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.

Polyphenolic Contents, Free Radical Scavenging and Cholinesterase Inhibitory Activities of Dalbergiella welwitschii Leaf Extracts.

A decoction of Dalbergiella welwitschii leaves has been used ethnomedicinally for the treatment of mental illness and inflammatory diseases amongst other diseases. In this study, the leaf methanol extract of D. welwitschii and its partition fractions: n-hexane, ethyl acetate and aqueous, were tested and evaluated for their polyphenolic contents, free radical scavenging and cholinesterase inhibitory activities. The total phenolic (TPC), flavonoid (TFC) and proanthocyanidin (TPA) contents were determined using standard colorimetric methods. The anti-radical activity of the extracts against the 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric ion and nitric oxide (NO) radicals as well as their effects on lipid peroxidation were monitored spectrophotometrically. The cholinesterase enzyme (AChE and BuChE) inhibitions by the extracts were determined by a modified method of Ellman. The result showed a concentration-dependent increase in inhibition of the free radicals and the cholinesterase enzymes, except for that of lipid peroxidation. The ethyl acetate (EtOAc) fraction exhibited the highest polyphenolic contents among the fractions, with a TPC of 1.08 mgGAE/g, TFC of 0.38 mgQuE/g and TPA of 0.21 mgGAE/g. It also demonstrated the highest free radical scavenging activities with 72.63% and 65.43% inhibitions of DPPH and NO, respectively. The EtOAc fraction inhibited AChE and BuChE enzymes with IC50 values of 0.94 and 8.49 mg/mL, respectively. Our findings show that the plant may have polyphenol contents, in particular in the methanol extract and EtOAc fraction. These extracts showed considerable free radical scavenging and cholinesterase inhibitory properties. Thus, the observed bioactivities may serve as a justification for its folkloric use as a remedy for mental illness. The study also provides relevant information that could help in the search for lead cholinesterase inhibitors from medicinal plants that can be exploited against neurodegenerative disorders.

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.

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.

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.

The protective effect of aqueous extract of Typha capensis rhizomes on cadmium-induced infertility in rats.

Background Typha capensis is one of the medicinal plants commonly used to manage male fertility problems. The objective of the present study was to assess its fertility-promoting effects in a rat model of cadmium-induced infertility. Methods A total of 30 male Wister rats were randomly divided into five groups of six animals each. Animals of group I, which served as control, were administered with cadmium chloride (CdCl2; 2.5 mg/kg) and normal saline (2 mL/kg). Group II was served with 0.5 mL normal saline only. Animals of groups III-V were treated with CdCl2 (2.5 mg/kg) plus T. capensis extract at doses of 100, 200, and 400 mg/kg, respectively. Animals were sacrificed under sedation. Testes and epididymal weights and sperm count were determined. Histological assessment of the testes was conducted. Results T. capensis at any dose did not improve (p > 0.05) testicular and epididymal weights compared with those of the CdCl2-exposed control group. Histology revealed moderate necrosis in the same group. T. capensis modestly increased the sperm count by 14%, 31%, and 35%, for groups treated with the extract at doses 100, 200, and 400 mg/kg, respectively, when compared with the CdCl2 control group, although the differences were not significant statistically (p > 0.05). Conclusions Results of our study demonstrated that T. capensis can neither offer protective effects against oxidative stress nor promote fertility in an animal model of cadmium-induced infertility.

Cardiovascular effects of Ekebergia capensis Sparrm (Meliaceae) ethanolic leaf extract in experimental animal paradigms.

The purpose of this study was to examine the in vivo effects of Ekebergia capensis leaf ethanolic extract (EKE) on the blood pressure of anaesthetised normotensive male Wistar rats and conscious weanling Dahl salt-sensitive (DSS) rats, which develop hypertension as they age. To investigate possible mechanism(s) of the extract's hypotensive effects, the contractile or relaxant responses to EKE in the absence or presence of reference drugs were evaluated in Wistar rat isolated aortic rings precontracted with methoxamine hydrochloride (ME, 10 microM). Acute intravenous administration of EKE elicited hypotensive responses in anaesthetised animals, while sub-chronic treatment with the extract averted the development of high blood pressure in weanling DSS rats. Isometric recordings of methoxamine hydrochloride (ME) pre-contracted, isolated, endothelium-intact and -denuded aortic rings revealed concentration-dependent relaxation responses to EKE (1-160 mg/ml). The potency was significantly less in the endothelium- denuded rings. Inhibitors of endothelium-derived relaxing factor (EDRF), L-NAME, methylene blue and indomethacin significantly reduced EKE-evoked vasorelaxations in endothelium-intact aortic rings. These results indicate that the vasorelaxant effect of EKE was in part mediated via EDRF-dependent or -independent pathways. These observations suggest that the hypotensive effect of EKE was in part mediated via modulation of total peripheral resistance of the vascular smooth muscles.

Cardiovascular effects of Helichrysum ceres S Moore [Asteraceae] ethanolic leaf extract in some experimental animal paradigms.

The aim of this study was to examine some in vivo and in vitro cardiovascular effects of Helichrysum ceres leaf ethanolic extract (HCE) in experimental animal paradigms. The acute effects of HCE on blood pressure were studied in anaesthetised normotensive male Wistar rats challenged with intravenous hypotonic saline infusion after a 3.5-hour equilibration for four hours of one-hour control, 1.5-hour treatment and 1.5-hour recovery periods. HCE was added to the infusate during the treatment period. Sub-chronic hypotensive effects of HCE were examined in weanling Dahl saltsensitive (DSS) genetically hypertensive rats, which progressively develop hypertension with age, treated with HCE (80 mg/kg) every third consecutive day for seven weeks. Isolated atrial muscle strips, portal veins and descending thoracic aortic rings of healthy normotensive Wistar rats were used to investigate the vascular effects of HCE. Acute HCE administration caused a significant (p < 0.05) fall in blood pressure in the normotensive anaesthetised Wistar rats. DSS hypertensive rats treated with HCE displayed low arterial blood pressure and heart rate values from weeks five to seven. HCE produced concentrationdependent negative inotropic and chronotropic effects on rat isolated electrically driven left, and spontaneously beating right atrial muscle preparations, respectively. HCE also evoked concentration-dependent relaxation responses of endothelium-intact aortic rings and portal veins isolated from healthy normotensive Wistar rats. The vasorelaxant effects of HCE in intact aortic rings were significantly reduced, but not completely abolished by adding endothelial- derived factor (EDRF) inhibitor, L-NAME, suggesting that the vasorelaxant effect of the extract is mediated via EDRF-dependent and independent mechanisms. The results of the study suggest that the hypotensive action of HCE is elicited, in part, directly by decreasing myocardial contractile performance and total peripheral vascular resistance due to its negative inotropic and chronotropic effects on rat isolated atrial muscle strips; and vasorelaxant effects on isolated vascular smooth muscles. The observed cardiovascular effects of HCE partly support the basis for its use in the management of high blood pressure in folkloric medicine.