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This research investigated the effect of Andrographis paniculata (AP) on oxidative stress following indomethacin-induced gastric ulcer in rats. A total of 20 male albino Wistar rats (150-180g) used for this study were grouped into four (n=5): 1, Negative Control; 2, Positive Control and 3, test group treated with normal chow, 20mg/kg indomethacin, 20 mg/kg indomethacin plus omeprazole at 20mg/kg and 20mg/kg indomethacin plus AP at 16.7 mg/kg respectively. After treatment period, estimation of oxidative stress parameters was carried out on the animals. The LD50 of aqueous extract of AP was 50mg/kg bw. Body weight change was significantly reduced in omeprazole treated group compared to all other groups while extract treated group had significantly increased body weight change. There was a significant increase in malondialdehyde (MDA) level of ulcer untreated group compared to other groups. The two treated groups had significantly reduced MDA compared to ulcer untreated group. There was a significant decrease in the levels of GPx and SOD of ulcer untreated group compared to control. Meanwhile, these were significantly increased in extract and omeprazole treated groups compared to ulcer untreated group. Catalase was significantly increased in all three groups when compared to control but its level was significantly increased in extract treated group compared to ulcer untreated and omeprazole treated groups. From this study, AP has proved to protect against oxidative stress implicated in the pathogenesis of ulcer. If this result is applicable to humans, further research and use of AP in ameliorating debilitating consequences of peptic ulcer should be encouraged.
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The last essential enzyme in the biosynthetic pathway of trilobatin, phloretin-4'-O glycosyltransferase (P4'-OGT), catalyzes the conversion of trilobatin to phloretin in vitro. However, only a few P4'-OGTs have been found in plants. This study used Malus domestica phloretin-4'-O glycosyltransferase (MdPh-4'-OGT) as a query to identify and clone two UDP-glucuronosyltransferase (UGT) genes, designated UGT74L2 and UGT74L3, from the transcriptome of Andrographis paniculata. According to a phylogenetic tree analysis, UGT74L2 and UGT74L3 belonged to the UGT74 family, which has been linked to several activities in other species. The in vitro enzymatic reaction demonstrated that UGT74L2 could particularly catalyze the formation of trilobatin from phloretin, but UGT74L3 had no effects. By using Ni-NTA affinity chromatography to extract the soluble UGT74L2 recombinant protein, the enzymatic kinetics of the activity was investigated using phloretin as the substrate. The results showed that the optimal temperature and pH for UGT74L2 enzymatic reaction were 40 ℃ and 8.0 (Tris-HCl system), respectively. Three metal ions (Ca2+, Mn2+ and Co2+) showed inhibitory effect on the activity of UGT74L2, while Mg2+ could improve the activity of UGT74L2. Other tested metal ions have no significant effect on UGT74L2. The results of enzymatic kinetic parameters that the Km value was 29.84 μmol·L-1, the kcat was 0.02 s-1, and the kcat·Km-1 was 572.6 mol-1·s-1. By homology modeling, molecular docking and mutation experiments, we found that multiple amino acids residues around the substrate binding pocket play quite an important role during catalytic process, In summary, we identified a novel P4'-OGT gene from medicinal plant Andrographis paniculata and provided a new efficient catalyst to synthesize trilobatin. Meanwhile, this study provides a reference for mining new efficient glycosylation modules from plants.
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ObjectiveTo study the effect of a microbial compound fertilizer on the growth， quality， and soil properties of Andrographis paniculata and provide a basis for its application in the cultivation and production of A. paniculata. MethodThrough five treatment tests in pots， the control group （CK， no fertilization）， the treatment A group （chemical fertilization）， the treatment B group （microbial fertilization at 2.5 g·kg-1 soil）， the treatment C group （microbial fertilization at 7.5 g·kg-1 soil）， and the treatment D group （microbial fertilization at 12.5 g·kg-1 soil） were established. The effects of a compound microbial fertilizer on the agronomic properties， the content of active ingredients， the number of rhizosphere soil bacteria， Actinomycetes， and fungi， and soil physicochemical properties of A. paniculata were studied. ResultAs compared with the CK group and the treatment A group， the plant height， leaf number， leaf area， and above-ground and below-ground fresh weight of A. paniculata were significantly increased after microbial fertilization， with differences in different growth periods. The effect of the compound microbial fertilizer on the content of andrographolide， dehydrated andrographolide， neandrographolide， and 14-deoxyandrographolide differed. The content of andrographolide significantly increased by 26.13% and 13.23% in the treatment C group， respectively， as compared with the CK group and the treatment A group （P<0.05）. The content of neandrographolide increased with the increasing amount of microbial fertilizer， and the content in the treatment D group increased by 9.06% and 50.33%， respectively， as compared with the CK group and the treatment A group （P<0.05）， which was the most obvious. The content of 14-deoxyandrographolide in the treatment B group significantly increased by 42.04% and 1.74%， respectively， as compared with the treatment A group and the CK group （P<0.05）. The content of dehydrated andrographolide content in the treatment B group increased most significantly， significantly increasing by 11.73% and 27.74%， respectively， as compared with the CK group and the treatment A group （P<0.05）. The soil pH of the treatment B， C， and D groups was higher than that of the CK group and the treatment A group. The content of total nitrogen and effective phosphorus increased most significantly in the treatment B group， and the content of fast-acting potassium increased most significantly in the treatment D group. The application of the compound microbial fertilizer increased the number of rhizosphere soil bacteria and Actinomycetes， which was significantly higher than that in the CK group and the treatment A group （P<0.05）， and increased with the increase of applied amount. The number of fungi decreased with the increase of the compound microbial fertilizer application， which was significantly different from that in the CK group （P<0.05）. The fungi/bacteria of all treatment groups were significantly lower than those of the CK group （P<0.05） and increased with the increase of microbial fertilizer application. ConclusionThe application of the compound microbial fertilizer transforms the plant-soil-microbial system in a benign direction， which is beneficial to the growth of A. paniculata and the accumulation of active ingredients.
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Background: Nowadays, myocardial infarction has been regarded as one of the chronic diseases with increasing mortality rate worldwide. The use of medicinal plants in the treatment of this chronic disease is gaining wide acceptance globally. Materials and Methods: This study was carried out to evaluate the cardio-protective effect of the leaf extract of A. paniculata in isoproterenol-induced myocardial infarction. Fresh green leaves of A paniculata were collected from the Faculty of Agriculture farmland, Nnamdi Azikiwe University, Awka, Nigeria. The plant was identified and authenticated at the Department of Botany, Nnamdi Azikiwe University and a voucher specimen was deposited at the herbarium accordingly. The shredded, air-dried sample was then pulverized and weighed. Solvent-solvent (ethanol and water) (7:3) was used for extraction via maceration for 72 hr. The filtrate was evaporated to dryness to obtain the ethanol extract which was used for further bioassay study. The bioactive constituents of the plant extract were quantitatively analyzed by Gas chromatography mass spectrometry (GC-MS). The animals were administered with the extract of A. paniculata orally for seven days at a divided dose of 100 mg/kg, 200 mg/kg and 400 mg/kg body weights. On the eight day, myocardial infarction was induced through subcutaneous administration of isoproterenol at a dose of 150 mg/kg/day diluted in 2 ml of saline on two consecutive days. Subsequently, the blood pressures were monitored and blood collected for bioassay studies. Results: The results of the study showed that the leaf extract of A. paniculata was rich in 2,5-Octadecadiynoic acid, methyl ester (28.21%); 1,2,3,5-Cyclohexanetetrol,(1à,2á,3à,5á)- (15.10 %) and 10-12-Pentacosadiynoic acid (13.05%). The findings also showed a significant decrease (p>0.05) in the Mean arterial blood pressure, heart rate, aspartate transaminase, alanine transaminase, creatinine kinase and lactate dehydrogenase activities of the treatment group compared with the untreated control group while the antioxidant (superoxide dismutase, catalase and glutathione) activities were significantly increased in the treatment group, compared with the untreated control group. Conclusion: The findings of this work have shown that leaf of A. paniculata was rich in bioactive compounds which could be synthesized to produce plant based products to combat cardiovascular diseases especially myocardial infarction.
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Data on Traditional Medicine Practice (TMP) in population with access to modern medicine is not clear, though, it has gained huge popularity in all regions of developing countries over decades. This research was conducted to investigate the Knowledge, Attitude and Practice (KAP) of people using Andrographis paniculata (Burm. f.) Nees as a medical herb and the effects of the crude extracts on some microbial isolates. Quantitative-based cross-sectional survey was carried out on 100 participants around Auta-Baleifi and Bingham University communities through the use of structured questionnaires. Data collected from the participants were analyzed using descriptive statistics. The plant species leaves were collected, washed and extracted by boiling, soaking and macerating using distilled water. The crude extracts were tested for its antimicrobial activities on Salmonella typhi, Escherichia coli and Staphylococcus aureus using ciprofloxacin as the control. From the result of the KAP analysis, majority (36%) of the participants were between 19-28 years old, followed by 29 � 38 years (32%) and only 5% were 59 years and above . 91% of the participants have good knowledge of traditional medicine, while only 9% were not aware of the practice , 32.0% of the participant claimed that the use of traditional medicine preparation had no adverse effects as compared to modern medicine,, while larger percentage (68%), do not agree that traditional medicine is safer than modern medicine., 36% of the participants claimed to have used A. paniculata, a traditional herb, for one medicinal purpose or the other, while 54% said they have never used it, but may considered using it in future,. The population in Auta-baleifi and Bingham University communities has good knowledge with high acceptability of the use of traditional medicine. Although the result of the antimicrobial showed that the crude extracts of A. paniculata had no clear zone of inhibition against the test organisms, but the plant have demonstrated effective used in traditional medicine against symptoms very similar to that of malaria.
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Natural products and their semi synthesized molecules have been used as efficient antibiotics since a long time. The present global health scenario has raised the demand for novel antimicrobial agents and drug targets that are effective against drug resistant pathogens, emerging infections etc. The current study has promoted the antibacterial activity of the glucoside labdane ‘neoandrographolide’, isolated from the methanolic extract of the medicinal plant Andrographis paniculata. Further modification at its glucoside hydroxyl groups to generate ester and acetonide derivatives was done and the antibacterial potential of these compounds was screened against common bacterial pathogens. Among various derivatives, 4?,6?-O-(4-methoxybenzylidene) neoandrographolide exhibited promising results. In addition, molecular modeling study of the active compound was also explored to identify its probable binding mode on the bacterial target. The present study reported antibacterial activity of neoandrographolide derivatives for first time and also the bioactive molecule, 4?,6?-O-(4-methoxybenzylidene) neoandrographolide was examined as a potent antibacterial agent against different strains.
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Andrographis Herba, the aerial part of Andrographis paniculata (Burm. f.) Wall. ex Nees (Acanthaceae), has a wide geographic distribution and has been used for the treatment of fever, cold, inflammation, and other infectious diseases. In markets, sellers and buyers commonly inadvertently confuse with related species. In addition, most Chinese medicinal herbs are subjected to traditional processing procedures, such as steaming and boiling, before they are sold at dispensaries; therefore, it is very difficult to identify Andrographis Herba when it is processed into Chinese medicines. The identification of species and processed medicinal materials is a growing issue in the marketplace. However, conventional methods of identification have limitations, while DNA barcoding has received considerable attention as a new potential means to identify species and processed medicinal materials. In this study, 17 standard reference materials of A. paniculata, 2 standard decoctions, 27 commercial products and two adulterants were collected. Based on the ITS2 sequence, it could successfully identify A. paniculata and adulterants. Moreover, a nucleotide signature consisting of 71 bp was designed, this sequence is highly conserved and specific within A. paniculata while divergent among other species. Then, we used these new primers to amplify the nucleotide signature region from processed materials. In conclusion, the DNA barcoding method developed in the present study for authenticating A. paniculata is rapid and cost-effective. It can be used in the future to guarantee the quality of Andrographis Herba of each regulatory link for clinical use.
Subject(s)
Andrographis , Andrographis paniculata , DNA Primers , Drugs, Chinese HerbalABSTRACT
The plant growth, development, and secondary metabolism are regulated by R2 R3-MYB transcription factors. This study identified the R2 R3-MYB genes in the genome of Andrographis paniculata and analyzed the chromosomal localization, gene structure, and conserved domains, phylogenetic relationship, and promoter cis-acting elements of these R2 R3-MYB genes. Moreover, the gene expression profiles of R2 R3-MYB genes under abiotic stress and hormone treatments were generated by RNA-seq and validated by qRT-PCR. The results showed that A. paniculata contained 73 R2 R3-MYB genes on 21 chromosomes. These members belonged to 34 subfamilies, 19 of which could be classified into the known subfamilies in Arabidopsis thaliana. The 73 R2 R3-MYB members included 36 acidic proteins and 37 basic proteins, with the lengths of 148-887 aa. The domains, motifs, and gene structures of R2 R3-MYBs in A. paniculata were conserved. The promoter regions of these genes contains a variety of cis-acting elements related to the responses to environmental factors and plant hormones including light, ABA, MeJA, and drought. Based on the similarity of functions of R2 R3-MYBs in the same subfamily and the transcription profiles, ApMYB13/21/35/67/73(S22) may regulate drought stress through ABA pathway; ApMYB20(S11) and ApMYB55(S2) may play a role in the response of A. paniculata to high temperature and UV-C stress; ApMYB5(S7) and ApMYB33(S20) may affect the accumulation of andrographolide by regulating the expression of key enzymes in the MEP pathway. This study provides theoretical reference for further research on the functions of R2 R3-MYB genes in A. paniculata and breeding of A. paniculata varieties with high andrographolide content.
Subject(s)
Andrographis paniculata , Gene Expression Regulation, Plant , Genes, myb , Multigene Family , Phylogeny , Plant Proteins/metabolismABSTRACT
ObjectiveTo screen the appropriate reference genes for real-time fluorescence-based quantitative polymerase chain reaction（Real-time PCR）analysis of the Andrographis paniculata under methyl jasmonate（MeJA）and various abiotic stresses. MethodThe actin 1（ACT1），actin 2（ACT2），elongation factor（EF-1α），glyceraldehyde-3-phosphate dehydrogenase（GAPDH），tubulin（TUB），polyubiquitin（UBQ）， and 18S rRNA（18S）gene were selected as candidate reference genes based on the RNA-seq data of high temperature，drought， UV， and MeJA. The expression of seven candidate reference genes in the A. paniculata leaves was assessed by Real-time PCR，and the stability was analyzed by geNorm，NormFinder，BestKeeper， and Refinder. ResultThe results of stability evaluated by geNorm，NormFinder， and BestKeeper were not the same due to different indicators. As analyzed by Refinder， for the stability of the expression， the genes were ranked as UBQ>18S>EF-1α>ACT2>ACT1>GAPDH>TUB under high temperature stress， ACT1>UBQ>EF-1α>18S>ACT2>GAPDH>TUB under drought stress， EF-1α>TUB>ACT2>UBQ>18S>GAPDH>ACT1 under UV stress， and ACT1>EF-1α>UBQ>ACT2>18S>TUB>GAPDH under MeJA stress. Among them，18S gene was not suitable as an internal reference gene duo to its high expressive abundance. This study also verified the relative expression level of andrographolide synthesis-related gene hydroxy-methylglutaryl-CoA synthase （HMGS） in the four stresses on the basis of transcriptome data，and found that the Real-time PCR results of appropriate internal reference genes were accurate and reliable. ConclusionUBQ-ACT1-UBQ，EF-1α-TUB，and ACT1-EF-1α were the suitable combinations under stresses of high temperature，drought，UV， and MeJA. This study is expected to provide references for the research on function regulation and expression of genes in A. paniculata under high temperature，drought，UV， and MeJA stresses.
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Aims@#Andrographis paniculata (AP), a medicinal herb was selected to investigate the antifungal activity on selected dermatophyte fungi. The phytochemical screening was also carried out to evaluate its chemical constituents.@*Methodology and results@#The potato dextrose agar (PDA) incorporated with aqueous, ethanol and methanol AP extracts at concentrations 0.99% (v/v), 1.96% (v/v) and 7.41% (v/v) were used for selected fungi culturing; Trichophyton mentagrophytes, T. rubrum, T. interdigitale, Microsporum fulvum, M. nanum, M. gypseum, M. canis, Fusarium solani and Aspergillus fumigatus. Phytochemical screening showed the presence of flavonoids, saponins and tannins in the ethanol extract and flavonoids alone in both aqueous and methanol extracts. Studies on antifungal effects indicated that the ethanol extract significantly increased the mycelial inhibition percentage of all tested fungi, especially at a concentration of 7.41% (v/v). All ethanol AP extract concentrations inhibited M. gypseum and M. canis (p<0.05) with at least 36.00% mycelial inhibition. In aqueous AP extract, it significantly increased the mycelial inhibition of T. mentagrophytes, T. interdigitale and M. gypseum (p<0.05), while the methanol AP extract significantly inhibited all fungi at a concentration of 7.41% (v/v) except for T. rubrum, M. gypseum and F. solani (p<0.05). No spore sedimentation was recorded for the fungal spores of T. rubrum, M. nanum, T. mentagrophytes, M. gypseum and T. interdigitale at 7.41% (v/v) ethanol AP. @*Conclusion, significance and impact of study@#It is concluded that the ethanol AP extract contained phytochemical constituents and showed the highest antifungal activity. In addition, this extract has a great potential to treat dermatophytes effectively.
Subject(s)
Antifungal Agents , Phytochemicals , Andrographis paniculata , DermatomycosesABSTRACT
Aims@#Acne is a common skin disease among teenagers and also affects other ages. It occurs when the oil and dead skin cells plug into the hair follicles and causing pimples or whitehead. Although antibiotics have been used for many years in treating acne, the widespread use of it has led to the development of bacterial resistant, which resulted in unsuccessful treatment. Thus, in this study, Andrographis paniculata (AP) herbal formulation gel is proposed in order to determine its effectiveness in treating acne. Three different methodologies were used to compare the antimicrobial effect of A. paniculata herbal gel against acne-associated pathogens. @*Methodology and results@#Well diffusion, disc diffusion and broth dilution methods were applied to evaluate the antimicrobial effect of AP herbal gel at concentrations of 1.5% (w/w), 2.5% (w/w) and 5.0% (w/w) onto selected pathogens associated with acne which consisted of Staphylococcus epidermidis, Staphylococcus aureus, Propionibacterium acnes and Candida albicans. Among the three methods, broth dilution showed the best antimicrobial effect towards all microorganisms used. AP herbal gel at concentration 2.5% (w/w) showed the optimum antimicrobial effect of S. aureus and C. albicans, while 5.0% (w/w) exhibited the best antimicrobial activities for P. acnes and S. epidermidis. @*Conclusion, significance and impact of study@#Broth dilution method appears to be a reliable method for the determination of antimicrobial effects for the pathogens tested. In addition, AP herbal formulation gel has great potential to treat acne effectively.
Subject(s)
Anti-Infective Agents , Andrographis paniculataABSTRACT
Objective: Andrographis paniculata is a well-known medicinal plant in Southeast Asia, India and China. The plant contains andrographolide (AN), a very important phytochemical used in various health problems. However, AN is low in oral absorption bioavailability of AN due to the rapid clearance and high protein binding capacity. Methods: The present study was aimed to develop a nano-phytovesicular formulation of semi-purified AN extracts from a naturally occurring phospholipid (soya phosphatidylcholine) in order to increase the oral absorption and antihyperglycemic activity in rats. Results: The nano-phyto vesicle of semi-purified AN extracts equivalent to 25 mg /kg AN significantly protected the hyperglycemic condition of rats. The in vitro and in vivo experiments results proved that the nano- phytovesicular system of plant extracts containing AN produced better oral absorption, bioavailability and improved antihyperglycemic activity compared with that of free AN at dose of 50 mg/kg. Conclusion: Hence, the prepared semi-purified extract nano-phytovesicular system is helpful in solving the problem of rapid clearance of AN.
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Dengue is a debilitating disease that poses a perpetual threat to human health and increases the global economic burden every year. Despite advances in medical sciences, dengue virus (DENV) infects approximately 200 million people every year. To date, no effective antiviral is valiable to treat DENV in individuals despite great efforts in accomplishing these goals. Numerous approaches have been used in the search for dengue antiviral like screening of combinatorial compounds against DENV enzymes and structure-based computational discovery. In recent years, investigators have turned their focus into medicinal plants, trying to identify compounds that can be used as dengue antiviral. Nature represents a great reservoir of potential substances that can be explored with the aim of discovering new drugs that can be either used directly as pharmaceuticals or can provide drug leads, which can be scrutinized further for the development of new anti-dengue natural product. Many previous investigations have dealt with numerous plant extracts or bioactive principles for their antiviral property as they normally considered being safer when compared to synthetic drugs. Andrographis paniculata belongs to family Acanthaceae and is generally known as 'king of bitters'. Diverse bioactive compounds from this plant such as diterpenes, flavonoids, xanthones, noriridoides and other miscellaneous compounds have exhibited their potential as therapeutics for various chronic as well as infectious diseases. This review is based on literature review on scientific journals, books and electronic sources, which highlights the pathogenesis of DENV and describe an assortment of bioactive principles that have been possessing antiviral potential, which include dengue and discuss the therapeutic efficacy and mechanism of action of Andrographis paniculata. However, a detailed and more comprehensive clinical trial on mammalian tissues and organs is needed in future studies.
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In this study, Andrographis paniculata seedlings were used as experimental materials to study the effects of salicylic acid(SA) on the growth and effective component accumulation of A. paniculata under NaCl stress. The results showed that with the increase of NaCl concentration, the growth of A. paniculata seedlings was significantly inhibited, and the content of carotene and carotenoid decreased. The activity of antioxidant enzyme was enhanced. At the same time, the contents of proline, proline and soluble protein were on the rise. The contents of andrographolide, new andrographolide and deoxyandrographolide showed an upward trend, while deoxyandrographolide showed a downward trend. Treatment with 100 mmol·L~(-1) NaCl+5 mg·L~(-1) SA showed a significant increase in antioxidant enzyme activity in A. paniculata leaves. Treatment with 100 mmol·L~(-1) NaCl+10 mg·L~(-1) SA showed significant changes in soluble protein and proline content in A. paniculata leaves, while MDA content in A. paniculata leaves significantly decreased. 10 mg·L~(-1) SA had the best effect on the growth of A. paniculata seedlings under salt stress. Under the treatment of 50 mmol·L~(-1) NaCl+10 mg·L~(-1) SA, fresh weight, dry weight and leaf dry weight of A. paniculata seedlings reached the highest level, which were 1.02, 1.09 and 1.11 times of those in the control group, respectively. The concentrations of NaCl and 10 mg·L~(-1) SA were significantly higher than those of the control group. Four key enzyme genes of A. paniculata diterpene lactone synthesis pathway were selected to explore the molecular mechanism of salicylic acid to alleviate salt stress. With the increase of salt stress, the relative expressions of HMGR, GGPS and ApCPS were up-regulated, indicating that salt stress may enhance the synthesis of A. paniculata diterpene lactone through MVA pathway. SA can effectively promote the growth and development of A. paniculata under salt stress, improve its osmotic regulation and antioxidant capacity, improve its salt tolerance, and alleviate the effects of salt stress on A. paniculata.
Subject(s)
Andrographis , Plant Leaves , Salicylic Acid , Salt Tolerance , Seedlings/geneticsABSTRACT
To investigate the effect of Polygonum multiflorum-Andrographis paniculata intercropping system on rhizosphere soil actinomycetes of P. multiflorum, the community structure and diversity of soil actinomycetes were studied by using the original soil as the control group and the rhizosphere soil actinomycetes communities of P. multiflorum under monoculture and intercropping systems as the experimental group. In this study 655 221 effective sequences were obtained with an average length of 408 bp. OTU coverage and rarefaction curve showed that the sequencing could represent the real situation of soil actinomycetes. According to the results of alpha diversity analysis, the diversity soil actinomycetes varied as follows: original soil>intercropping soil>monoculture soil. The soil actinomycetes community structure and the relative abundance of dominant genera were significantly changed by both monoculture and intercropping, especially monoculture. OTU clustering and PCA analysis of soil samples showed that all the soil samples were divided into three distinct groups and the original soil was more similar to intercropping soil. In addition, intercropping increased the relative abundance of some beneficial actinomyces, such as Kitasatospora and Mycobacterium, which was beneficial to maintain soil health and reduce the occurrence of soil-borne diseases. The results show that, P. multiflorum-A. paniculata intercropping reduced the change of community structure and the decrease of diversity of soil actinomycetes caused by P. multiflorum monoculture, and made the actinomycete community in rhizosphere soil of P. multiflorum close to the original soil.
Subject(s)
Actinobacteria , Actinomyces , Agriculture , Andrographis , Fallopia multiflora , Rhizosphere , Soil , Soil MicrobiologyABSTRACT
Dengue is a debilitating disease that poses a perpetual threat to human health and increases the global economic burden every year. Despite advances in medical sciences, dengue virus (DENV) infects approximately 200 million people every year. To date, no effective antiviral is valiable to treat DENV in individuals despite great efforts in accomplishing these goals. Numerous approaches have been used in the search for dengue antiviral like screening of combinatorial compounds against DENV enzymes and structure-based computational discovery. In recent years, investigators have turned their focus into medicinal plants, trying to identify compounds that can be used as dengue antiviral. Nature represents a great reservoir of potential substances that can be explored with the aim of discovering new drugs that can be either used directly as pharmaceuticals or can provide drug leads, which can be scrutinized further for the development of new anti-dengue natural product. Many previous investigations have dealt with numerous plant extracts or bioactive principles for their antiviral property as they normally considered being safer when compared to synthetic drugs. Andrographis paniculata belongs to family Acanthaceae and is generally known as 'king of bitters'. Diverse bioactive compounds from this plant such as diterpenes, flavonoids, xanthones, noriridoides and other miscellaneous compounds have exhibited their potential as therapeutics for various chronic as well as infectious diseases. This review is based on literature review on scientific journals, books and electronic sources, which highlights the pathogenesis of DENV and describe an assortment of bioactive principles that have been possessing antiviral potential, which include dengue and discuss the therapeutic efficacy and mechanism of action of Andrographis paniculata. However, a detailed and more comprehensive clinical trial on mammalian tissues and organs is needed in future studies.
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The study was conducted to determine the antipyretic and anti-inflammatory activity of the methanolic extract of Andographispaniculata (APE) in albino rats. Acute oral LD50 of APE in female rats was more than 2000 mg/kg. The antipyretic activitywas studied by inducing pyrexia with Brewer’s yeast. A total number of thirty albino rats (200 g) were used for the study ofanti-pyretic activity they were divided into five groups of six rats in each group. Group I served as control Normal saline andGroup II were given brewer’s yeast alone (20 ml/kg), Group III was administered standard drug Aspirin @ 100 mg /kg bodywt. while groups IV and V were treated with 200 mg/kg and 400 mg/kg of Andrographis paniculata extract respectively.Pyrexia was induced by subcutaneously injecting 20% w/v brewer’s suspension in below the nape of the neck of the animals.The anti-inflammatory activity of APE was assessed by measuring the reduction in carrageenan-induced paw oedema in rats.A twenty four albino rats (200 g) were used for the study of anti-inflammatory activity. Four groups were divided with six ratsin each group. Group I served as control Normal saline solution and Group II was administered standard drug phenylbutazone@ 100 mg/kg While, groups III and IV were treated with 200mg/kg and 400mg/kg of APE respectively. APE (@ 400 mg/kghad significant antipyretic and anti-inflammatory activity against reduced brewer’s yeast induced pyrexia and carrageenaninduced rat paw edema in rats suggesting potent antipyretic effect of APE. From these results it may be concluded that crudemethanolic extract of Andrographis paniculata have significant antipyretic activity and anti-inflammatory activity that mightbe due to combined effect of active constituents present in plant extract this strongly support the ethno pharmacologicaluse of the plant for the management of fever and inflammation
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The anti-venom activity of Andrographis paniculata (Burm.f.) Nees roots (APR) dichloromethane crude extractsand a promising APR constituent, skullcapflavone I (SKI) was investigated by monitoring the inhibition of secretoryphospholipase A2 (sPLA2) of Naja philippinensis Taylor venom (NPV) crystallized samples. Gas chromatographymass spectrometry was used for the characterization of extracts, while molecular docking was utilized to understandanti-venom properties. Chromatographic analyses primarily revealed the presence of methoxylated flavones. NPV wasfound to have sPLA2 activity (0.0796 ± 0.0018 μmol/minutes/ml) that has been attributed to the poisonous effects.SKI (IC50: 51.1 ± 3.5 μg/ml), isolated from APR showed strong inhibitory effect on phospholipase activity comparedwith dichloromethane extracts of APR (IC50: 192.7 ± 10.9 μg/ml) indicating that SKI was the cause of the bioactivityin APR. Molecular docking simulations showed corresponding results with highly negative binding energies (−6.59 to−8.72 kcal/mol) predicted for the binding of SKI to PLA2 proteins. An important trend found was the presence of freebound Ca2+ lowered binding energies signifying that Ca2+ a has role in the binding of the SKI to PLA2 proteins. Theanti-venom property of APR and the pure compound SKI, upon further studies, could be the first line of defense in themedical protocol of snake venom neutralization.
ABSTRACT
The anti-venom activity of Andrographis paniculata (Burm.f.) Nees roots (APR) dichloromethane crude extractsand a promising APR constituent, skullcapflavone I (SKI) was investigated by monitoring the inhibition of secretoryphospholipase A2 (sPLA2) of Naja philippinensis Taylor venom (NPV) crystallized samples. Gas chromatographymass spectrometry was used for the characterization of extracts, while molecular docking was utilized to understandanti-venom properties. Chromatographic analyses primarily revealed the presence of methoxylated flavones. NPV wasfound to have sPLA2 activity (0.0796 ± 0.0018 μmol/minutes/ml) that has been attributed to the poisonous effects.SKI (IC50: 51.1 ± 3.5 μg/ml), isolated from APR showed strong inhibitory effect on phospholipase activity comparedwith dichloromethane extracts of APR (IC50: 192.7 ± 10.9 μg/ml) indicating that SKI was the cause of the bioactivityin APR. Molecular docking simulations showed corresponding results with highly negative binding energies (−6.59 to−8.72 kcal/mol) predicted for the binding of SKI to PLA2 proteins. An important trend found was the presence of freebound Ca2+ lowered binding energies signifying that Ca2+ a has role in the binding of the SKI to PLA2 proteins. Theanti-venom property of APR and the pure compound SKI, upon further studies, could be the first line of defense in themedical protocol of snake venom neutralization.
ABSTRACT
Objective: To isolate and characterize the endophytic fungi from the leaves of Andrographis paniculata for free radical scavenging antioxidant and hepatoprotective activity against CCl4 induced hepatotoxicity Methods: Two fungal endophytes, APLF-3 (Andrographis paniculata leaf fungi-3) and APLF-4 (Andrographis paniculata leaf fungi-4) were isolated from leaves of Andrographis paniculata to get chloroform (A3C, A4C), ethyl acetate (A3EA, A4EA) and n butanol (A3nB, A4nB) extracts. rDNA sequencing by PCR technique was carried out for identification of APLF-3 and APLF-4. All the APLF-3 and APLF-4 extracts were assayed for in vitro free radical scavenging activity against 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl radical and reducing power. Then, A4EA and A4nB were screened for hepatoprotective activity against CCl4 induced hepatotoxicity at 50 mg/kg and100 mg/kg doses. Results: The endophytic fungi, APLF-3 and APLF-4, were identified as Phyllosticta sp. ZLY-2010 isolate M13 and Aspergillus tubingensis strain Cs/7/2 respectively based on their morphological and molecular characterization. A4EA and A4nB showed significant in vitro free radical scavenging activity as compared to other extracts. A4EA and A4nB (50 mg/kg and100 mg/kg) reversed the increased serum biochemical parameters as compared to CCl4 treated group (p<0.001). A4EA and A4nB (100 mg/kg p. o) also restored the LPO, SOD and CAT levels. Conclusion: These findings suggested that the extracts (A4EA and A4nB) obtained from endophytic fungi APLF-4 contributed towards hepatoprotective activity.