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Inactivation of enveloped viruses by anthraquinones extracted from plant
Antimicrobial Agents and Chemotherapy
Abstract
To determine the extent of antiviral activity present in a number of plant extracts, hot glycerin extracts were prepared from
Rheum officinale, Aloe barbadensis, Rhamnus frangula, Rhamnus purshianus, and Cassia angustifolia and their virucidal effects
were tested against herpes simplex virus type 1. All the plant extracts inactivated the virus. The active components in these
plants were separated by thin-layer chromatography and identified as anthraquinones. A purified sample of aloe emodin was
prepared from aloin, and its effects on the infectivity of herpes simplex virus type 1 and type 2, varicella-zoster virus,
pseudorabies virus, influenza virus, adenovirus, and rhinovirus were tested by mixing virus with dilutions of aloe emodin
for 15 min at 37 degrees C, immediately diluting the sample, and assaying the amount of infectious virus remaining in the
sample. The results showed that aloe emodin inactivated all of the viruses tested except adenovirus and rhinovirus. Electron
microscopic examination of anthraquinone-treated herpes simplex virus demonstrated that the envelopes were partially disrupted.
These results show that anthraquinones extracted from a variety of plants are directly virucidal to enveloped viruses.
... Importantly, aloe-emodin is a natural anthraquinone derivative found in the rhizome and root of Rheum palmatum [118]. It has demonstrated inhibition of the replication of EV71 [119], human cytomegalovirus (HCMV) [120], HSV [120], and influenza virus (IAV) [121]. These findings suggest a potential starting point for the development of novel broad-spectrum antivirals based on anthraquinone [118]. ...
... Importantly, aloe-emodin is a natural anthraquinone derivative found in the rhizome and root of Rheum palmatum [118]. It has demonstrated inhibition of the replication of EV71 [119], human cytomegalovirus (HCMV) [120], HSV [120], and influenza virus (IAV) [121]. These findings suggest a potential starting point for the development of novel broad-spectrum antivirals based on anthraquinone [118]. ...
Japanese encephalitis virus (JEV) belongs to the Flaviviridae family and is a representative mosquito-borne flavivirus responsible for acute encephalitis and meningitis in humans. Despite the availability of vaccines, JEV remains a major public health threat with the potential to spread globally. According to the World Health Organization (WHO), there are an estimated 69,000 cases of JE each year, and this figure is probably an underestimate. The majority of JE victims are children in endemic areas, and almost half of the surviving patients have motor or cognitive sequelae. Thus, the absence of a clinically approved drug for the treatment of JE defines an urgent medical need. Recently, several promising and potential drug candidates were reported through drug repurposing studies, high-throughput drug library screening, and de novo design. This review focuses on the historical aspects of JEV, the biology of JEV replication, targets for therapeutic strategies, a target product profile, and drug development initiatives.
... 14.94 Altersolanol A An anthraquinone derivative, Anthraquinones can inactivate enveloped viruses [27] A potential inhibitor for COVID-19 by docking study [28] [25] HIV-1 shares similar mode of actions with SARS for viral entry [26] transforming [29] . No obvious evidence points out its potentiality in deactivating COVID-19. ...
... Altersolanol A is an anthraquinone derivative. Anthraquinones can inactivate enveloped viruses [27] , and it is a potential inhibitor for COVID-19 according to a docking study [28] . Alterporriol G/H is a tetrahydroanthraquinone derivative and some tetrahydroanthraquinones have anti-viral activity [24] . ...
Many efforts have been exerted toward screening potential drugs for targets, and conducting wet experiments remains a laborious and time-consuming approach. Artificial intelligence methods, such as Convolutional Neural Network (CNN), are widely used to facilitate new drug discovery. Owing to the structural limitations of CNN, features extracted from this method are local patterns that lack global information. However, global information extracted from the whole sequence and local patterns extracted from the special domain can influence the drugtarget affinity. A fusion of global information and local patterns can construct neural network calculations closer to actual biological processes. This paper proposes a Fingerprint-embedding framework for Drug-Target binding Affinity prediction (FingerDTA), which uses CNN to extract local patterns and utilize fingerprints to characterize global information. These fingerprints are generated on the basis of the whole sequence of drugs or targets. Furthermore, FingerDTA achieves comparable performance on Davis and KIBA data sets. In the case study of screening potential drugs for the spike protein of the coronavirus disease 2019 (COVID-19), 7 of the top 10 drugs have been confirmed potential by literature. Ultimately, the docking experiment demonstrates that FingerDTA can find novel drug candidates for targets. All codes are available at http://lanproxy.biodwhu.cn:9099/mszjaas/FingerDTA.git.
... SARS-CoV and Vero E6 cell inter-action was also blocked by preincubating S protein or S protein-pseudo typed retrovirus with emodin. These findings suggested that emodin could prevent SARS-CoV infection by blocking the S protein-ACE2 interaction site [56] , in addition to disrupting the viral envelope ( Figure 10). ...
... Promazine possesses anti-SARS characteristics via blocking viral entry and protein processing, according to these results. [56][57][58][59][60] With a K1/2 value of roughly 20 M, emodin can inhibit the 3a ion channel of coronaviruses SARS-CoV and HCoV-OC43, as well as virus discharge from HCoV-OC43, according to Schwarz et al. Viral ion channels, they say, could be a suitable target for antiviral drug development. ...
Coronavirus spreads from human to human or human to animal via airborne droplets. Coronavirus penetrates human cells via the membrane ACE-2 exopeptidase receptor. There are no specific anti-virus medi- cations or vaccinations available to treat this sudden and fatal sickness during COVID-19 except vaccination. Still, it will take months, if not years, to create these antiviral drug therapies to combat against this pandemic. Phytochemicals have a huge significant anti-inflammatory activity, which can reduce lung injury like major inflammation occurring in the lungs of a covid19 patient. To improve the symptoms of COVID-19 infected patients, supportive care and non-specific treatment are now required. As an alternate measure, fast application of herbal medicine or phyto-chemicals can help with this specific indication. Phytochemicals are a potent class of compounds generated from plants that have less adverse effects due to the lack of additives, preservatives, and excipients. The new COVID19 variants are much dangerous than the early ones which is a major drawback for the early developed vaccines. As a result, the focus of this review will be on certain phytochemicals and their mechanism of action that may be used to manage and prevent SARS-CoV-2 and its major variants emerging nowadays.
... A. vera extracts have also exhibited dose-dependent inhibitory effects on herpes simplex virus 1 and 2 (HSV1 and HSV2) in vitro [9,10]. Interestingly, hot glycerin extract from A. vera gel was able to inhibit the pre-entry, entry, and post-attachment stages of HSV2 infection, suggesting multiple targets in the HSV2 replication cycle. ...
... A seminal study performed by Sydiskis et al. showed that AEM reduced the infectivity of several enveloped viruses, namely, HSV1, HSV2, varicella-zoster virus (VZV), pseudorabies virus, and influenza A virus (IAV) without apparent cytotoxic effects in vitro ( Table 2) [9]. Transmission electron microscopy revealed that preincubation with anthraquinones, including AEM, disrupted the HSV1 envelope, suggesting that AEM may be used against enveloped viruses to destroy the lipid envelope. ...
Plants contain underutilized resources of compounds that can be employed to combat viral diseases. Aloe vera (L.) Burm. f. (syn. Aloe barbadensis Mill.) has a long history of use in traditional medicine, and A. vera extracts have been reported to possess a huge breadth of pharmacological activities. Here, we discuss the potential of A. vera compounds as antivirals and immunomodulators for the treatment of viral diseases. In particular, we highlight the use of aloe emodin and acemannan as lead compounds that should be considered for further development in the management and prevention of viral diseases. Given the immunomodulatory capacity of A. vera compounds, especially those found in Aloe gel, we also put forward the idea that these compounds should be considered as adjuvants for viral vaccines. Lastly, we present some of the current limitations to the clinical applications of compounds from Aloe, especially from A. vera.
... However, autophagy can also be activated as a cytoprotective mechanism against chemotherapeutic agents. In which, autophagy counteracts the action of apoptosis Anthraquinone derivatives were proven to possess antifungal, antibacterial [22,23,24,25,26] and in vitro antiviral activity [27,28,29]. Anthraquinones are also used in the treatment of other diseases and already available in the market [30]. ...
... Due to this effect, emodin decreases the HER-2/neu tyrosine kinase (Receptor tyrosine-protein kinase erbB-2) which is involved in the development of chemoresistance. Anthraquinone derivatives were proven to possess antifungal, antibacterial [22][23][24][25][26] and in vitro antiviral activity [27][28][29]. Anthraquinones are also used in the treatment of other diseases and already available in the market [30]. Senna glycosides are previously proven to have a stimulant laxative effect [15,31,32]. ...
Anthraquinone derivatives exhibit various biological activities, e.g., antifungal, antibacterial and in vitro antiviral activities. They are naturally produced in many fungal and plant families such as Rhamnaceae or Fabaceae. Furthermore, they were found to have anticancer activity, exemplified by mitoxantrone and pixantrone, and many are well known redox-active compounds. In this study, various nature inspired synthetic anthraquinone derivatives were tested against colon, prostate, liver and cervical cancer cell lines. Most of the compounds exhibit anticancer effects against all cell lines, therefore the compounds were further studied to determine their IC50-values. Of these compounds, 1,4-bis(benzyloxy)-2,3-bis(hydroxymethyl)anthracene-9,10-dione (4) exhibited the highest cytotoxicity against PC3 cells and was chosen for a deeper look into its mechanism of action. Based on flow cytometry, the compound was proven to induce apoptosis through the activation of caspases and to demolish the ROS/RNS and NO equilibrium in the PC3 cell line. It trapped cells in the G2/M phase. Western blotting was performed for several proteins related to the effects observed. Compound 4 enhanced the production of PARP and caspase-3. Moreover, it activated the conversion of LC3A/B-I to LC3A/B-II showing that also autophagy plays a role in its mechanism of action, and it caused the phosphorylation of p70 s6 kinase.
... In fact, the anthraquinone constituents like rhein, physcion, chrysophanol, and aloe-emodin have proven effective against common pathogenic bacterial species, viz. methicillin-resistant Staphylococcus aureus (Alaadin et al. 2007) and Escherichia coli K12 (Hatano et al. 1999), etc. Aloe-emodin had also been shown to inhibit growth of H. pylori through NAT N-acetyltransferase enzyme inhibition (Sydiskis et al. 1991), whereas rhein is known to have an antibacterial effect against Bacteroides fragilis and different acid-fast and gram-positive bacteria (Jong-Chol et al. 1987;Lewis and Elvin-Lewis 1977). Besides anthraquinones, the potent phytoceutical flavonoids, such as myricetin, quercetin, and rutin are also known to possess antibacterial activity. ...
... Some of the recent investigations have highlighted the efficacy of anthraquinone derivatives isolated from the rhizomes of R. australe as important antibacterial (Lu et al. 2011) and antiviral (Hussain et al. 2015) agents. The extracts from rhubarb rhizomes have shown virucidal effect against HSV-I, polio, influenza, and the measles virus in vitro (Sydiskis et al. 1991;May and Willuhn 1978;Kurokawa et al. 1993;Wang et al. 1996). Indeed, R. palmatum extracts are known C o p y r i g h t T a y l o r & F r a n c i s L L C / F o r P e r s o n a l U s e O n l y as a potential drug against SARS coronaviruses due to their inhibitory activity against 3CL protease (Miraj 2016). ...
... The extracts from Abies sachalinensis also induced envelope disruption in Beta coronavirus virions. Lipid vesicles rupture as a result of flavonoids like flavan-3-ols, which are the constituents of condensed tannins, causing phospholipid aggregation inside lipid membranes and consequent membrane stiffness [36]. Quinones have also been shown to breach the viral envelope [37] and pierce lipid bilayers, altering their biophysical characteristics [38]. ...
1) Background: Due to the wide application in medicinal and pharmaceutical chemistry of flavonoid molecules, which are one of the most famous types of secondary plant metabolites, our work has come within the framework of bio-consulting to help in the identification of the molecule(s) responsible for the antibacterial effect which will be the active principle of a natural antibiotic developed from Algerian fir using bioinformatics tools. (2) Methods: The docking method was used to test the antiviral activity on SARS-CoV-2 virus and the antibacterial activity on Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli of 12 polyphenolic molecules present in the ethyl acetate and n-butanol extracts of Numidian fir leaves, and identify the molecules responsible for these specific biological activities. (3) Results: The findings revealed that it is possible that two molecules, hyperoside and quercitrin, have a high capacity to inhibit SARS-CoV-2, and it is important to mention that they are the most quantitatively abundant molecules in the extract. The molecule luteolin-7-glucoside is probably responsible for the antibacterial activity in the extract against Gram-negative bacteria such as Escherichia coli, and the molecule hesperidin is responsible for the antibacterial activity in the extract against Gram-positive bacteria such as Staphylococcus aureus.
... The extracts from Abies sachalinensis also induced envelope disruption in Beta coronavirus virions. Lipid vesicles rupture as a result of flavonoids like flavan-3-ols, which are the constituents of condensed tannins, causing phospholipid aggregation inside lipid membranes and consequent membrane stiffness [36]. Quinones have also been shown to breach the viral envelope [37] and pierce lipid bilayers, altering their biophysical characteristics [38]. ...
1) Background: Due to the wide application in medicinal and pharmaceutical chemistry of flavonoid molecules, which are one of the most famous types of secondary plant metabolites, our work has come within the framework of bio-consulting to help in the identification of the molecule(s) responsible for the antibacterial effect which will be the active principle of a natural antibiotic developed from Algerian fir using bioinformatics tools. (2) Methods: The docking method was used to test the antiviral activity on SARS-CoV-2 virus and the antibacterial activity on Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli of 12 polyphenolic molecules present in the ethyl acetate and n-butanol extracts of Numidian fir leaves, and identify the molecules responsible for these specific biological activities. (3) Results: The findings revealed that it is possible that two molecules, hyperoside and quercitrin, have a high capacity to inhibit SARS-CoV-2, and it is important to mention that they are the most quantitatively abundant molecules in the extract. The molecule luteolin-7-glucoside is probably responsible for the antibacterial activity in the extract against Gram-negative bacteria such as Escherichia coli, and the molecule hesperidin is responsible for the antibacterial activity in the extract against Gram-positive bacteria such as Staphylococcus aureus.
... Correspondingly, Gelonium multiflorum and Momordica charantia are similarly contemplated as beneficial sources of an anti-HIV protein GAP31 and MAP30, which are like RIPs that have been recognized for their antihuman immunodeficiency virus strength (Schreiber et al., 1999). The plant of Rheum palmatum consists of organic aloe-emodin and anthraquinone used in Chinese medicine, active against influenza viruses, herpes simplex virus and cytomegalovirus (Sydiskis et al., 1991). Gallotannins, one of most powerful antiviral constituents recognize to suppress and reduce Epstein-Barr virus, wild-variety of herpes simplex virus-2, acyclovir-phosphonoacetic acid resilient herpes simplex virus-1, as well as thymidine kinasedeficient herpes simplex virus-1 (Hussain et al., 2017). ...
Plants are useful as food and drugs to human beings. People are becoming progressively conscious of complications with the abuse and over prescription of conventional antibiotics. Plant extracts can be good alternative in day-today illness instead of antibiotics misuse. Complementary and alternative medicines are good option for treatment of routine ailments. Complexes and constituents with antiviral activity exists in numerous plants, for instance, rutin, a flavonoid glycoside generally found in a range of botanicals, is efficient against herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2), and influenza A virus. Ascorbic acid, beta carotene and lots of phenolics play active parts in decreasing inflammation, postponing aging, and averting certain kinds of carcinomas. There are some phenolic compounds such as tannins, flavonoids, vitamins and lignins derived from plants acts as antioxidants. In this review article, we discussed upon history of use of plants as medicine, role of plants in viral infections, and anti-viral effects of various plants.
... The pharmacological actions of Aloe Vera as studied in vitro and in vivo include anti-inflammatory 13,14,15,16,17,18 , antibacterial 19,20 , antioxidant 21 , antiviral 22,23,24 , anti-fungal 25 and hypoglycemic properties 26 . The decrease in gingival index can also be attributed to presence of sterols as anti-inflammatory agents and lapel as antiseptic analgesics 27 . ...
Background: Aloe Vera can be used as adjunct to conventional periodontal therapy in patients with chronic periodontitis. The purpose of this study was to investigate the clinical effectiveness of local application of Aloe Vera gel used as an adjunct to scaling and root planing in the treatment of patients with chronic periodontitis.
... Triterpene acids, such as masalinic and ursolic acid, expressed a potent inhibitory effect against HIV-1 protease [78]. Various anthraquinone extracts of Aloe barbadensis, Rhamnus purshianus, Cassia angustifolia, etc. showed potent activity against HSV-1 [79]. In 1996, Marchetti et al., revealed that scleroglucan polysaccharide binds with membrane glycoproteins of viral particles and impedes the complexation of the virus with the plasma cell membrane [80]. ...
Since ancient times, plants have been used for their medicinal properties. They provide us with many phytomolecules, which serve a synergistic function for human well-being. Along with anti-microbial, plants also possess anti-viral activities. In Western nations, about 50% of medicines were extracted from plants or their constituents. The spread and pandemic of viral diseases are becoming a major threat to public health and a burden on the financial prosperity of communities worldwide. In recent years, SARS-CoV-2 has made a dramatic lifestyle change. This has promoted scientists not to use synthetic anti-virals, such as protease inhibitors, nucleic acid analogs, and other anti-virals, but to study less toxic anti-viral phytomolecules. An emerging approach includes searching for eco-friendly therapeutic molecules to develop phytopharmaceuticals. This article briefly discusses numerous bioactive molecules that possess anti-viral properties, their mode of action, and possible applications in treating viral diseases, with a special focus on coronavirus and various nano-formulations used as a carrier for the delivery of phytoconstituents for improved bioavailability.
... However, it was observed that the same extract had no effect on Varicella-zoster virus, even at a concentration 90 times higher than that used for HSV-1. The responsible chemical constituent in the glycerine extract was identified as sennosides, including aloe-emodin [52]. The anti-viral activity of senna demands thorough investigation, including the identification of its active chemical components. ...
... Aloe-emodin was also tested against different viruses listed below with their ID 50 values (concentration of aloe-emodin that reduced virus plaque formation or infectivity by 50%) by plaque reduction assay (Table 4). Only adenovirus and rhinovirus remain unaffected on aloe-emodin treatment while all other enveloped viruses were inactivated [59]. ...
... Aloe vera contains nearly 75 active constituents [6], making it a miraculous plant, which include vitamins, enzymes, minerals, amino acids, saponins, sugars, lignin, hormones, and salicylic acids [7]. Evidence-based studies claim healing properties [8], anti-inflammatory effects [9], enhanced immune system [10], antiviral [11], cancer prevention [12], radiation damage [13], and anti-tumour [14]. Aloe vera is commercially used in various food and pharmaceutical industries for its versatile purposes. ...
Advanced food processing techniques have drastic effects on the food, mainly on the nutritional profile; furthermore, the sedentary lifestyle led by people makes the body starve for nutrients and has a negative impact on proper growth and health. Addressing those major issues, various organic and functional foods have been widely recognised in recent times. The current work intends to prepare and evaluate a functional food made out of Aloe Vera. The health claims of Aloe Vera were uncountable. From the organoleptic profiling of the milk shake up to the 5% addition of Aloe Vera, all the sensory parameters were more satisfying. Incorporating Aloe Vera in the milkshake will be an innovative novel food product while enhancing the functional properties of Aloe Vera.
... Compounds that can target virions are a developing strategy and have been used by health organizations as prophylactic methods to avoid virus infection and control epidemics [62]. Compounds such as nonoxynol-9, para-aminobenzoic acid, fullerene derivatives, and anthraquinones have been reported as virucidal compounds against the enveloped virus [63][64][65][66][67]. Mastoparan, an invertebrate host defence peptide that penetrates lipid bilayers, and its derivatives interact with viral lipid envelopes, and thereby reduce the infectivity of West Nile virus, avian influenza, and henipavirus [68]. ...
Re-emerging arboviruses represent a serious health problem due to their rapid vector-mediated spread, mainly in urban tropical areas. The 2013–2015 Zika virus (ZIKV) outbreak in South and Central America has been associated with cases of microcephaly in newborns and Guillain–Barret syndrome. We previously showed that the conjugate gallic acid—Hecate (GA-FALALKALKKALKKLKKALKKAL-CONH2)—is an efficient inhibitor of the hepatitis C virus. Here, we show that the Hecate peptide is degraded in human blood serum into three major metabolites. These metabolites conjugated with gallic acid were synthesized and their effect on ZIKV replication in cultured cells was evaluated. The GA-metabolite 5 (GA-FALALKALKKALKKL-COOH) was the most efficient in inhibiting two ZIKV strains of African and Asian lineage at the stage of both virus entry (virucidal and protective) and replication (post-entry). We also demonstrate that GA-metabolite 5 does not affect cell growth after 7 days of continuous treatment. Thus, this study identifies a new synthetic antiviral compound targeting different steps of ZIKV replication in vitro and with the potential for broad reactivity against other flaviviruses. Our work highlights a promising strategy for the development of new antivirals based on peptide metabolism and bioconjugation.
... Aloe's anti-inflammatory effects may be due to a bardykinin, degrading glycoprotem [25] and mannose-6-phosphate may have a role in wound healing process (Davis et al., 1994) [26] . Anthraquinones form various plant extracts have been studied for their possible antiviral properties (Sydiskis et al., 1991) [27] . The discovery of a potent herbal remedy that is safe will be a big advancement in fungal infection therapies. ...
... A few cancer prevention agents form part of the body's normal directing apparatus whereas other dietary cancer prevention agents are inferred from slim-down sources. Aloe vera is an amazing illustration of how a natural agent can play a noteworthy part in protecting the body from the destructive effects of oxidative stress (15,16). ...
... The presence of anthraquinones, flavonoids, minerals, vitamins, phenolic acids, sterols, and polysaccharides in this plant contributes to its antiviral action. Aloe-emodin is an anthraquinone found in Aloe vera and was shown to exhibit antiviral activity against the following viruses: influenza, pseudorabies, herpes simplex types 1 and 2, and varicella-zoster [59,60]. The extracts from Aloe vera leaves were found to have antiviral properties against the human cytomegalovirus in vitro [61]. ...
Coronavirus disease 2019 (COVID-19) is a pandemic first identified in China and rapidly transmitted to other countries all over the world. The lack of effective vaccines and treatments against COVID-19 causes its devastating aftermath. Therefore, it is urgently required to identify effective and safe treatments for COVID-19 and a variety of studies have been conducted for elucidating the antiviral effects of natural and plant based agents. As COVID-19 is caused by the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), inhibitors against SARS-CoV-2 are expected to be efficacious for the treatment of COVID-19. In this review, we will introduce the molecular simulation studies for exploring novel plant based agents as potent inhibitors against the main protease of SARS-CoV-2. These agents are expected to be utilized safely for the COVID-19 treatment.
... Ранее нами был проанализирован ассортимент зарегистрированного в Республике Беларусь, Российской Федерации и Республике Казахстан лекарственного растительного сырьякрушины ломкой коры, а также ассортимент лекарственных растительных препаратов на его основе (таблетки, сборы) и установлено, что большинство их них применяют в качестве слабительных лекарственных средств [5]. Также комплекс биологически активных веществ растения проявляет антимикробное, противовирусное, противогрибковое и антиоксидантное действие [6][7][8][9][10][11]. ...
Objective: optimization of extraction conditions for anthraglycosides of alder buckthorn bark, development and validation of a method for their quantitative determination using high performance liquid chromatography. Materials and methods. The object of the study was alder buckthorn bark from different manufacturers. The work was performed on an Agilent 1100 liquid chromatograph complete with a G1311A four-solvent supply and degassing system, a G1315B diode array detector, a G1316A column thermostat, and a G1313A automatic sample injection device. Chromatographic analysis was carried out on a Zorbax SB-C18 reverse-phase column (4.6×250 mm, 5 μm) in a gradient elution mode of the mobile phase consisting of acetonitrile and highly purified water, adjusted to pH 2 with phosphoric acid. Results. As a result of the study, the optimal conditions for the chromatographic separation of anthraglycosides of alder buckthorn bark were determined. The optimal conditions for their extraction have been established: the grinding of plant raw materials is 250 µm, the extractant is ethyl alcohol 40%, the extraction temperature is 80℃, the extraction time is 90 minutes, the ratio of raw materials and extractant is 1:50. It has been proved that the developed method for the quantitative determination of anthraglycos
... The antiviral activity of Aloe vera is due to its content of anthraquinones, avonoids, minerals, vitamins, phenolic acids, sterols, and polysaccharides [8,13]. Aloe-emodin (A10 of Fig. 1), an anthraquinone present in Aloe vera, has been reported to have antiviral activity against the following viruses: herpes simplex types 1 and 2, varicella-zoster, pseudorabies, and in uenza [13,14]. ...
The novel coronavirus 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread rapidly worldwide, and new drug treatments for COVID-19 are urgently required. To find the potential inhibitors against main protease (Mpro) of SARS-CoV-2, we investigated the inhibitory potential of naturally occurring compounds from the plants Moringa oleifera , Aloe vera , and Nyctanthes arbor-tristis , using molecular docking, classical molecular mechanics optimizations, and ab initio fragment molecular orbital calculations. Of the 35 compounds that we simulated, feralolide from Aloe vera exhibited the highest binding affinity against Mpro. Therefore, we proposed novel compounds based on the feralolide and investigated their binding properties to the Mpro. The results indicated that the introduction of a hydroxyl group into feralolide significantly enhances its binding affinity against Mpro. These results provide useful information for developing potent Mpro inhibitors.
... It can constitute up to 30% of aloe plants dried leaf exudates [1], and is considered to be a part of their defense mechanisms against herbivores [5] [6]. This anthraquinone is known for its biological activities, such as antiviral [7] [8], antioxidant [9][10] [11], anti-inflammatory [12] [13], and anti-cancer [14] [15] activities, and as an inhibitory agent [16] [3]. Previous studies revealed that Barbaloin has a much higher inhibitory efficacy in histamine release from human mast cells [17] than some anti-inflammatory drugs [18]. ...
Barbaloin (10 – glucopyranosyl – 1,8 – dihydroxy – 3 – (hydroxymethyl) – 9(10H) – anthraquinone: aloin A), present in Aloe species, is widely used in food, cosmetic and pharmaceutical industries. Here we characterize its optical absorption and emission spectra in aqueous solution at different pH values. Through pH titration, using both absorption and fluorescence spectroscopy, two pKa values for Barbaloin were determined: pKa1=9.6±0.6 and pKa2=12.6±0.8. These acidity constants were found to be higher than those found for Emodin, a similar molecule which lacks the sugar moiety present in Barbaloin. Performing quantum mechanical calculations for non-ionized, singly, doubly, and triply deprotonated forms of Barbaloin in vacuum and in water, we assigned the positions of the site for the first and third deprotonation in the anthraquinone group, and the second deprotonation in the glucose group. The instability of Barbaloin in high pH solutions is discussed here, and the optical absorption and fluorescence spectra due to products resulted from Barbaloin degradation at high pH is well separated from the Barbaloin original spectra. Biological fluids have specific pH values to maintain homeostasis, hence determining the pKaof Barbaloin is important to evaluate the mechanism of action of this drug in different parts of an organism as well as to predict pharmacological relevant parameters, such as absorption, distribution, metabolism, and excretion.
... Rhein and other anthraquinone drugs, including emodin and aloe-emodin, have been extracted from rhubarb. Emodin and aloe-emodin have antibacterial or virucidal activity by destroying the envelope of bacteria or viruses (40)(41)(42)(43). Rhein was previously demonstrated to directly inhibit the growth of S. aureus (33). ...
The global incidence of genital Chlamydia trachomatis infection increased rapidly as the primary available treatment of C. trachomatis infection being the use of antibiotics. However, the development of antibiotics resistant stain and other treatment failures are often observed in patients. Consequently, novel therapeutics are urgently required. Rhein is a monomer derivative of anthraquinone compounds with an anti-infection activity. This study investigated the effects of rhein on treating C. trachomatis infection. Rhein showed significant inhibitory effects on the growth of C. trachomatis in multiple serovars of C. trachomatis, including D, E, F and L1, and in various host cells, including HeLa, McCoy and Vero. Rhein could not directly inactivate C. trachomatis but could inhibit the growth of C. trachomatis by regulating pathogen-host cell interactions. Combined with azithromycin, the inhibitory effect of rehin was synergistic both in vitro and in vivo. Together these findings suggest that rhein could be developed for the treatment of C. trachomatis infections.
... Additionally C. angustifolia extract have also been reported to possess virucidal efficacy 16 . Recently, a report elucidated presence of different flavonoids which were found associated with anti-microbial, anti-cancer and anti-inflammatory effects 17 . However, to best of our knowledge there is an inadequacy of literature reporting the exploration of C. angustifolia in modulating the proliferation or exerting anti-cancer effects on glioblastoma C6 cells. ...
Glioblastoma multiforme or GBM is a destructive malignancy of the central nervous system and is accountable for leading cause of cancer related mortality. Inadequate success rate of surgical interventions and development of resistance towards the current therapeutical regime provides impetus for exploring novel therapeutical interventions against the disease. Recently, several epidemiological studies have explored the plausible utility of natural, dietary compounds in influencing the development, progression, and cancer metastasis. Recently, different phytoconstituents of Cassia angustifolia were found to be associated with anti-microbial, anti-cancer and anti-inflammatory effects. Therefore, the aim of the present study was to evaluate the anti-proliferative efficacy of ethanolic leaf extract of C. angustifolia (LCaEt-OH) against rat derived glioblastoma C6 cells. Briefly, the anti-proliferative potential of LCaEt-OH was assessed using MTT assay, quantitative estimation of ROS, and evaluation of mitochondrial membrane potential (ΔΨm). Moreover, the activity of caspases involved in intrinsic apoptotic pathways was also investigated using colorimetric kit followed by quantitative RT-PCR evaluation of modulation in gene expressions triggered due to LCaEt-OH treatment. Treatment of LCaEt-OH on C6 cells elucidated substantial dose-dependent decline in cellular viability. Furthermore, LCaEt-OH showed its efficacy in substantially enhancing intracellular ROS. LCaEt-OH also incited apoptosis in C6 cells by instigating nuclear condensation and dissipation of ΔΨm. In addition, LCaEt-OH mediated instigation of apoptosis was directly influenced by increased activity of caspases indispensable for intrinsic apoptotic pathway. These conclusive evidences indicate towards anticancer efficacy of LCaEt-OH against C6 cells.
graphical abstract Fullsize Image
... The antiviral activity of Aloe vera is due to its content of anthraquinones, flavonoids, minerals, vitamins, phenolic acids, sterols, and polysaccharides [8,13]. Aloe-emodin (A10 of Fig. 1), an anthraquinone present in Aloe vera, has been reported to have antiviral activity against the following viruses: herpes simplex types 1 and 2, varicella-zoster, pseudorabies, and influenza [13,14]. Substances extracted from Aloe vera leaves have antiviral effects against human cytomegalovirus in vitro [15]. ...
The novel coronavirus 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread rapidly worldwide, and new drug treatments for COVID-19 are urgently required. To find the potential inhibitors against the main protease (Mpro) of SARS-CoV-2, we investigated the inhibitory potential of naturally occurring compounds from the plants Moringa oleifera, Aloe vera, and Nyctanthes arbor-tristis, using molecular docking, classical molecular mechanics optimizations, and ab initio fragment molecular orbital (FMO) calculations. Of the 35 compounds that we simulated, feralolide from Aloe vera exhibited the highest binding affinity against Mpro. Therefore, we proposed novel compounds based on the feralolide and investigated their binding properties to Mpro. The FMO results indicated that the introduction of a hydroxyl group into feralolide significantly enhances its binding affinity to Mpro. These results provide useful information for developing potent Mpro inhibitors.
Supplementary information:
The online version contains supplementary material available at 10.1007/s11224-022-02021-y.
... The following botanicals or plant extracts when used in vitro or vivo have demonstrated efficacy against HSV type 1 and 2.They have also been highlighted to be possibly considered in the management of herpes zoster [25][26][27][28][29][30] .These include:- Honey/Propolis Sangre de Grado (Croton lechleri) Aloe (Aloe vera) St John's wort (Hypericum perforatum and spp) ...
Streblus asper Lour. (Moraceae)is a small tree found in tropical regions of the world and used for the treatment of fever, diarrhea, dysentery, elephantiasis, filariasis, gingivitis, leprosy, piles, skin diseases, toothache and wounds. Phytochemical investigation of a methanol extract of the roots led to the isolation of two new compounds characterized as lup-20(29)-en-3β-olyl octadec-9′-enoate (1) and stigmast-5-en-3β-olyl-26-oic acid-3β-hexadecanoate (4) together with the four known constituents identified as lupeol linoleate (2), stigmasterol palmitate (3), cerotic acid (5) and octacosanoic acid (6). The structures of all these compounds were elucidated on the basis spectral data analysis and chemical reactions.
... Emodin, an anthraquinone prepared from aloin, was shown to inactivate herpes simplex virus type 1 and type 2, varicella-zoster virus, pseudorabies virus, and influenza virus, not adenovirus and rhinovirus. Electron microscopic examination of the anthraquinone-treated herpes simplex virus demonstrated that the envelopes were partially disrupted [121]. ...
Introduction:
The Uganda National Drug Authority requires phytochemical screening, freedom from microbial contamination, and evidence of safety and efficacy of the constituent plants to register herbal products. Since Uganda has no pharmacopeia, safety, efficacy, and plant processing information are not readily available. We documented the plant materials used to manufacture products in Uganda and established evidence of their safety and efficacy and availability of monographs.
Methods:
The NDA register of herbal products was reviewed, and a product list was extracted. The herbal products were purchased from local pharmacies, and their labels were studied to identify plant ingredients and drug use. Literature was reviewed to document evidence of the safety and efficacy of the plant materials concerning manufacturer's claims. Also, the WHO and available African Pharmacopeia were searched to establish the availability of the plant monographs.
Results:
Of the 84 NDA-registered local products, only 18 were obtained from the market; 82% were indicated for respiratory tract disorders. Thirty-three plant materials were listed with Eucalyptus globulus Labill, being the commonest. Several in vitro and in vivo studies demonstrate efficacy, thus supporting the use of the selected plant species for empirical treatment as stated on the product label. While most plants were safe, some species such as Albizia coriaria Oliv. had dose-dependent toxicities that cannot be predicted in combinations. The WHO, African Pharmacopoeia, and West African Herbal Pharmacopoeia had only 16 plant monographs of the 33 plants of interest. Nevertheless, Aloe vera (L.) Burm.f., Azadirachta indica A.Juss., Zingiber officinale Roscoe, and Allium sativum L. monographs were published by all three pharmacopoeias.
Conclusions:
Preclinical evidence of safety and efficacy exists in the literature for most of the plants used to manufacture registered herbal products in Uganda. More specific bioassays and clinical trials are required for the products to provide conclusive evidence of safety and toxicity. Monographs are urgently needed for the Ugandan plants.
... As mentioned before, A. vera contains anthraquinones and lectin, which have antiviral effects and prevent cytomegalovirus proliferation (Kahlon et al. 1991;Saoo et al. 1996). Emodin is effective against several infectious viruses such as herpes simplex virus (Sydiskis et al. 1991;Saoo et al. 1996). A study demonstrated antifungal properties of A. vera, as it gradually inhibited the growth of Malassezia furfur and Candida albicans (Rezazadeh et al. 2016). ...
Diabetes mellitus is defined as prolonged hyperglycemia, which can harm the eyes, kidneys, and cardiovascular and neurological systems. Herbal agents and their derived supplements have been used for treatment of diabetes mellitus as a part of integrated complementary medicine for centuries. Numerous studies have considered Aloe vera (L.) Burm.f, Xanthorrhoeaceae, as an alternative medicine due to its abundant bioactive chemicals, such as alkaloids, anthraquinones, and enthrones, with therapeutical properties including antioxidant, anti-inflammatory, neuro-protective, and anti-diabetic effects. Aloe vera has received considerable attention in traditional medicine for the treatment of several diseases including diabetes mellitus. Numerous studies have investigated the effects of herbal agents on diabetes mellitus using a streptozotocin-induced diabetic model. Thereby, this article reviews the effects of Aloe vera prescription on streptozotocin-induced diabetes mellitus to provide a clear insight into the role of this medicinal plant in several biological functions, such as antioxidant, wound healing, anti-inflammatory, anti-hyperglycemic, and anti-hyperlipidemic in diabetic models.
Graphical abstract
... Another flavonoid, emodin, like quercetin, prevents SARS-CoV entry in a dose-dependent fashion by attaching to the viral S protein to prevent its binding to the angiotensin-converting enzyme 2 (ACE2) receptor on host cells at concentration ranges from as low as 1 to 10 µg/mL in vitro without detectable cytotoxicity (Ho et al., 2007). Beyond the inhibition of viral attachment, emodin was postulated to interact with and disrupt the lipid bilayer of the viral envelope, unlike quercetin (Sydiskis et al., 1991). ...
Isatis indigotica Fortune is a biennial Chinese woad of the Cruciferae family. It is primarily cultivated in China, where it was a staple in indigo dye manufacture till the end of the 17th century. Today, I. indigotica is used primarily as a therapeutic herb in traditional Chinese medicine (TCM). The medicinal use of the plant is separated into its leaves (Da-Qing-Ye) and roots (Ban-Lan-Gen), whereas its aerial components can be processed into a dried bluish-spruce powder (Qing-Dai), following dehydration for long-term preservation. Over the past several decades, I. indigotica has been generally utilized for its heat-clearing effects and bodily detoxification in TCM, attributed to the presence of several classes of bioactive compounds, including organic acids, alkaloids, terpenoids, and flavonoids, as well as lignans, anthraquinones, glucosides, glucosinolates, sphingolipids, tetrapyrroles, and polysaccharides. This paper aims to delineate I. indigotica from its closely-related species (Isatis tinctoria and Isatis glauca) while highlighting the ethnomedicinal uses of I. indigotica from the perspectives of modern and traditional medicine. A systematic search of PubMed, Embase, PMC, Web of Science, and Google Scholar databases was done for articles on all aspects of the plant, emphasizing those analyzing the bioactivity of constituents of the plant. The various key bioactive compounds of I. indigotica that have been found to exhibit anti-inflammatory, antimicrobial, anticancer, and anti-allergic properties, along with the protective effects against neuronal injury and bone fracture, will be discussed. Collectively, the review hopes to draw attention to the therapeutic potential of I. indigotica not only as a TCM, but also as a potential source of bioactive compounds for disease management and treatment.
... Aloin is an anthraquinone abundantly found in aloe vera plant. Anthraquinones including aloin A and B exhibit analgesic, antimicrobial [33][34][35] and antiviral properties [36][37][38] . Recent reports suggest that aloin B inhibits hepatitis B virus replication in an in vitro setting 39 . ...
The most common host entry point of human adapted coronaviruses (CoV) including SARS-CoV-2 is through the initial colonization in the nostril and mouth region which is responsible for spread of the infection. Most recent studies suggest that the commercially available oral and nasal rinse products are effective in inhibiting the viral replication. However, the anti-viral mechanism of the active ingredients present in the oral rinses have not been studied. In the present study, we have assessed in vitro enzymatic inhibitory activity of active ingredients in the oral mouth rinse products: aloin A and B, chlorhexidine, eucalyptol, hexetidine, menthol, triclosan, methyl salicylate, sodium fluoride and povidone, against two important proteases of SARS-CoV-2 PLpro and 3CLpro. Our results indicate only aloin A and B effectively inhibited proteolytic activity of PLpro with an IC50 of 13.16 and 16.08 μM. Interestingly, neither of the aloin isoforms inhibited 3CLpro enzymatic activity. Computational structural modelling of aloin A and B interaction with PLpro revealed that, both aloin isoforms form hydrogen bond with Tyr²⁶⁸ of PLpro, which is critical for their proteolytic activity. Furthermore, 100 ns molecular dynamics (MD) simulation studies predicted that both aloin isoforms have strong interaction with Glu¹⁶⁷, which is required for PLpro deubiquitination activity. Our results from the in vitro deubiquitinase inhibition assay show that aloin A and B isomers exhibit deubiquitination inhibitory activity with an IC50 value of 15.68 and 17.51 µM, respectively. In conclusion, the isoforms of aloin inhibit both proteolytic and the deubiquitinating activity of SARS-CoV-2 PLpro, suggesting potential in inhibiting the replication of SARS-CoV-2 virus.
... (1,3,8-trihydroxy-6-methylanthraquinone) is chiefly extracted from some plant species such as Cassia, Polygonum, and Rhamnus species, which belong to families Fabaceae, Polygonaceae, and Rhamnaceae, respectively (Dong et al., 2016). It showed antiviral properties through inactivation of enveloped viruses by disrupting the lipid bilayer (Sydiskis et al., 1991) and inhibition of casein kinase 2 (CK2) that is required and exploited by numerous viruses to phosphorylate essential proteins needed to complete their life cycle (Battistutta et al., 2000). It was likely proven to display antiviral activity via the prevention of S protein binding to ACE 2 receptors (Dabaghian et al., 2020). ...
... This may be due to the presence of a more robust icosahedral capsid surrounding the DNA genome of herpesviruses compared to the more flexible, N-associated vRNPs of HCoVs. However, PhytoQuin likely also damages herpesvirus envelopes as earlier work demonstrated the ability of anthraquinones to disrupt HSV-1 virions [53]. Evidence of physical damage to viral particles due to PhytoQuin treatment was further supported by the appearance of high molecular weight forms of SARS-CoV-2 S on purified, pseudotyped lentiviruses following light exposure ( Figure 5). ...
Photodynamic inactivation (PDI) employs a photosensitizer, light, and oxygen to create a local burst of reactive oxygen species (ROS) that can inactivate microorganisms. The botanical extract PhytoQuinTM is a powerful photosensitizer with antimicrobial properties. We previously demonstrated that photoactivated PhytoQuin also has antiviral properties against herpes simplex viruses and adenoviruses in a dose-dependent manner across a broad range of sub-cytotoxic concentrations. Here, we report that human coronaviruses (HCoVs) are also susceptible to photodynamic inactivation. Photoactivated-PhytoQuin inhibited the replication of the alphacoronavirus HCoV-229E and the betacoronavirus HCoV-OC43 in cultured cells across a range of sub-cytotoxic doses. This antiviral effect was light-dependent, as we observed minimal antiviral effect of PhytoQuin in the absence of photoactivation. Using RNase protection assays, we observed that PDI disrupted HCoV particle integrity allowing for the digestion of viral RNA by exogenous ribonucleases. Using lentiviruses pseudotyped with the SARS-CoV-2 Spike (S) protein, we once again observed a strong, light-dependent antiviral effect of PhytoQuin, which prevented S-mediated entry into human cells. We also observed that PhytoQuin PDI altered S protein electrophoretic mobility. The PhytoQuin constituent emodin displayed equivalent light-dependent antiviral activity to PhytoQuin in matched-dose experiments, indicating that it plays a central role in PhytoQuin PDI against CoVs. Together, these findings demonstrate that HCoV lipid envelopes and proteins are damaged by PhytoQuin PDI and expands the list of susceptible viruses.
This book is a comprehensive review of secondary metabolite production from plant tissue culture. The editors have compiled 12 meticulously organized chapters that provide the relevant theoretical and practical frameworks in this subject using empirical research findings. The goal of the book is to explain the rationale behind in vitro production of secondary metabolites from some important medicinal plants. Biotechnological strategies like metabolic engineering and the biosynthesis, transport and modulation of important secondary metabolites are explained along with research studies on specific plants. In addition to the benefits of secondary metabolites, the book also aims to highlight the commercial value of medicinal plants for pharmaceutical and healthcare ventures.
Topics covered in this part include:
1. In vitro propagation and tissue culture for several plants including Withania somnifera (L.) Dunal, Aloe vera, Oroxylum indicum (L) Kurz, Ocimum basilicum L, Rhubarb, Tea, and many others (including plants in Northern India).
2. Genetic Improvement of Pelargonium
3. Bioactive Components in Senna alata L. Roxb
4. Plant tissue culture techniques
The book caters to a wide readership. It primarily prepares graduate students, researchers, biotechnologists, giving them a grasp of the key methodologies in the secondary metabolite production. It is a secondary reference for support executives, industry professionals, and policymakers at corporate and government levels to understand the importance of plant tissue culture and maximizing its impact in the herbal industry.
The history for the use of Aloe vera for medicinal purposes starts from about 3000 years. Medicinally, this plant may be able to treat skin cancer as well as sunburns, burns, and small wounds. More than 104 compounds from various parts of this plant, including minerals, vitamins, amino acids, enzymes, sterols, anthraquinone, flavonoids, terpenoids, coumarins, polysaccharides, sugars, and polyphenols, have been isolated thus far, according to scientific reports on phytochemical analysis of this plant. The biological activities of these compounds are diverse and include anthelmintic, hepatoprotective, antidiabetic, diuretic, antibacterial, antiviral, antioxidant, antiseptic, anti-inflammatory, anticancer, and cosmetic effects for medical therapy. This article mainly emphasizes therapeutic, medicinal and food uses of A. vera.
The novel coronavirus (COVID 19) is a respiratory disease that has affected the entire globe and has been recorded as one of the fastest spreading in the new era with a high mortality rate. The purpose of this study was to introduce the medicinal plants used for the treatment of coronavirus disease by traditional practitioners of Kabul city.
The study was a field research. Kabul city was selected as the field of study. Convenience sampling was -used for data collection. The required information was randomly collected from eight districts of Kabul city and accepted as a sample. Traditional practitioners were selected as participants and interviewed using prepared questionnaires.
The results of this study revealed that a total of 24 medicinal plants from18 plant families are used by traditional practitioners to treat Coronavirus disease. According to the results of this study, Thymus sp., Descurainia sophia Salvia rhytidea, Cassia angustifolia, Zingiber officinale, Papaver somniferum and Glycerrhiza glabra had the highest effectiveness in treating Coronavirus disease, respectively.
The effectiveness of using medicinal plants to treat Coronavirus disease by traditional practitioners in Kabul city, in most of the cases, matches the rational phytotherapy. As the used medical plants have various properties such as antiviral, anti-inflammatory, antimicrobial, analgesic, antipyretic, antitussive, antioxidant, immune modulatory etc to alleviate the pathogenic signs and symptoms over the course of covid-19. Moreover, in some cases usage of medicinal plants including Fumaria sp., Hymenocrater sessilifolius, and Plantago ovata requires further research.
Hyaluronic acid, as a widely used polymer material in clinical practice, has been proven to have numerous biological functions. In Oral medicine, the application of hyaluronic acid also has certain advantages, which can be used to treat oral diseases. However, there are still many issues that need to be explored in research. Therefore, this article aims to explore the current situation and problems of hyaluronic acid in Aphthous stomatitis, and further test the effectiveness and safety of hyaluronic acid in Aphthous stomatitis, so as to propose a more reasonable and effective treatment plan for oral Aphthous stomatitis.
Researching the beneficial health properties of wood byproducts can prevent wastage by turning them into valuable resources. In this study, the virucidal activity of two extracts from Abies sachalinensis byproducts, ASE1, and ASE2, against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was investigated. ASE1 is rich in monoterpenoid volatile compounds, whereas ASE2 contains nonvolatile polyphenols. SARS-CoV-2 solutions were mixed with ASE1 or ASE2, and viral titer reduction was evaluated. At their original acidic pH, ASE2 showed stronger virucidal activity than ASE1. The virucidal activity of ASE2 was also significantly enhanced when pH was increased to neutral or basic, which was not the case for ASE1. At a neutral pH, ASE2 induced statistically significant viral titer reduction in 1 min. HCl and NaOH solutions, which had a pH close to that of acidic and basic ASE2 test mixtures, respectively, exhibited no virucidal activity against SARS-CoV-2. Among the SARS-CoV-2 variants, Omicron showed the highest vulnerability to ASE2. Western blotting, RT-PCR, and electron microscopic analysis revealed that neutral ASE2 interacts with SARS-CoV-2 spike proteins and moderately disrupts the SARS-CoV-2 genome and viral envelope. These findings reveal the virucidal potential of ASE2.
An essential category of the biological resources of Africa are plants with nutritional and therapeutic properties and they are common all over Africa. Folk remedies are relied on by almost 80% of people in underdeveloped and developing nations because of their indigenous knowledge, availability, and cost-effectiveness. Aloe barbadensis Miller, generally known as Aloe vera, is one of more than 400 species of Aloe belonging to the Liliaceae family that originated in Africa, but is considered native to arid subtropical and tropical regions of the world. More than 200 distinct biologically active compounds have been found in the plant and most of them possess one biological activity or the other. Also, more than a hundred different nutrients and beneficial chemicals make up the leaf gel's interior composition. This chapter discusses the occurrence and botanical description, processing, chemistry, historical use, options for domestication, technologies for the production of high-value therapeutics potentials, medicinal uses, and safety, toxicity, and conservation strategies of the Aloe barbadensis.Keywords
Aloe barbadensis
Therapeutic potentialSafetyToxicityMedicinal usesChemistryCultivationConservation strategies
The spike protein of coronavirus is crucial in binding and arrival of the virus to the human cell via binding to the human ACE2 receptor. In this study, at first 25 antiviral phytochemicals were docked into the RBD domain of spike protein, and then all complexes and free RBD domains were separately subjected to molecular dynamics simulation for 100 ns and MM/PBSA binding free energy calculation. In this phase, four ligands were chosen as hit compounds and a natural compound database (NPASS) was screened based on high similarity with these ligands, and 367 ligands were found. Then the same previous procedure was repeated for these ligands and ADME properties were investigated. Finally, virtual screening and 4400 ns MD simulation and MM/PBSA calculation revealed that new ligands including NPC67959, NPC157855, NPC248793, and NPC216361 can inhibit the RBD domain of spike protein and we propose them as potential drugs for experimental studies.
Communicated by Ramaswamy H. Sarma
The Dengue virus (DENV) has caused heavy concern worldwide because of its high infectivity and mortality rate. Still, there's no specific drug or preventive medication to treat DENV infection despite comprehensive analysis by the researchers. This study was designed to demonstrate the efficacy of some plant-derived bioactive compounds against DENV by using ligand-based virtual screening methods. A total of 52 plant metabolites and 74 plant peptides were screened on the basis of their reported pharmacological activities against DENV NS2B-NS3 protease(4M9T) employing a molecular docking approach. Furthermore, the ADMET properties were also predicted for screened top candidates i.e., gossypol, theaflavin, cycloviolacin O24,and cycloviolacin H3. Results showed that screened top candidates i.e., gossypol, theaflavin, cycloviolacin O24, and cycloviolacin H3 provide the highest binding affinity to the targeted DENV protein. The Crucial binding sites, as well as drug surfacehotspots were unraveled for viral targeted protein. The analysis of ADME properties exhibited that none of the compounds had side effects that would reduce their drug-like properties. As compared, the toxicity pattern analysis has unmasked the non-toxic essence of screened drug candidates. The NMA analysis revealed the docked complex was compact and it demonstrated its resistance to deformation. These results may lead to the development of effective anti-DENV natural medicines. Further in vivo trials are strongly recommended.
Surprisingly little overlap has been found in the studies of the several hundred plant and herb species with promise as new antiviral medicines. Given the rise in migration, international travel, and urbanization today, viral infections are one of the leading causes of disease around the world. Researchers are looking to the plant world as a source of potential novel antiviral treatments due to the numerous adverse effects of synthetic medicines and the growing problem of resistance. For their various therapeutic purposes, a large number of biologically active compounds have been discovered. Over the past few decades, thorough research into phytochemicals’ antiviral properties has gained relevance. This chapter demonstrates the abundance of potentially beneficial medicinal plants and herbs that are only waiting to be assessed and used for therapeutic applications against genetically and functionally varied plant and viral families.
Background
H1N1 influenza viruses are the leading cause of severe respiratory virus infections worldwide. Resistance to the current selections of anti-influenza agents are still of concern. The Zingiber officinale root is one of the most heavily consumed dietary substances. It is also been traditionally used against common cold in Ayurveda and Chinese herbal medicine.
Purpose
Investigation on in vitro and in vivo effect of [6]-gingerol from Zingiber officinale against influenza virus infection.
Methods
In vitro antiviral property of [6]-gingerol was measured by the plaque reduction assay in which MDCK cells were infected with PR8 strain of H1N1 influenza A virus in the presence of gingerol. Gingerol-mediated inhibition of influenza neuraminidase activity was tested by MUNANA assay in vitro. In vivo activity was tested in PR8 strain of H1N1 influenza virus infected mice. Modulation of anti-influenza immunity was tested by the study of hemagglutinin-specific T cells in vivo.
Results
[6]-Gingerol significantly reduced in vitro infection by PR8 strain of H1N1 influenza virus, with an IC50 value 2.25±0.18 μM. The inhibition was associated with the inhibition of viral neuraminidase activity, over 75% of the NA enzymatic activity of 2.5 × 10³ PFUs of PR8 strain influenza virus at a concentration of 2 μM. Oseltamivir (Tamiflu) served as a positive control, which inhibited the NA enzymatic activity with an IC50 value of 1.88±0.05 μM. In H1N1 influenza virus infected mice, gingerol treatment (oral, once daily for 5 days) reduced virus load in the lungs and attenuated body weight loss and mortality. Gingerol inhibited viral neuraminidase-mediated intracellular TGF-β activation of lung-infiltrating CD4⁺ T cells. With the constrained active-TGF-β and immune suppression, influenza hemagglutinin-specific Th1 and Th17 immunity was increased.
Conclusion
[6]-Gingerol from Z. officinale is a potent anti-influenza compound that inhibits viral neuraminidase activity and boosts hemagglutinin-specific CD4⁺ T cell response to the infection. Taken together, gingerol has the potential to be further evaluated for clinical applications in human influenza.
La grande majorité des colorants alimentaires naturels, utilisés dans la formulation des aliments et des boissons, proviennent des pigments extraits de matières premières végétales. Plusieurs couleurs dérivées de plantes peuvent entraîner des problèmes de formulation. Des facteurs, comme par exemple, la région, le climat, l'environnement, la variété cultivée, ont un effet de nuances de couleurs, de résistance et surtout de stabilité dans le produit final. Par ailleurs, les champignons filamenteux du genre Monascus, Penicillium et Talaromyces sont connus comme d'excellents producteurs de pigments rouges. Ces pigments intéressent de ce fait les industries car ils sont stables, non-toxiques et peuvent être utilisés comme colorants alimentaires.La recherche présentée dans le cadre de cette thèse de doctorat concerne la description des propriétés du pigment rouge que produit la souche de Talaromyces albobiverticillius isolée du milieu marin tropical autour de l'île de La Réunion. Les plans d’expérience (DOE) et la méthodologie des surfaces de réponses (RSM) ont été utilisés pour optimiser les conditions de culture et la formulation du milieu de fermentation, dans le but d'accroître les teneurs en polykétides colorés. Douze structures différentes ont été identifiées dans des extraits intracellulaires et extracellulaires des cultures fongiques, à l'aide de séparations et d'analyses spectroscopiques (HPLC-PDA-ESI/MS et RMN). Les pigments N-thréonine-monascorubramine, N-glutaryl-rubropunctamine et PP-O figurent ainsi parmi les 12 composants.Avec la demande croissante de composés colorés naturels dans le secteur industriel, les champignons isolés du milieu marin semblent présenter de nombreux intérêts. Des essais ont ainsi été menés afin d'étudier 1) l'amélioration des conditions de fermentation en fioles agitées ou en fermenteur de 2 litres; 2) les effets de la teneur en sel marin sur la synthèse des pigments; 3) des méthodes d'extraction respectueuses de l'environnement. Globalement, ces résultats font ressortir le grand potentiel des champignons marins produisant ce colorant rouge et la possibilité d'obtenir les colorants alimentaires adaptés.
Herpes simplex virus (HSV) infections are commonly epidemic and increasing worldwide. As such, they are a serious health concern. HSV type 1 (HSV‐1) and type 2 (HSV‐2) are two important members that are both common and endemic in many parts of the world. Although HSV infections are often mild or asymptomatic, they can lead to moderate or severe diseases, especially in immunocompromised patients. Currently, few medications have been approved for HSV infection diseases. Acyclovir, one of the first‐line therapies for HSV infections, and most modern anti‐HSV medications possess the same mechanism of action, i.e., DNA polymerase inhibition. Spacious clinical use of this medication has caused a drug‐resistant virus. Therefore, an alternative treatment of HSV infections needs to be searched. Recently, several published data from both in vitro and in vivo assays have described the anti‐HSV activity of many plant extracts, including Clinacanthus nutans, Melissa officinalis, Moringa oleifera, Punica granatum , and Lobelia chinensis through a wide range of mechanisms of action. Moreover, some phytochemicals, such as glucoevatromonoside, curcumin, and mangiferin, have shown significant inhibitory activity against acyclovir‐resistant HSV. However, the efficacy and safety of these compounds as alternative anti‐HSV agents warrants further clinical validation to gain regulatory approval.
Quinones have been of particular enthusiasm to established researchers because of their enormous applicable properties. Synthesized and natural anthraquinone based derivatives are now era of concern for researchers due to their distinctive properties. Intensive research has been made with special focus on laxative, antiulcerogenic, inhibition of enzymes, cytotoxicity, antimicrobial, anti-inflammatory, antiarthritic, antirheumatic, antidepressant, fungicidal, insecticidal, antioxidant and antitumor activity of anthraquinone based derivatives. With the awareness of environment protection need, safe and healthy, free of pollution, disease and particularly to maintain green, these derivatives are being used, acknowledged in medicinal research as well as in pharmaceutical world. Anthraquinone linked with amino derivatives have wide-spectrum therapeutic applications and being a center of focus as important biological scaffold in different fields like medicines, electronic industry, cosmetics. Owing to the remarkable activities of anthraquinone we outline the structural data, their sources, synthetic routes and therapeutic potentials.
Introduction
Viruses are known to significantly affect global health and are the leading cause of death worldwide as evident from numerous virus epidemics/ pandemics in the present and past. Though there are several antiviral therapies for human health care, only a few of them have significant therapeutic efficacy. The high costs of synthetic antiviral drugs, the rapid emergence of resistance, and the related side effects, are important challenges faced in anti-viral therapies. Traditional Indian Medicine (TIM) has a major advantage over modern medicine with their wider therapeutic window and rare side effects. The phytochemicals from the plants have shown strong inhibition of many viral infections.
Method
In the present study, the TIM plants in the classical codified texts of Ayurveda, Unani, Siddha, Homoeopathy, Sowa Rigpa (AYUSH) and plant repository of the National Innovation Foundation –India (NIF) database was reviewed to explore plants that have sufficient scientific experimental data demonstrating efficacy against different viruses. Fifteen years of literature presenting different treatment options available for control of viral infections was reviewed.
Result
It was found that reducing inflammation, enhancing immunity, and disrupting viral infection cycle were useful strategies for combating acute viral infections. In this paper, the authors suggest an integrative strategy of incorporating TIM plants in preventive healthcare that may act as the first line of defence against acute viral infections.
Conclusion
Development of an effective polyherbal formulation from a combination of potent TLR antagonists (anti-inflammatory), immuno-modulators, antivirals, and herbs that are rich source of micronutrients (especially Vitamin C and Zn) can act as a preventive strategy for a wide range of viral infections.
Radial thin-layer plates provide numerous advantages.
Various anthraquinones substituted with hydroxyl, amino, halogen, carboxylic acid, substituted aromatic group, and sulfonate were tested to determine their activity against human immunodeficiency virus type 1 (HIV-1) in primary human lymphocytes. Among the compounds tested, polyphenolic and/or polysulfonate substituted anthraquinones were found to possess the most potent antiviral activity. Hypericin, an anthraquinone dimer previously shown to have activity against nonhuman retroviruses also exhibited anti-HIV-1 activity in lymphocytes. the active anthraquinones inhibited HIV-1 reverse transcriptase. However, this enzyme inhibition was selective only for 1,2,5,8-tetrahydroanthraquinone and hypericin. Hypericin interacts nonspecifically with protein suggesting that this effect may dictate its inhibitory activity against the viral reverse transcriptase.
Two aromatic polycyclic diones hypericin and pseudohypericin have potent antiretroviral activity; these substances occur in plants of the Hypericum family. Both compounds are highly effective in preventing viral-induced manifestations that follow infections with a variety of retroviruses in vivo and in vitro. Pseudohypericin and hypericin probably interfere with viral infection and/or spread by direct inactivation of the virus or by preventing virus shedding, budding, or assembly at the cell membrane. These compounds have no apparent activity against the transcription, translation, or transport of viral proteins to the cell membrane and also no direct effect on the polymerase. This property distinguishes their mode of action from that of the major antiretro-virus group of nucleoside analogues. Hypericin and pseudohypericin have low in vitro cytotoxic activity at concentrations sufficient to produce dramatic antiviral effects in murine tissue culture model systems that use radiation leukemia and Friend viruses. Administration of these compounds to mice at the low doses sufficient to prevent retroviral-induced disease appears devoid of undesirable side effects. This lack of toxicity at therapeutic doses extends to humans, as these compounds have been tested in patients as antidepressants with apparent salutary effects. Our observations to date suggest that pseudohypericin and hypericin could become therapeutic tools against retroviral-induced diseases such as acquired immunodeficiency syndrome (AIDS).
The cytotoxicity of a newly developed dentin bonding system was examined in African green monkey kidney cells and human embryonic lung cells. A tissue culture agar overlay procedure, a longitudinal study, and a cell replication assay were employed to evaluate cytotoxicity. Several of the components were discovered to be cytotoxic when tested individually in vitro. However, when used in the prescribed manner, little or no cytotoxic effect was elicited. The results of this study support further testing of these materials in vivo.
Lysates of HEp-2 cells productively infected with herpes simplex virus yielded two bands on isopycnic centrifugation in CsCl gradients, ranging from 1.2 to 1.6 g/cm(3). One band, designated alpha, had a mean buoyant density of 1.27 g/cm(3) and contained herpes virions. Band beta had a mean density of 1.305 g/cm(3) and contained primarily complement-fixing viral antigens and little or no viral deoxyribonucleic acid (DNA). The products banding in the alpha and beta bands were unstable; fivefold or higher amounts were recovered by treating the cell extract with formaldehyde prior to centrifugation. Formaldehyde treatment increased the buoyant density of viral products in both the alpha and beta bands by about 0.015 g/cm(3). In addition, it stabilized hitherto inapparent products, forming a broad band gamma with a density range of 1.37 to 1.45 g/cm(3). The material in the gamma band was heterogeneous; it contained viral DNA, cellular DNA, and viral antigen. Formalinized lysates of DK cells abortively infected with herpes simplex virus yielded a beta band undifferentiated from that formed by extracts of productively infected cells. The gamma band was less dense and narrower. The alpha band was entirely missing.
The intracellular and extracellular localization of pseudorabies virions and subvirion components was determined at various stages in the replicative cycle. It was discovered that infectious pseudorabies virus appears first in the nucleus of the infected cell early in the infectious cycle but later accumulates in the cytoplasm. Subvirion components (nucleoids and nucleocapsids) are restricted to the nucleus, and only the complete virion is released from the infected cell.
Crude herpes virus suspensions were fractionated by the cesium chloride density gradient sedimentation method into enveloped and naked virus particles. Particles without envelopes were found to be almost non-infectious, whereas fractions containing enveloped particles were highly infectious. It appears, therefore, that the envelope plays an essential role in herpes virus infection.
Lysates of BHK-21 cells, infected with pseudorabies and labeled with (3)H-thymidine, were treated with formaldehyde and centrifuged in preformed CsCl gradients. Five peaks, designated bands A to E, were detected and shown to contain the following virus-specific products: band A, aggregates of virions; band B, virions; band C, empty capsids and nucleocapsids; bands D and E, small nucleoid-like particles. All five bands contained viral deoxyribonucleic acid and virous-specific antigens. Deoxyribonuclease treatment of the lysates before centrifugation resulted in the complete loss of (3)H-thymidine-labeled material from bands D and E; bands B and C were unaffected. Pulse-chase studies showed that (3)H-thymidine can be rapidly chased into the virus-specific products sedimenting in bands D and E. Further chase resulted in the gradual loss of label from bands D and E with a concomitant increase in the amount of label in bands A, B, and C. These results indicate that the virus-specific products in bands D and E are precursors of pseudorabies virions and may represent the nucleoid of the virion.
HIV-1 infected patients respond favorable to oral acemannan
- H R Mcdaniel
- M Carpenter
- J Kemp
- B Kahlon
- Mcanalley
McDaniel, H., R. Carpenter, M. Kemp, J. Kahlon, and B. McAnalley. 1990. HIV-1 infected patients respond favorable to oral acemannan (ACE-M), p. 83. Sixth International Conference on AIDS. San Franscico.
- R J Sydiskis
- D G Owen
Sydiskis, R. J., and D. G. Owen. June 1987. U.S. patent
4,670,265.