Citrus limon Wastes from Part of the Eastern Cape Province in South Africa: Medicinal, Sustainable Agricultural, and Bio-Resource Potential.

The fruits of Citrus limon are often purchased for their vitamin C-rich juice, while the fruit peel and the tree leaves are discarded as wastes. This study obtained the chemical profiles of the essential oils (EOs) of C. limon wastes (the peel and leaves), evaluated their medicinal value as antioxidants, their potential for sustainable use in agriculture as an insecticide for post-harvest preservation of grains, and their potential as a bioresource in livestock feed formulations. The EOs were isolated from C. limon leaves and peel using a hydro-distillation method on a Clevenger apparatus. The oil constituents were identified using the gas chromatography-mass spectrometry (GC-MS) hyphenated technique. The oils were evaluated for their in vitro antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric-reducing antioxidant power methods. An insecticidal study was conducted using contact toxicity, fumigation, and repellence bioassay methods against Sitophilus zeamais (maize weevils). Finally, the predicted income from using lemon peel as an alternative or substitute ingredient for maize in livestock feed formulations was obtained through a conventional simulation method. Chemically, limonene was found to be present in all the EOs analyzed (12-52%), while α-pinene was only found in the fresh leaf and peel oils (13.3% and 10.6%). Caryophyllene oxide was identified as the major component of the dried leaf oil (17.7%). At 20 µg m, the dry peel oil exhibited the highest inhibitory activity (52.41 ± 0.26%) against the DPPH radical, which was comparable to L-ascorbic acid (a standard antioxidant) at 54.25 ± 3.55%. The insecticidal study revealed that the dry peel oil is a better insect repellent (73.33 ± 6.95% at 10 µL) and fumigant (LC50 = 0.17 µL g-1 after 48 h) natural agent compared to the peel oil. Conversely, the dry peel oil showed a better contact activity (LC50 = 1.69 µL g-1) against the maize weevils compared to the dry leaf oil. The simulation study showed the cost of using dry lemon peel as an alternative to maize in livestock feed formulation to be ZAR 2.8 billion, compared against the higher cost of feed formulation with maize, which currently stands at ZAR 24.9 billion. This study has shown that C. limon wastes (the peel and leaves) contain EOs with unique chemical profiles, valuable medicinal properties as free radical scavengers, and considerable insecticidal properties for agricultural use in post-harvest grain preservation, presenting a cost-effective and promising bioresource for livestock feed production.

Therapeutic Potential of Pectin and Its Derivatives in Chronic Diseases.

Non-communicable diseases (NCDs) are described as a collection of chronic diseases that do not typically develop from an acute infection, have long-term health effects, and frequently require ongoing care and therapy. These diseases include heart disease, stroke, cancer, chronic lung disease, neurological diseases, osteoporosis, mental health disorders, etc. Known synthetic drugs for the treatment or prevention of NCDs become increasingly dangerous over time and pose high risks due to side effects such as hallucination, heart attack, liver failure, etc. As a result, scientists have had to look for other alternatives that are natural products and that are known to be less detrimental and contain useful bioactive compounds. The increasing understanding of the biological and pharmacological significance of carbohydrates has helped to raise awareness of their importance in living systems and medicine, given they play numerous biological roles. For example, pectin has been identified as a class of secondary metabolites found in medicinal plants that may play a significant role in the treatment and management of a variety of NCDs. Pectin is mainly made of homogalacturonan, which is a linear polymer composed primarily of D-galacturonic acid units (at least 65%) linked in a chain by α-(1,4)-glycosidic linkages. There are also modified pectins or derivatives that improve pectin's bioavailability. Pectin is found in the cell walls of higher plants (pteridophytes, angiosperms, and gymnosperms), particularly in the middle lamella of the plant material. Citrus pectin is used in various industries. This article compiles information that has been available for years about the therapeutic importance of pectin in chronic diseases, different modes of pectin extraction, the chemistry of pectin, and the potency of pectin and its derivatives.

Synthesis of Ursolic Acid-based Hybrids: In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic Properties.

BACKGROUND: There is a critical need for the discovery of novel and effective antibacterial or anticancer molecules. OBJECTIVES: Amine-linked ursolic acid-based hybrid compounds were prepared in good yields in the range of 60-68%. METHODS: Their molecular structures were successfully confirmed using different spectroscopic methods including 1H/13C NMR, UHPLC-HRMS and FTIR spectroscopy. The in vitro cytotoxicity of some of these hybrid molecules against three human tumour cells, such as MDA-MB23, MCF7, and HeLa was evaluated using the MTT colorimetric method. RESULT: Their antibacterial efficacy was evaluated against eleven bacterial pathogens using a serial dilution assay. Majority of the bacterial strains were inhibited significantly by compounds 17 and 24, with the lowest MIC values in the range of 15.3-31.25 µg/mL. Compound 16 exhibited higher cytotoxicity against HeLa cells than ursolic acid, with an IC50 value of 43.64 g/mL. CONCLUSION: The in vitro antibacterial activity and cytotoxicity of these hybrid compounds demonstrated that ursolic acid-based hybrid molecules are promising compounds. Further research into ursolic acid-based hybrid compounds is required.

Chemical Composition, Analgesic and Anti-Inflammatory Activity of Pelargonium peltatum Essential Oils from Eastern Cape, South Africa.

Pelargonium species are native to South Africa, and they have a long history in medicinal use. This study aimed to extract essential oils from different parts of P. peltatum, determine the chemical composition of the essential oils, and assess the essential oils' biological potential as analgesic and anti-inflammatory agents. The essential oils were obtained by hydro-distilling different parts of P. peltatum, and the essential profile was determined by GC-FID and GC-MS. The analgesic activity of the essential oil was determined by using a tail immersion in hot water method in rats, whereas the anti-inflammatory activity of the essential oils was assessed according to right hind paw oedema induced by egg albumin; the three doses selected for each experiment were 100, 200, and 400 mg/kg. According to the GC-FID and GC-MS analysis, camphene (3.6-33.4%), α-terpineol (4.8-19.1%), α-thujone (1.5-15.6%), piperitone (0.9-12.2%), linalool (1.6-11.7%), myrcene (5.2-10.7%), germacrene D (3.7-10.4%), ß-caryophyllene (1.2-9.5%), ß-cadinene (3.4-6.7%), and ß-bourbonene (4.2-6.2%) were some of the major compounds identified in the oil. P. peltatum essential oils demonstrated analgesic activity by increasing pain latency in hot water; furthermore, in an inflammation test, the essential oil reduced the egg-albumin-induced paw oedema in both the first and second phases. Therefore, the current findings suggest that P. peltatum essential oils have analgesic and anti-inflammatory properties.

Synthesis of Ester-Linked Ursolic Acid-Based Hybrid Compounds: Potential Antibacterial and Anticancer Agents.

The molecular hybridization of two or more drugs into a single molecule is an effective drug design approach to reduce pill burden and improve patient treatment adherence. Ursolic acid-based hybrid compounds were synthesized and characterized followed by molecular docking studies. In vitro studies against various bacterial strains and human cancer cells (MDA-MB-231, HeLa, and MCF-7) were performed. Compounds 14-19, 21, 34, 31, and 30 demonstrated significant antibacterial activities with MIC values of 15.625 µg/ml. Compounds 29 and 34 were more cytotoxic than ursolic acid, with IC50 values of 46.99 and 48.18 µg/ml. Compounds 29 and 34 in the docking studies presented favourable binding interactions and better docking energy against the Epidermal Growth Factor Receptor (EGFR) than the parent compound, ursolic acid. The findings revealed that the ursolic acid scaffold is a promising precursor for the development of molecules with promising anticancer and antimicrobial activities. However, more studies are needed to fully understand their mode of action.

Enzyme Activities in Reduction of Heavy Metal Pollution from Alice Landfill Site in Eastern Cape, South Africa.

Heavy metals are unbreakable, and most of them are poisonous to animals and people. Metals are particularly concerning among environmental contaminants since they are less apparent, have extensive effects on ecosystems, are poisonous, and bioaccumulate in ecosystems, biological tissues, and organs. Therefore, there is a need to use biological agents and phytoremediation processes such as enzymes because they have a high potential for effectively transforming and detoxifying polluting substances. They can convert pollutants at a detectable rate and are potentially suitable for restoring polluted environments. We investigated heavy metal concentrations in different soil samples collected in four sections in Alice and determined the enzyme activity levels present in the soil. The Pearson correlation analysis was conducted to check whether there was any relationship between heavy metal concentrations and enzyme activities in the soil. Samples were randomly collected in three weeks, and the microwave digestion method was used for sample treatment and preparation. Quantitation was achieved by inductively coupled plasma mass spectrometry (ICP-MS). The enzyme assay through incubation method was implemented for discovering the four selected enzymes (urease, invertase, catalase, and phosphatase), and their activity levels were examined colorimetrically by colorimetry spectrophotometer. The ICP-MS results revealed 16 predominating elements, namely: Al, Ba, Ca, Co, Cr, Cu, Fe, K, Mg, Mn, Na, Ni, Sr, and Zn, and the presence of a non-mental, which is phosphorus (P), and a metalloid in the form of silicon (Si) in all soil samples. Significant differences in metal concentrations were observed among the collection sites. The Al, Fe, K, Mg, and Ca concentrations were above WHO's permissible limits. While Ba, Mn, Na, and P were in moderate concentration, Cu, Cr, Co, Zn, Sr, and Ni were in small amounts recorded mostly below the permissible values from WHO. Four soil enzyme activities were determined successfully (urease, invertase, phosphatase, and catalase). A negative non-significant correlation existed between urease, invertase, phosphatase enzyme activity, and the concentration levels of all selected metals (Al, Ba, Ca, Co, Cu, Fe, K, Mg, Mn, Na, Ni, Cr, Sr, and Zn. In contrast, the content of catalase activity was associated non-significantly but positively with the range of selected heavy metals. This study suggests proper monitoring of residences' areas, which can provide detailed information on the impact of high heavy metal content on people's health. They are easily dispersed and can accumulate in large quantities in the soil. The necessary implementation of waste management programs will help the municipality adopt a strategy that will promote recycling programs and protect the residence health from this threat.

The Medicinal Natural Products of Cannabis sativa Linn.: A Review.

Cannabis sativa is known among many cultures for its medicinal potential. Its complexity contributes to the historical application of various parts of the plant in ethno-medicines and pharmacotherapy. C. sativa has been used for the treatment of rheumatism, epilepsy, asthma, skin burns, pain, the management of sexually transmitted diseases, difficulties during child labor, postpartum hemorrhage, and gastrointestinal activity. However, the use of C. sativa is still limited, and it is illegal in most countries. Thus, this review aims to highlight the biological potential of the plant parts, as well as the techniques for the extraction, isolation, and characterization of C. sativa compounds. The plant produces a unique class of terpenophenolic compounds, called cannabinoids, as well as non-cannabinoid compounds. The exhaustive profiling of bioactive compounds and the chemical characterization and analysis of C. sativa compounds, which modern research has not yet fully achieved, is needed for the consistency, standardization, and the justified application of Cannabis sativa products for therapeutic purposes. Studies on the clinical relevance and applications of cannabinoids and non-cannabinoid phenols in the prevention and treatment of life-threatening diseases is indeed significant. Furthermore, psychoactive cannabinoids, when chemically standardized and administered under medical supervision, can be the legal answer to the use of C. sativa.

Polymer-Based Scaffolds Loaded with Aloe vera Extract for the Treatment of Wounds.

The treatment of wounds is one challenging biomedical field due to delayed wound healing common in chronic wounds. Several factors delay wound healing, including microbial infections, malnutrition, underlying physiological conditions, etc. Most of the currently used wound dressing materials suffer from poor antimicrobial properties, poor biodegradability and biocompatibility, and weak mechanical performance. Plant extracts, such as Aloe vera, have attracted significant attention in wound management because of their interesting biological properties. Aloe vera is composed of essential constituents beneficial for the wound healing process, such as amino acids, vitamins C and E, and zinc. Aloe vera influences numerous factors that are involved in wound healing and stimulates accelerated healing. This review reports the therapeutic outcomes of aloe vera extract-loaded polymer-based scaffolds in wound management.

Chemical Profiling, Toxicity and Anti-Inflammatory Activities of Essential Oils from Three Grapefruit Cultivars from KwaZulu-Natal in South Africa.

The medicinal potential and volatile composition of different parts of three cultivars of grapefruit (Citrus paradisi) were evaluated for their toxicity and anti-inflammatory activities. Fresh leaf and fruit peel were separately isolated by hydrodistillation for 4 h. The essential oils were subjected to GC/GC-MS analysis for chemical profile. Toxicity of the essential oils in mice were evaluated using Lorke's method, while an anti-inflammatory assay was performed in a rat model using egg albumin-induced oedema. The oils obtained were light yellow in colour, and odour varied from strong citrus smell to mild. Percentage yield of fresh peel oil (0.34-0.57%) was greater than the fresh leaf oil yield (0.21-0.34%). D-limonene (86.70-89.90%) was the major compound identified in the leaf oil, while ß-phellandrene (90.00-91.01%) dominated the peel oil. At a dosage level of 5000 mg/kg, none of the oils showed mortality in mice. An anti-inflammatory bioassay revealed that all the oils caused a significant (p < 0.05-0.01) reduction in oedema size when compared to the negative control group throughout the 5 h post induction assessment period. The study reveals that the oils are non-toxic and demonstrate significant anti-inflammatory activity. Our findings suggest that the leaf and peel oils obtained from waste parts of grapefruit plants can be useful as flavouring agents, as well as anti-inflammatory agents.

Pentacyclic Triterpenoids with Nitrogen-Containing Heterocyclic Moiety, Privileged Hybrids in Anticancer Drug Discovery.

Pentacyclic triterpenoids are well-known phytochemicals with various biological activities commonly found in plants as secondary metabolites. The wide range of biological activities exhibited by triterpenoids has made them the most valuable sources of pharmacological agents. A number of novel triterpenoid derivatives with many skeletal modifications have been developed. The most important modifications are the formation of analogues or derivatives with nitrogen-containing heterocyclic scaffolds. The derivatives with nitrogen-containing heterocyclic compounds are among the most promising candidate for the development of novel therapeutic drugs. About 75% of FDA-approved drugs are nitrogen-containing heterocyclic moieties. The unique properties of heterocyclic compounds have encouraged many researchers to develop new triterpenoid analogous with pharmacological activities. In this review, we discuss recent advances of nitrogen-containing heterocyclic triterpenoids as potential therapeutic agents. This comprehensive review will assist medicinal chemists to understand new strategies that can result in the development of compounds with potential therapeutic efficacy.

Synthesis, Antibacterial, and Cytotoxicity Evaluation of Oleanolic Acid-4-aminoquinoline Based Hybrid Compounds.

AIM: The study aims to prepare a class of oleanolic-based compounds. BACKGROUND: Conventional drugs used to treat infectious diseases suffer from limitations such as drug toxicity and drug resistance. The resistance of microbes to antimicrobial agents is a significant challenge in treating microbial infections. Combining two or more drugs with different modes of action to treat microbial infections results in a delay in developing drug resistance by the microbes. However, it is challenging to select the appropriate drugs for combination therapy due to the differences in stability and pharmacokinetic profile of the drugs. Therefore, developing hybrid compounds using the existing drugs is a promising approach to design effective antimicrobial agents. OBJECTIVES: To prepare oleanolic-based hybrid compounds followed by characterization, in vitro antibacterial and cytotoxicity evaluation. METHODS: Oleanolic acid-4-aminoquinoline-based hybrid compounds were synthesized via esterification and amidation. The compounds were characterized using FTIR, NMR, and UHPLC-HRMS. Oleanolic acid (OA) was isolated from the flower buds of Syzygium aromaticum (L.) Merr. & L.M.Perry, a species from Kingdom Plantae, order Mytales in the Myrtaceae family. Antibacterial activity was determined against selected strains of bacteria using the microdilution assay and cytotoxicity activity was assessed using the sulforhodamine B assay against selected cancer cell lines. RESULTS: The synthesized hybrid compounds exhibited antibacterial activity against the Gram-positive bacteria Enterococcus faecalis (ATCC13047), Bacillus subtilis (ATCC19659), Staphylococcus aureus as well as Gram-negative bacteria, Klebsiella oxytoca (ATCC8724), Escherischia coli (ATCC25922), and Proteus vulgaris (ATCC6380) with minimum inhibitory concentrations of 1.25 mg/mL compared to oleanolic acid (2.5 mg/mL). Compounds 13 and 14 displayed cytotoxicity in vitro against the cancer cell lines (MCF-7 and DU 145) compared to the oleanolic acid (IC50 ˃ 200 µM). CONCLUSION: Modification of C28 of OA enhanced its biological activity.

Ursolic Acid-Based Derivatives as Potential Anti-Cancer Agents: An Update.

Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.

The Effects of Physicochemical Parameters on Analysed Soil Enzyme Activity from Alice Landfill Site.

The soil pollution as a product of xenobiotics, industrial action, agricultural chemicals, or inappropriate disposal of waste can change the natural environment of soil indices and trigger life-threatening situations. Soil enzyme activity is the suitable bio-indicator or parameter for monitoring soil pollution due to their sensitivity that quickly responds to any soil disturbances. Also, they are known to play an essential role in maintaining soil health and a quality environment. This study aimed to determine the levels of enzyme activity in soil from polluted and unpolluted sites and study the relationship between the physicochemical properties and soil enzyme activity to manage soil pollution. Four selected enzymes (Urease, Invertase, Catalase, and Phosphatase) were examined for their activity from forty samples using the assay method for 24 h; the colorimetry spectrophotometer measured their activity. The obtained data revealed that Invertase activity was a predominant enzyme in all soil samples. Whereas, the urease activity had obtained in low amounts for all collection sites, especially on Site A1. Soil pH had discovered to range between 5.8 and 8.51, moisture content values recorded to vary from 0.12% to 9.09%, and soil organic carbon recorded to fluctuate between 0.08% and 1.54%. Urease and phosphatase activity correlated positively with all soil physicochemical properties except for moisture content, which correlated negatively (r = -0.297; p ≥ 0.05). The invertase activity negatively associated all soil physicochemical properties, excluding the moisture content that correlated positively and significantly with invertase activity. We noted that the dumpsite soil contains low enzyme activity levels, which might attribute to the type of waste disposed off. Also, only the phosphatase activity reported correlating positively with all examined physicochemical parameters entirely.

In Vitro and In Vivo Antioxidant Properties of Taraxacum officinale in Nω-Nitro-l-Arginine Methyl Ester (L-NAME)-Induced Hypertensive Rats.

Oxidative stress has gained attention as one of the fundamental mechanisms responsible for the development of hypertension. The present study investigated in vitro and in vivo antioxidant effects of 70% ethanol-water (v/v) leaf and root extracts of T. officinale (TOL and TOR, respectively). Total phenolic and flavonoid content of plant extracts were assessed using Folin Ciocalteau and aluminium chloride colorimetric methods; while, 2,2-diphenyl-1-picrlhydrazyl (DPPH), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant power (FRAP) protocols were used to determine the free radical scavenging and total antioxidant capacities (TAC), respectively. The in vivo total antioxidant capacity and malondialdehyde acid (MDA) levels for lipid peroxidation tests were performed on organ homogenate samples from Nω-nitro-L-arginine methyl ester (L-NAME)-induced hypertensive rats treated with leaf extract, TOL (500 mg/kg/day) and TOR (500 mg/kg/day) for 21 days. Results showed that compared to TOR, TOL possessed significantly higher (p < 0.01) polyphenol (4.35 ± 0.15 compared to 1.14 ± 0.01) and flavonoid (23.17 ± 0.14 compared to 3 ± 0.05) content; free radical scavenging activity (EC50 0.37 compared to 1.34 mg/mL) and total antioxidant capacities (82.56% compared to 61.54% ABTS, and 156 ± 5.28 compared to 40 ± 0.31 FRAP) and both extracts showed no toxicity (LD50 > 5000 mg/kg). TOL and TOR significantly (p < 0.01) elevated TAC and reduced MDA levels in targets organs. In conclusion, T. officinale leaf extract possesses significant anti-oxidant effects which conferred significant in vivo antioxidant protection against free radical-mediated oxidative stress in L-NAME-induced hypertensive rats.

Ursolic Acid and Its Derivatives as Bioactive Agents.

Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 ß-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCDs.

Antihypertensive effects of the hydro-ethanol extract of Senecio serratuloides DC in rats.

BACKGROUND: Senecio serratuloides DC is used in folk medicine for treating hypertension, skin disorders, internal and external sores, rashes, burns and wounds. This study aimed at investigating the antihypertensive effects of the hydroethanol extract of S. serratuloides (HESS) in N-Nitro-L-arginine methyl ester (L-NAME) induced hypertension in rats. METHODS: Acute toxicity of HESS was first determined to provide guidance on doses to be used in this study. Lorke's method was used to determine safety of the extract in mice. Female Wistar rats were treated orally once daily with L-NAME (40 mg/kg) for 4 weeks and then concomitantly with L-NAME (20 mg/kg) and plant extract (150 and 300 mg/kg), captopril (20 mg/kg) or saline as per assigned group for 2 weeks followed by a 2-week period of assigned treatments only. Blood pressure was monitored weekly. Lipid profile, nitric oxide, renin and angiotensin II concentrations were determined in serum while mineralocorticoid receptor concentration was quantified in the kidney homogenate. Nitric oxide (NO) concentration was determined in serum and cardiac histology performed. RESULTS: HESS was found to be non-toxic, having a LD50 greater than 5000 mg/kg. Blood pressure increased progressively in all animals from the second week of L-NAME treatment. HESS treatment significantly and dose-dependently lowered systolic blood pressure (p < 0.001), diastolic blood pressure (p < 0.01), low density lipoprotein cholesterol (p < 0.01) and triglycerides (p < 0.01). It significantly prevented L-NAME induced decrease in serum angiotensin II (p < 0.01), high density lipoprotein cholesterol (p < 0.001) and serum nitric oxide concentrations (p < 0.001). HESS also significantly (p < 0.01) prevented collagen deposition in cardiac tissue. CONCLUSION: The hydro-ethanol extract of Senecio serratuloides showed antihypertensive, antihyperlipidemic and cardioprotective effects in rats thus confirming its usefulness in traditional antihypertensive therapy and potential for antihypertensive drug development.

Antiviral Activities of Oleanolic Acid and Its Analogues.

Viral diseases, such as human immune deficiency virus (HIV), influenza, hepatitis, and herpes, are the leading causes of human death in the world. The shortage of effective vaccines or therapeutics for the prevention and treatment of the numerous viral infections, and the great increase in the number of new drug-resistant viruses, indicate that there is a great need for the development of novel and potent antiviral drugs. Natural products are one of the most valuable sources for drug discovery. Most natural triterpenoids, such as oleanolic acid (OA), possess notable antiviral activity. Therefore, it is important to validate how plant isolates, such as OA and its analogues, can improve and produce potent drugs for the treatment of viral disease. This article reports a review of the analogues of oleanolic acid and their selected pathogenic antiviral activities, which include HIV, the influenza virus, hepatitis B and C viruses, and herpes viruses.

Evaluation of Trace Metal Profile in Cymbopogon validus and Hyparrhenia hirta Used as Traditional Herbs from Environmentally Diverse Region of Komga, South Africa.

FAAS was used for the analysis of trace metals in fresh and dry plant parts of Cymbopogon validus and Hyparrhenia hirta species with the aim of determining the trace metals concentrations in selected traditional plants consumed in Eastern Cape, South Africa. The trace metal concentration (mg/kg) in the samples of dry Cymbopogon validus leaves (DCVL) showed Cu of 12.40 ± 1.000; Zn of 2.42 ± 0.401; Fe of 2.50 ± 0.410; Mn of 1.31 ± 0.210; Pb of 3.36 ± 0.401 mg/kg, while the samples of fresh Hyparrhenia hirta flowers (FHHF) gave Cu of 9.77 ± 0.610; Zn of 0.70 ± 0.200; Fe of 2.11 ± 0.200; Mn of 1.15 ± 0.080; Pb of 3.15 ± 0.100 mg/kg. Abundance of metal concentrations follows the order: Cu > Fe > Pb > Mn > Zn in the flower samples of Cymbopogon validus and Hyparrhenia hirta species. The concentrations of trace metals in both plant parts were below the permissible limits (PL) set by WHO. It is suggested that pharmacovigilance be carried out periodically to improve the quality, safety, and efficiency of various herbal products.

Semisynthesis of Derivatives of Oleanolic Acid from Syzygium aromaticum and Their Antinociceptive and Anti-Inflammatory Properties.

Oleanolic acid is a pentacyclic triterpenoid compound widely found in plants and well known for its medicinal properties. Oleanolic acid (OA) was isolated from the ethyl acetate extract of Syzygium aromaticum flower buds. Semisynthesis afforded both acetate and ester derivatives. The derived compounds were monitored with thin layer chromatography and confirmed with nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry (MS), Fourier infrared (FT-IR) spectroscopy, and melting point (Mp). All these compounds were evaluated for their analgesic and anti-inflammatory properties at a dose of 40 mg/kg. Significant analgesic and anti-inflammatory effects were noted for all OA-derived compounds. In the formalin-induced pain test, the derivatives showed better analgesic effects compared to their precursor, whereas, in the tale flick test, oleanolic acid proved to be superior in analgesic effects compared to all its derivatives with the exception of the acetyl derivative. Acute inflammatory tests showed that acetyl derivatives possessed better anti-inflammatory activity compared to the other compounds. In conclusion, semisynthesis of oleanolic acid yielded several derivatives with improved solubility and enhanced analgesic and anti-inflammatory properties.

Synthesis of Silver Nanoparticles Using Buchu Plant Extracts and Their Analgesic Properties.

We herein report for the first time the synthesis and analgesic properties of silver nanoparticles (Ag-NPs) using buchu plant extract. The as-synthesised Ag-NPs at different temperatures were characterised by UV-Vis spectroscopy, Fourier transform infra-red spectroscopy (FTIR) and transmission transform microscopy (TEM) to confirm the formation of silver nanoparticles. Phytochemical screening of the ethanolic extract revealed the presence of glycosides, proteins, tannins, alkaloids, flavonoids and saponins. The absorption spectra showed that the synthesis is temperature and time dependent. The TEM analysis showed that the as-synthesised Ag-NPs are polydispersed and spherical in shape with average particle diameter of 19.95 ± 7.76 nm while the FTIR results confirmed the reduction and capping of the as-synthesised Ag-NPs by the phytochemicals present in the ethanolic extract. The analgesic study indicated that the combined effect of the plant extract and Ag-NPs is more effective in pain management than both the aspirin drug and the extract alone.