The crystal structure of fac-tricarbonyl(N-benzoylN,N-cyclohexylmethylcarbamimidothioato-k(2)S,O)(pyridine-kN)rhenium(I), C23H24N3O4ReS

Please read abstract in the article.The National Research Foundation of South Africa, Tshwane University of Technology and the University of Pretoria.https://www.degruyter.com/view/j/ncrsChemistr

Review of the Traditional Uses, Phytochemistry, and Pharmacological Activities of Rhoicissus Species (Vitaceae)

Species within the genus Rhoicissus (Vitaceae) are commonly used in South African traditional medicine. The current review discusses the occurrence, distribution, traditional uses, phytochemistry, and pharmacological properties of Rhoicissus species covering the period 1981–2020. The data reported were systematically collected, read, and analysed from scientific electronic databases including Scopus, Scifinder, Pubmed, and Google Scholar. Reported evidence indicates that species in this genus are used for the treatment of gastrointestinal complaints, sexually transmitted infections (STIs), and infertility, as well as to tone the uterus during pregnancy and to facilitate delivery. Pharmacological studies have further shown that members of the Rhoicissus genus display antidiabetic, uterotonic, ascaricidal, hepatoprotective, antioxidant, antimicrobial, anticancer, and anti-inflammatory properties. They are linked to the presence of bioactive compounds isolated from the genus. Hence, Rhoicissus species can potentially be an alternative therapeutic strategy to treat diseases and develop safer and more potent drugs to combat diseases. Plant species of this genus have valuable medicinal benefits due to their significant pharmacological potential. However, scientific investigation and information of the therapeutic potential of Rhoicissus remain limited as most of the species in the genus have not been fully exploited. Therefore, there is a need for further investigations to exploit the therapeutic potential of the genus Rhoicissus. Future studies should evaluate the phytochemical, pharmacological, and toxicological activities, as well as the mode of action, of Rhoicissus crude extracts and secondary compounds isolated from the species

Flavonoids from the Genus Euphorbia

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents

Flavonoids from the genus Euphorbia : isolation, structure, pharmacological activities and structure–activity relationships

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as D-glucose, L-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.NRF-TWAS, South Africa, National Research Foundation Research and Tshwane University of Technology, Pretoria, South Africa.http://www.mdpi.com/journal/pharmaceuticalspm2022Paraclinical Science

In vitro cytotoxic effects of chemical constituents of Euphorbia grandicornis Blanc against breast cancer cells

Euphorbia grandicornis Blanc is widely utilized in traditional medicine for a variety of ailments including body pains associated with skin irritations, inflammation, and snake or scorpion bites. Compounds from E. grandicornis were characterized using spectroscopic techniques, NMR, IR, MS, and melting points and alongside the extracts were evaluated for in vitro anticancer activity against several cancer cell lines. The root extract afforded known, β-glutinol (1), β-amyrin (2), 24-methylenetirucalla-8-en-3β-ol (3), tirucalla-8,25-diene-3β,24R-diol (4), stigmasterol (5), sitosterol (6), and hexyl (E)-3-(4-hydroxy-3-methoxyphenyl)-2-propenoate (7) based on their NMR spectroscopic data for the first report in E. grandicornis. The extracts and isolated compounds were evaluated for anticancer activities against hormone receptor-positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines. The CH2Cl2 extract exhibited potent, cytotoxicity against MCF-7, HCC70, and MCF-12A cells. The aerial extract exhibited IC50 values of 1.03, 0.301, and 1.68 µg/mL, and root extract displayed IC50 values of 0.83, 0.83 and 3.98 µg/mL against MCF-7, HCC70, and MCF-12A cells respectively. The root extract thus showed selectivity for the cancer cell lines over the non-cancerous control cell line (SI = 4.80). Hexyl (E)-3-(4-hydroxy-3-methoxyphenyl)-2-propenoate (7) showed significant activity with IC50 values of 23.41, 29.45 and 27.01 µM against MCF-7, HCC70 and MCF-12A cells respectively, suggesting non-specific cytotoxicity

Cytotoxicity of triterpenoids from Clerodendrum glabrum against triple negative breast cancer cells in vitro:

Clerodendrum glabrum is an indigenous medicinal plant that is used to treat cough, cold, sore throat and chest complaints. The stem bark of Clerodendrum glabrum afforded four tritepenoids namely, 3β-olean-12-en-3-yl palmitate (β-amyrin palmitate), (1), 3β hydroxy 5-glutinene (glutinol), (2), 3β-lup-20(29)-en-3-palmitate (Lupeol-3-palmitate), (3), 3β-lup-20(29)-en-3-ol (lupeol) (4) and one common phytosterol (stigmasterol) (5). The structures were established on the basis of their spectroscopic analysis. The compounds were screened for cytotoxicity against the HCC70 triple negative breast cancer (TNBC), MCF-7 hormone receptor positive breast cancer and MCF-12A non-cancerous mammary epithelial cell lines

The Use of Medicinal Plant-Derived Metallic Nanoparticles in Theranostics

In the quest to effectively diagnose and treat the diseases that afflict mankind, the development of a tool capable of simultaneous detection and treatment would provide a significant cornerstone for the survival and control of these diseases. Theranostics denotes a portmanteau of therapeutics and diagnostics which simultaneously detect and treat ailments. Research advances have initiated the advent of theranostics in modern medicine. Overall, theranostics are drug delivery systems with molecular or targeted imaging agents integrated into their structure. The application of theranostics is rising exponentially due to the urgent need for treatments that can be utilized for diagnostic imaging as an aid in precision and personalised medicine. Subsequently, the emergence of nanobiotechnology and the green synthesis of metallic nanoparticles (MNPs) has provided one such avenue for nanoscale development and research. Of interest is the drastic rise in the use of medicinal plants in the synthesis of MNPs which have been reported to be potentially effective in the diagnosis and treatment of diseases. At present, medicinal plant-derived MNPs have been cited to have broad pharmacological applications and have been studied for their potential use in the treatment and management of cancer, malaria, microbial and cardiovascular diseases. The subject of this article regards the role of medicinal plants in the synthesis of MNPs and the potential role of MNPs in the field of theranostics

Ethnomedicinal and phytochemical properties of sesquiterpene lactones from Dicoma (Asteraceae) and their anticancer pharmacological activities : a review

Dicoma species belonging to the Asteraceae family are commonly utilized as traditional medicine in Southern Africa. Dicoma anomala, Dicoma capensis, Dicoma schinzii and Dicoma zheyeri are the most common ethnomedicinal plant species used in Southern Africa. The plant species of Dicoma genus are identified as the main source of sesquiterpene lactones. Dicoma species are associated with pharmacological properties such as antiviral, antibacterial, antihelminthic, antispasmodic antiplasmodial, as analgesic, antiinflammatory, , anticancer, , and wound healing properties. The plant species of Dicoma genus are identified as the main source of sesquiterpene lactones. In this review, the authors report the ethnomedicinal and phytochemical properties, and pharmacology of sesquiterpene lactones from the genus Dicoma from 1978 to 2020. There are over eighty (80) reported sesquiterpene lactones isolated from Dicoma species including, germacronolides, eudesmanolides, melampolides, guaianolides and pseudoguaianolides. Sesquiterpene lactones possess antimalarial, anticancer and antiinflammation activities due to their structural diversity. The diagnostic search on phytochemistry of sesquiterpene lactones from Dicoma carried out in the 70’s has limited pharmacological screening activities; hence these may need to be revisited and explored. Furthermore, the literature search conducted in this review showed that out of the 35 Dicoma species, seven species were investigated, and their medicinal uses, pharmacology and photochemistry reported. The recommendation drawn is that Dicoma species that are not investigated and not fully exploited should be studied for their phytochemicals and efficacy. The information compiled in this review on the pharmacological, phytochemistry and ethnomedicinal activities of genus Dicoma was obtained from relevant literature sources, including books, book chapters, websites, theses, reviews and research articles from databases such as Web of Science, Scopus, Science Direct, BioMed Central, Springer link, PubMed, and Google Scholar.The South African National Research foundation (NRF)http://www.elsevier.com/locate/sciafhj2022Chemistr

<i>Ent</i>-abietane diterpenoids from <i>Suregada zanzibariensis</i> Baill. (Euphorbiaceae), their cytotoxic and anticancer properties

<p>The stem bark extract of <i>Suregada zanzibariensis</i> afforded a previously undescribed <i>ent</i>-abietane diterpenoid trivially named mangiolide (<b>1</b>) and a known jolkinolide B (<b>2</b>) via anticancer bioassay-guided fractionation. The CH₂Cl₂:MeOH extract of <i>S. zanzibariensis</i> was initially analysed for its anticancer properties against three cancer cell lines, renal (TK10), melanoma (UACC62), and breast (MCF7) and was found to be potent at low μg/mL ranges. Compound <b>1</b>, 6α-acetoxy-14-keto-<i>ent</i>-abieta-7(8),13(15)-diene-16,12-olide (mangiolide) inhibited the growth of renal (TK10) with a GI₅₀ of 0.02 μg/mL; a GI₅₀ of 0.03 μg/mL for melanoma (UACC62) and a GI₅₀ of 0.05 μg/mL for breast (MCF7) cancer cell lines. Compound <b>2</b>, 8,13-diepoxy-13,15-<i>ent</i>-abietene-16,12-olide (jolkinolide B) inhibited the growth (GI₅₀) of the cell lines at 3.31 μg/mL for renal (TK10), 0.94 μg/mL for melanoma (UACC62) and 2.99 μg/mL for the breast (MCF7). The structures were established on the basis of their spectroscopic analysis and the absolute stereostructures assigned using electronic circular dichroism (ECD).</p