) were highly stable during the entire simulation period, compared with the standard CPUY192018-Keap1 complex. Based on these findings, the three top-scored phytocompounds may be used as significant and safe Keap1 inhibitors, and could potentially be used for the treatment of oxidative-stress-induced health complications.
Assuntos
Antioxidantes , Hemidesmus , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Hemidesmus/química , Hemidesmus/metabolismo , Proteína 1 Associada a ECH Semelhante a Kelch/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo , Extratos Vegetais/químicaRESUMO
The present study evaluated the antibacterial and antibiofilm activity of methanolic extract of Hemidesmus indicus root (MHIR) in combination with amoxicillin and clindamycin against biofilm-forming methicillin-resistant Staphylococcus aureus (MRSA) isolated from milk samples of mastitic cows. Microdilution susceptibility testing and microtitre plate assays were used to evaluate the in vitro efficacy of MHIR and antibiotic combinations against MRSA (n = 12). Furthermore, in vitro findings were validated in a murine model. Minimum inhibitory concentration and minimum biofilm inhibitory concentration of amoxicillin and clindamycin in combination with MHIR were significantly (P < 0·05) lower than when used alone against MRSA. In terms of antibacterial activity, MHIR showed additive interaction (fractional inhibitory concentrationindex >0·5-4) with amoxicillin and clindamycin against all the MRSA isolates, whereas MHIR synergizes (fractional biofilm inhibitory concentrationindex ≤0·5) the antibiofilm activity of amoxicillin and clindamycin against 58·33% and 83·33% of the MRSA isolates respectively. Amoxicillin/clindamycin in combination with MHIR significantly (P < 0·05) reduced disease activity score, and bacterial load and Gram-positive spots in kidney and liver of MRSA-infected mice. The combined efficacy of MHIR and amoxicillin/clindamycin was comparable to clindamycin alone but superior to amoxicillin alone. Hence, the combination of MHIR with amoxicillin/clindamycin is advocated in the treatment of MRSA-associated infections.
Assuntos
Hemidesmus , Staphylococcus aureus Resistente à Meticilina , Infecções Estafilocócicas , Feminino , Bovinos , Animais , Camundongos , Clindamicina/farmacologia , Amoxicilina/farmacologia , Metanol , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana , Biofilmes , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/veterinária , Infecções Estafilocócicas/microbiologiaRESUMO
The aim of this study was to determine the content of rutin in Hemidesmus indicus and to optimize the high-performance thin-layer chromatography method. The method was validated in compliance with the International Council for Harmonisation guidelines Q2 (R1) for parameters such as linearity, accuracy, precision, robustness, limit of detection, and limit of quantitation. A Box-Behnken design and response surface methodology has been used to investigate the impact of independent variables on the response. Three independent variables, mobile phase composition (% v/v), mobile phase volume (mL), and duration of saturation (min), were studied. Rutin was verified, and its content was determined using a validated high-performance thin-layer chromatography method with good linearity within the range of 200-1000 ng spot-1 with r2 = 0.9998 and correlation coefficient with calibration curve equation y = 0.0297x + 0.0001. The average percentage recovery values varied from 99.03 to 101.15 and 98.88 to 100.12%, respectively, for in-house and marketed mother tincture). The peak area determination at three different concentration levels shows low values of percentage relative standard deviation (<2%) for inter-day (0.04-0.06) and intra-day (0.04-0.05) precision of rutin. The average content of rutin in extract and marketed mother tincture was 229 ± 0.57 and 210 ± 0.57 µg g-1 . The proposed method was simple, precise, and accurate for the determination of rutin with frequent quality control assessment of H. indicus.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Cromatografia em Camada Fina/métodos , Hemidesmus/química , Extratos Vegetais/química , Rutina/análise , Limite de Detecção , Modelos Lineares , Reprodutibilidade dos Testes , Projetos de PesquisaRESUMO
Hemidesmus indicus (L.) R. Br. ex Schult., commonly known as Indian sarsaparilla or Anantamul, is an ethnopharmacologically important medicinal plant from the family Apocynaceae. Biosynthesis of an array of bioactive compounds such as methoxybenzaldehydes and their derivatives has been accountable for its intensive medicinal attributes. Low seed setting, over-exploitation from natural habitat and a need for selection and preservation of elite germplasms yielding higher levels of bioactive compounds have led researchers to enquire the standardization of micropropagation techniques and quantitative estimation of phytochemicals from H. indicus. The present work aims to have a comprehensive account on micropropagation in H. indicus, a comparative estimation of biotic and abiotic factors, viz. elicitors and precursors playing a crucial role in H. indicus tissue culture, a critical appraisal of applied protocols to nullify embellished claims and a discussion on future perspectives. The review also highlights the comparative effect of different plant growth regulators as well as their combined role in rhizogenesis, callogenesis, base callus formation, callusing and somatic embryo-mediated indirect organogenesis, outcome of explant selection, contribution of abiotic (temperature, photoperiod, moisture, inorganic molecules) factors, role of carbon source, application of sterilization techniques and associated success rates, role of factors essential for acclimatization and secondary metabolite production, synthetic seed production and genetic transformation techniques. The compiled information along with individual study details, respective outcome and variability of reports will aid in proper assessment of cited standardized tissue culture protocols in H. indicus especially in relation to secondary metabolite production. Moreover, the assessment of applicability of different methodologies in this aspect will aid in the selection of high-yielding germplasms or chemotypes which is not only profitable for industrial application but also important for basic and applied preclinical and clinical research studies. KEY POINTS: ⢠Critical and updated assessment on in vitro biotechnology in Hemidesmus indicus. ⢠Biotechnological advancement via Agrobacterium-mediated transformation. ⢠Key shortcomings and future research directions Graphical abstract Effect of biotic and abiotic factors on Micropropagation and secondary metabolite synthesis in Hemidesmus indicus.
Assuntos
Hemidesmus , Plantas Medicinais , Biotecnologia , Compostos Fitoquímicos , Extratos Vegetais , Raízes de PlantasRESUMO
Hemidesmus indicus (L.) R. Br. ex Schult is commonly known as anantmul or Indian sarsaparilla. The roots of this plant, which display a wide range of medicinal, biological, and phytopharmaceutical properties, are used in the pharmaceutical and food industries. Conventionally, the plant is propagated by seed germination or vegetatively, but the efficacy of traditional methods has some limitations: plants derived from seed germination are prone to seed-borne diseases, or plantlet production using vegetative propagation is limited. In contrast, plant tissue culture allows for large-scale propagation and secondary metabolite production in vitro without sacrificing plants from their natural habitats. Many efforts have been made over 40 years of research to establish efficient micropropagation protocols to speed up cultivation of this plant, including callus-mediated in vitro propagation, somatic embryogenesis, and shoot multiplication using cotyledenory nodes, stem segments, shoot tips, and nodal explants. Among these explants, nodal explants are the most commonly used for H. indicus micropropagation. The application of adenine sulfate, citric acid, ascorbic acid, and arginine may be useful in preventing explant browning, premature leaf senescence, and shoot tip abscission during in vitro culture. This review provides insight into micropropagation, use of synthetic seeds for short-term germplasm preservation, and in vitro production of secondary metabolites such as 2-hydroxy-4-methoxybenzaldehyde, lupeol, vanillin, and rutin, from in vitro root and callus cultures. Furthermore, unexplored and possible innovative areas of research in Hemidesmus biotechnology are also discussed. KEY POINTS: ⢠Hemidesmus indicus has multiple therapeutic applications. ⢠H. indicus roots are used in confectionary and pharmacy. ⢠This review comprehensively assesses H. indicus tissue culture. ⢠Challenges and future research of H. indicus biotechnology are discussed.
Assuntos
Biotecnologia/métodos , Hemidesmus/química , Extratos Vegetais/química , Técnicas de Cultura de Tecidos/métodos , Hemidesmus/crescimento & desenvolvimento , Raízes de Plantas/química , Metabolismo SecundárioRESUMO
Staphylococcus epidermidis (SE) is an opportunistic nosocomial pathogen that accounts for recalcitrant device-related infections worldwide. Owing to the growing interest in plants and their secondary metabolites targeting bacterial adhesion, this study was intended to uncover the anti-biofilm potential of Hemidesmus indicus and its major constituent 2-hydroxy-4-methoxybenzaldehyde (HMB) against SE. The minimum biofilm inhibitory concentration (MBIC) of H. indicus root extract and HMB were found to be 500 and 250 µg ml-1, respectively. The results of time-dependent biofilm inhibition and mature biofilm disruption assays confirmed that HMB targets initial cell adhesion. Furthermore, interference by HMB in the expression of adhesin genes (icaA, aap and bhp) and biofilm components was associated with an increased susceptibility of SE to oxidative stress and antibiotics. To conclude, this study reports for the first time HMB as a potential drug against SE biofilms.
Assuntos
Antibacterianos/toxicidade , Benzaldeídos/toxicidade , Biofilmes/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos , Hemidesmus , Humanos , Infecções EstafilocócicasRESUMO
BACKGROUND: Fungal endophytes are the living symbionts which cause no apparent damage to the host tissue. The distribution pattern of these endophytes within a host plant is mediated by environmental factors. This study was carried out to explore the fungal endophyte community and their distribution pattern in Asparagus racemosus and Hemidesmus indicus growing in the study area. RESULTS: Foliar endophytes were isolated for 2 years from A. racemosus and H. indicus at four different seasons (June-August, September-November, December-February, March-May). A total of 5400 (675/season/year) leaf segments harbored 38 fungal species belonging to 17 genera, 12 miscellaneous mycelia sterile from 968 isolates and 13 had yeast like growth. In A. racemosus, Acremonium strictum and Phomopsis sp.1, were dominant with overall relative colonization densities (RCD) of 7.11% and 5.44% respectively, followed by Colletotrichum sp.3 and Colletotrichum sp.1 of 4.89% and 4.83% respectively. In H. indicus the dominant species was A. strictum having higher overall RCD of 5.06%, followed by Fusarium moniliforme and Colletotrichum sp.2 with RCD of 3.83% and 3%, respectively. Further the overall colonization and isolation rates were higher during the wet periods (September-November) in both A. racemosus (92.22% and 95.11%) and H. indicus (82% and 77.11%). CONCLUSION: Study samples treated with 0.2% HgCl2 and 75% EtOH for 30 s and 1 min, respectively, confirmed most favorable method of isolation of the endophytes. Owing to high mean isolation and colonization rates, September-November season proved to be the optimal season for endophyte isolation in both the study plants. Assessing the bioactive potential of these endophytes, may lead to the isolation of novel natural products and metabolites.
Assuntos
Asparagus/microbiologia , Endófitos/fisiologia , Fungos/fisiologia , Hemidesmus/microbiologia , Microbiota , Endófitos/classificação , Fungos/classificação , Índia , Folhas de Planta/microbiologia , Estações do AnoRESUMO
Herpes simplex virus types 1 (HSV-1) and 2 (HSV-2) cause several clinically relevant syndromes in both adults and neonates. Despite the availability of efficient anti-HSV agents, the search for new therapeutic approaches is highly encouraged due to the increasing drug resistance of virus strains. Medicinal plants represent a source of potential bioactive compounds. In this context we evaluated the anti-herpetic activity of Hemidesmus indicus (L.) R. Br., a plant widely used in traditional Indian medicine. The hydroalcoholic extract prepared from roots was characterized by NMR and HPLC analysis and assayed in vitro by CPE reduction and virus infectivity assays to define its anti-viral effect. The extract's mechanism of action was investigated by virucidal and time-of-addition assays and by in vitro α-glucosidase inhibitory assay. The extract exhibited a remarkable anti-herpetic activity at 100 mg/mL, at non-cytotoxic concentration, through multiple mechanisms: it reduced the infectivity of viral particles released from infected cells possibly through its anti-ER α-glucosidase inhibitory activity and it inhibited the beginning stage of HSV infection acting as a virucide agent and/or preventing virus attachment to the host cell surface.
Assuntos
Hemidesmus/química , Herpesvirus Humano 1/fisiologia , Herpesvirus Humano 2/fisiologia , Extratos Vegetais/farmacologia , Replicação Viral/efeitos dos fármacos , Animais , Antivirais/química , Antivirais/farmacologia , Sobrevivência Celular , Chlorocebus aethiops , Relação Dose-Resposta a Droga , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Herpesvirus Humano 1/efeitos dos fármacos , Herpesvirus Humano 2/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Células Vero , alfa-Glucosidases/metabolismoRESUMO
In the present investigation, we described the green synthesis of silver nanoparticles using plant leaf extract of Hemidesmus indicus. The synthesized silver nanoparticles were characterized by UV-visible spectroscopy, fourier transform infra-red spectroscopy (FTIR), X-ray diffraction (XRD), transmission electron microscopy (TEM) and energy dispersive X-ray spectroscopy (EDX). TEM images proved that the synthesized silver nanoparticles were spherical in shape with an average particle size of 25.24 nm. To evaluate antibacterial efficacy, bacteria was isolated from poultry gut and subjected to 16S rRNA characterization and confirmed as Shigella sonnei. The in vitro antibacterial efficacy of synthesized silver nanoparticles was studied by agar bioassay, well diffusion and confocal laser scanning microscopy (CLSM) assay. The H. indicus mediated synthesis of silver nanoparticles shows rapid synthesis and higher inhibitory activity (34 ± 0.2 mm) against isolated bacteria S. sonnei at 40 µg/ml.
Assuntos
Antibacterianos/metabolismo , Hemidesmus/metabolismo , Nanopartículas/metabolismo , Shigella sonnei/efeitos dos fármacos , Prata/metabolismo , Animais , Antibacterianos/farmacologia , Trato Gastrointestinal/microbiologia , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Transmissão , Nanopartículas/química , Nanopartículas/microbiologia , Extratos Vegetais/metabolismo , Folhas de Planta/metabolismo , Aves Domésticas , Shigella sonnei/isolamento & purificação , Prata/química , Prata/farmacologia , Análise Espectral , Difração de Raios XRESUMO
Indian Sarsaparilla (Hemidesmus indicus R. Br.) is widely used in Indian traditional medicine. In the present work, we explored the effects of decoction, traditional Ayurvedic preparation, and hydroalcoholic extract, a phytocomplex more traditionally studied and commercialized as food supplement in western medicine, from the roots as possible source of chemicals with new functional potential linked to their nutritional uses. The antiproliferative and antioxidant properties were assayed. To test antiproliferative affects, different cancer cell lines, growing both as monolayers (CaCo2, MCF-7, A549, K562, MDA-MB-231, Jurkat, HepG2, and LoVo) and in suspension (K562 and Jurkat) were used. The decoction showed strong activity on HepG2 cells, while the hydroalcoholic extracts were active on HepG2, LoVo, MCF-7, K562, and Jurkat cell lines. Weak inhibition of cancer cell proliferation was observed for the principal constituents of the preparations: 2-hydroxy-4-methoxybenzaldehyde, 2-hydroxy-4-methoxybenzoic acid, and 3-hydroxy-4-methoxybenzaldehyde that were tested alone. The antiradical activity was tested with 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)diammonium salt tests and inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 macrophages. Interesting result has also been obtained for hydroalcoholic extract regarding genoprotective potential (58.79% of inhibition at 37.5 µg/mL).
Assuntos
Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Hemidesmus/química , Extratos Vegetais/farmacologia , Animais , Linhagem Celular Tumoral/efeitos dos fármacos , Flavonoides/química , Humanos , Macrófagos/efeitos dos fármacos , Ayurveda , Camundongos , Extratos Vegetais/química , Raízes de Plantas/química , Polifenóis/química , Proantocianidinas/químicaRESUMO
The complete DNA A genome of a virus isolate associated with yellow mosaic disease of a medicinal plant, Hemidesmus indicus, from India was cloned and sequenced. The length of DNA A was 2825 nucleotides, 35 nucleotides longer than the unit genome of monopartite begomoviruses. Comparison of the nucleotide sequence of DNA A of the virus isolate with those of other begomoviruses showed maximum sequence identity of 69 % to DNA A of ageratum yellow vein China virus (AYVCNV; AJ558120) and 68 % with tomato yellow leaf curl virus- LBa4 (TYLCV; EF185318), and it formed a distinct clade in phylogenetic analysis. The genome organization of the present virus isolate was found to be similar to that of Old World monopartite begomoviruses. The genome was considered to be monopartite, because association of DNA B and ß satellite DNA components was not detected. Based on its sequence identity (<70 %) to all other begomoviruses known to date and ICTV (International Committee on Taxonomy of Viruses) species demarcating criteria (<89 % identity), it is considered a member of a novel begomovirus species, and the tentative name "Hemidesmus yellow mosaic virus" (HeYMV) is proposed.
Assuntos
Begomovirus/genética , Begomovirus/isolamento & purificação , Hemidesmus/virologia , Sequência de Aminoácidos , Sequência de Bases , Genoma Viral , Índia , FilogeniaRESUMO
Eleven decoctions, obtained from indian plants widely used in ayurvedic medicine, have been investigated as a possible source of molecules exhibiting biological activity on the interaction between DNA and NF-kB, a transcription factor involved in the expression of proinflammatory genes. Cystic fibrosis (CF) cell line stimulated by TNF-α has been used as inflammatory cellular model to determinate interleukin-8 (IL-8), one of the most relevant pro-inflammatory mediator in CF regulated by the NF-kB. The chemical characterization of these 11 decoctions by spectrophotometric analysis and NMR fingerprinting highlighted that sugars and polyphenols seemed to be the main compounds. Our results demonstrated that Azadirachta indica, Terminalia bellerica, Terminalia chebula, Hemidesmus indicus, Emblica officinalis and Swertia chirata are the most active decoctions in inhibiting NF-kB/DNA interactions by EMSA assay and in reducing pro-inflammatory IL- 8 expression in CF cells at IC50 concentrations by Real-Time and Bio-plex analyses. Finally, we observed the increase of all inhibitory activities with the rise of total polyphenols, procyanidins and flavonoids, except for the levels of IL-8 mRNA accumulation, that were as high as flavonoid content grown up by the statistical multivariate analyses. In conclusion, these six decoctions might be interesting to explore new anti-inflammatory treatments for diseases, such as CF.
Assuntos
Interleucina-8/metabolismo , Ayurveda , Extratos Vegetais/farmacologia , Azadirachta/química , Linhagem Celular , Fibrose Cística , Hemidesmus/química , Humanos , NF-kappa B/metabolismo , Phyllanthus emblica/química , Extratos Vegetais/química , Polifenóis/química , Swertia/química , Terminalia/química , Fator de Necrose Tumoral alfa/farmacologiaRESUMO
OBJECTIVES: To evaluate the antioxidant potential of porridges (kola kenda) made incorporating herbs. DESIGN: Experimental study. Main outcome measures Total phenolic content was estimated by Folin Ciocalteau method (GAEmg/g(FW) and the antioxidant potential by ABTS free radical scavenging activity (TEAC(µg)/100g (FW). RESULTS: Total phenolics and antioxidant potentials of porridges ranged from 5-73 TEAC(µg) /100g and 0.9- 34.2 GAEg/100g respectively. Significantly high (p ≤ 0.05) total phenolic contents were observed in C. auriculata ("Ranawara") [342 GAE mg/g (FW)] and in M. koenigii ("Karapincha") [199 GAEmg/g(FW)]. The highest antioxidant effect was in C. auriculata ("Ranawara") [73 TEAC(µg)/100g(FW)] followed by M. koenigi ("Karapincha") [26 TEAC(µg)/100g (FW)] and C. ternatea ("Ela Katarolu") [24 TEAC(µg)/100g (FW)]. Lowest antioxidant effect was in porridges made with rice and coconut milk both of which had comparable values. A positive correlation (correlation coefficient > 0.8) between total phenolics and the antioxidant potential was observed for all porridges except for Asparagus racemosus (Haathawariya) porridge which had a high antioxidant potential with a low phenolic content. CONCLUSIONS: This study provides evidence that green leafy porridges are a good source of antioxidants in addition to their reported low glycaemic indices.
Assuntos
Antioxidantes/farmacologia , Diabetes Mellitus/terapia , Sequestradores de Radicais Livres/farmacologia , Fenóis/farmacologia , Preparações de Plantas/farmacologia , Aegle , Amaranthaceae , Asparagus , Cassia , Clitoria , Cocos , Hemidesmus , Humanos , Medicina Tradicional , Murraya , Oryza , Fenóis/análise , Preparações de Plantas/química , Sapindaceae , Scoparia , Sri LankaRESUMO
The root of Hemidesmus indicus R. Br., commonly known as Indian Sarsaparilla, is used traditionally to treat a wide variety of illnesses including rheumatism, leprosy, impotence, urinary tract and skin infections. The anticancer, antioxidant, anti-inflammatory, antipyretic, analgesic, antimicrobial, antidiabetic, hepatoprotective, cardioprotective, renoprotective, neuroprotective and immunomodulatory properties of H. indicus have been investigated in numerous in vivo and in vitro studies. Among these, the antioxidant and antimicrobial activity was well documented. This review details the phytochemistry and therapeutic applications of H. indicus root.
Assuntos
Hemidesmus/química , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Células Cultivadas , Humanos , Fitoterapia , Extratos Vegetais/química , Raízes de Plantas/químicaRESUMO
Acetylcholinesterase inhibitors (AChEIs) are important for treatment of Alzheimer's disease and other neurological disorders. Search for potent and safe AChEIs from plant sources still continues. In the present work, we explored fragrant plant extracts that are traditionally used in flavoring foods, namely, Hemidesmus indicus and Vanilla planifolia, as possible sources for AChEI. Root and pod extracts of H. indicus and V. planifolia, respectively, produce fragrant phenolic compounds, 2-hydroxy-4-methoxybenzaldehyde (MBALD) and 4-hydroxy-3-methoxybenzaldehyde (vanillin). These methoxybenzaldehydes were shown to have inhibitory potential against acetylcholinesterase (AChE). Vanillin (IC50 = 0.037 mM) was detected as more efficient inhibitor than MBALD (IC50 = 0.047 mM). This finding was supported by kinetic analysis. Thus, plant-based food flavoring agents showed capacity in curing Alzheimer's disease and other neurological dysfunctions.
Assuntos
Inibidores da Colinesterase/farmacologia , Aromatizantes/química , Hemidesmus/química , Extratos Vegetais/farmacologia , Vanilla/química , Doença de Alzheimer/tratamento farmacológico , Benzaldeídos/farmacologia , Aditivos Alimentares , Cinética , Doenças do Sistema Nervoso/tratamento farmacológico , Fitoterapia , Raízes de Plantas/química , Sementes/químicaRESUMO
Hemidesmus indicus (L.) R. Br. ex Schult. and Tylophora indica (Burm. F.) Merrill shoot cultures were treated with different concentrations of yeast extract (YE; 25-200 mg/L) and salicylic acid (SA; 50-200 µM), and their effect on lupeol production was assessed. The maximum dry weight (DW) biomass was recorded when H. indicus shoots were treated with SA (50 µM) and T. indica shoots with YE (200 mg/L). Highest lupeol yield (335.40 ± 0.04 µg/g DW) was obtained in H. indicus shoots after treatment with 50 µM of SA for 3 weeks. Whereas in T. indica, maximum lupeol content (584.26 ± 8.14 µg/g DW) was recorded by giving treatment with 25 µM of SA for 6 weeks.
Assuntos
Hemidesmus , Tylophora , Ácido Salicílico/farmacologia , Biomassa , Triterpenos Pentacíclicos/farmacologiaRESUMO
This study delved into the exploration of novel antidiabetic medications acquired from natural resources, utilizing the Ayurvedic Rasayana herb Hemidesmus indicus through cutting-edge chemoprofiling and molecular modelling techniques. The methanolic extract of Hemidesmus indicus root exhibited the highest extractive yield (24.70 ± 0.08 %) and contained substantial levels of total phenolic and flavonoid content as 154.15 ± 1.24 mg Gallic Acid Equivalent/g extract and 70.61 ± 0.35 Quercetin Equivalent/g extract respectively. Invitro study revealed the potent inhibitory potential of methanolic extract of the herb against essential carbohydrate hydrolytic enzymes α-amylase (IC50 = 4.19 ± 0.04 mg/ml) and α-glucosidase (IC50 = 5.78 ± 0.10 mg/ml). Further, the enzyme kinetic study demonstrated the competitive mode of inhibition of both enzymes. HR-LCMS analysis identified the major phytoconstituents present in the extracts, including Solanocapsine, Cyclovirobuxine C, Lucidine B, Zygadenine, Aspidospermidine, silychristin, 3beta-3-Hydroxy-18-lupen-21-one, Manglupenone, and 19-Noretiocholanolone. Molecular docking, molecular dynamic simulation, and MM/GBSA analysis have proved stable, rigid, compact, and folded form of complexes during the entire 100 ns simulation, illustrating Zygadenine, Solanocapsine, and Cyclovirobuxine C as the superior inhibitors of α-A protein, while Zygadenine, Plumieride, and Phlegmarine exhibited greater inhibitory behaviour towards α-G protein than the FDA-approved drug acarbose. Collectively, our findings indicate that the Hemidesmus indicus could be a promising source of α-A and α-G inhibitors, potentially serving as a lead in order to develop medications for type-2 diabetes.
Assuntos
Diabetes Mellitus Tipo 2 , Hemidesmus , Humanos , Extratos Vegetais/farmacologia , Simulação de Acoplamento Molecular , Hipoglicemiantes/farmacologiaRESUMO
Ethanolic extracts of Cynodon dactylon, Aloe vera, Hemidesmus indicus and Coleus amboinicus were tested for their toxicity effect on the third-instar larvae of Anopheles stephensi, Culex quinquefasciatus and Aedes aegypti. The leaves of C. dactylon, A. vera, H. indicus and C. amboinicus were collected from natural habitats (forests) in Western Ghats, Tamil Nadu, India. A total of 250 g of fresh, mature leaves were rinsed with distilled water and dried in shade. The dried leaves were put in Soxhlet apparatus and extract prepared using 100% ethanol for 72 h at 30-40°C. Dried residues were obtained from 100 g of extract evaporated to dryness in rotary vacuum evaporator. Larvicidal properties of ethanolic leaf extracts showed that the extracts are effective as mosquito control agents. The larval mortality was observed after 24 h exposure. No mortality was observed in the control. The median lethal concentration (LC(50)) values observed for the larvicidal activities are 0.44%, 0.51%, 0.59% and 0.68% for extracts of C. dactylon, A. vera, H. indicus and C. amboinicus, respectively. The observed mortality were statistically significant at P < 0.05 level. C. dactylon showed the highest mortality rate against the three species of mosquito larvae in laboratory and field. The selected plants were shown to exhibit water purification properties. Water quality parameters such as turbidity, pH and water clarity were analyzed in the water samples (pre-treatment and post-treatment of plant extracts) taken from the different breeding sites of mosquitoes. Water colour, turbidity and pH were reduced significantly after treatment with C. dactylon (13 HU, 31.5 mg/l and 6.9), H. indicus (13.8 HU, 33 mg/l and 7.1), A. vera (16 HU, 33.8 mg/l and 7.4) and C. amboinicus (21 HU, 35 mg/l and 7.5) extracts. The study proved that the extracts of C. dactylon, A. vera, H. indicus and C. amboinicus have both mosquitocidal and water sedimentation properties.
Assuntos
Aloe/química , Coleus/química , Cynodon/química , Hemidesmus/química , Inseticidas/química , Extratos Vegetais/química , Purificação da Água/métodos , Aedes/efeitos dos fármacos , Animais , Anopheles/efeitos dos fármacos , Culex/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Índia , Inseticidas/análise , Larva/efeitos dos fármacos , Dose Letal Mediana , Controle de Mosquitos/métodos , Extratos Vegetais/análise , Folhas de Planta/química , Qualidade da ÁguaRESUMO
BACKGROUND: A standardized poly-herbal decoction of Nigella sativa seeds, Hemidesmus indicus roots and Smilax glabra rhizomes used traditionally in Sri Lanka for cancer therapy has been demonstrated previously, to have anti-hepatocarcinogenic potential. Cytotoxicity, antioxidant activity, anti-inflammatory activity, and up regulation of p53 and p21 activities are considered to be some of the possible mechanisms through which the above decoction may mediate its anti-hepatocarcinogenic action. The main aim of the present study was to determine whether apoptosis is also a major mechanism by which the decoction mediates its anti-hepatocarcinogenic action. METHODS: Evaluation of apoptosis in HepG2 cells was carried out by (a) microscopic observations of cell morphology, (b) DNA fragmentation analysis, (c) activities of caspase 3 and 9, as well as by (d) analysis of the expression of pro-apoptotic (Bax) and anti-apoptotic (Bcl-2) proteins associated with cell death. RESULTS: The results demonstrated that in HepG2 cells, the decoction can induce (a) DNA fragmentation and (b) characteristic morphological changes associated with apoptosis (nuclear condensation, membrane blebbing, nuclear fragmentation and apoptotic bodies). The decoction could also, in a time and dose dependent manner, up regulate the expression of the pro-apoptotic gene Bax and down regulate expression of anti-apoptotic Bcl-2 gene (as evident from RT-PCR analysis, immunohistochemistry and western blotting). Further, the decoction significantly (p < .001) enhanced the activities of caspase-3 and caspase-9 in a time and dose dependent manner. CONCLUSIONS: Overall findings provide confirmatory evidence to demonstrate that the decoction may mediate its reported anti-hepatocarcinogenic effect, at least in part, through modulation of apoptosis.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/tratamento farmacológico , Hemidesmus , Neoplasias Hepáticas/tratamento farmacológico , Nigella , Smilax , Antineoplásicos Fitogênicos/uso terapêutico , Carcinoma Hepatocelular/genética , Carcinoma Hepatocelular/metabolismo , Caspase 3/metabolismo , Caspase 9/metabolismo , Núcleo Celular/efeitos dos fármacos , Fragmentação do DNA , Relação Dose-Resposta a Droga , Regulação para Baixo , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células Hep G2 , Humanos , Neoplasias Hepáticas/genética , Neoplasias Hepáticas/metabolismo , Fitoterapia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Raízes de Plantas , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Padrões de Referência , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Rizoma , Sementes , Proteína X Associada a bcl-2/genética , Proteína X Associada a bcl-2/metabolismoRESUMO
Protective effect was evaluated in streptozoticin (STZ)-induced diabetes rats. 2-Hydroxy 4-methoxy benzoic acid (HMBA) was isolated from the roots of Hemidesmus indicus and administered (500 microg/kg body weight) orally for 7 weeks to STZ-induced diabetic and non-diabetic rats to study its effect on protein metabolism, serum electrolytes and on liver and kidney lipid peroxides. Oral administration of HMBA restored the altered biochemical parameters such as urea, uric acid, creatinine, plasma proteins and serum electrolytes to near-normal levels. HMBA treatment significantly decreased lipid peroxidation and malondialdehyde levels in diabetic liver and kidney. Effect of HMBA was equivalent to that of the standard drug, tolbutamide (100 mg/kg body wt). The histological changes were also in correlation with the biochemical findings. The present study showed that HMBA isolated from H. indicus roots had ameliorative effect on liver, kidney and pancreatic injury in STZ-induced diabetic rats.