Ethiopian Medicinal Plants Traditionally Used for the Treatment of Cancer; Part 3: Selective Cytotoxic Activity of 22 Plants against Human Cancer Cell Lines

Medicinal plants have been traditionally used to treat cancer in Ethiopia. However, very few studies have reported the in vitro anticancer activities of medicinal plants that are collected from different agro-ecological zones of Ethiopia. Hence, the main aim of this study was to screen the cytotoxic activities of 80% methanol extracts of 22 plants against human peripheral blood mononuclear cells (PBMCs), as well as human breast (MCF-7), lung (A427), bladder (RT-4), and cervical (SiSo) cancer cell lines. Active extracts were further screened against human large cell lung carcinoma (LCLC-103H), pancreatic cancer (DAN-G), ovarian cancer (A2780), and squamous cell carcinoma of the esophagus (KYSE-70) by using the crystal violet cell proliferation assay, while the vitality of the acute myeloid leukemia (HL-60) and histiocytic lymphoma (U-937) cell lines was monitored in the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) microtiter assay. Euphorbia schimperiana, Acokanthera schimperi, Kniphofia foliosa, and Kalanchoe petitiana exhibited potent antiproliferative activity against A427, RT-4, MCF-7, and SiSo cell lines, with IC₅₀ values ranging from 1.85 ± 0.44 to 17.8 ± 2.31 µg/mL. Furthermore, these four extracts also showed potent antiproliferative activities against LCLC-103H, DAN-G, A2780, KYSE-70, HL-60, and U-937 cell lines, with IC₅₀ values ranging from 0.086 to 27.06 ± 10.8 µg/mL. Hence, further studies focusing on bio-assay-guided isolation and structural elucidation of active cytotoxic compounds from these plants are warranted.     

In Vitro Antileishmanial and Antischistosomal Activities of Anemonin Isolated from the Fresh Leaves of Ranunculus multifidus Forsk

Leishmaniasis and schistosomiasis are neglected tropical diseases (NTDs) infecting the world’s poorest populations. Effectiveness of the current antileishmanial and antischistosomal therapies are significantly declining, which calls for an urgent need of new effective and safe drugs. In Ethiopia fresh leaves of Ranunculus multifidus Forsk. are traditionally used for the treatment of various ailments including leishmaniasis and eradication of intestinal worms. In the current study, anemonin isolated from the fresh leaves of R. multifidus was assessed for its in vitro antileishmanial and antischistosomal activities. Anemonin was isolated from the hydro-distilled extract of the leaves of R. multifidus. Antileishmanial activity was assessed on clinical isolates of the promastigote and amastigote forms of Leishmania aethiopica and L. donovani clinical isolates. Resazurin reduction assay was used to determine antipromastigote activity, while macrophages were employed for antiamastigote and cytotoxicity assays. Antischistosomal assays were performed against adult Schistosoma mansoni and newly transformed schistosomules (NTS). Anemonin displayed significant antileishmanial activity with IC₅₀ values of 1.33 nM and 1.58 nM against promastigotes and 1.24 nM and 1.91 nM against amastigotes of L. aethiopica and L. donovani, respectively. It also showed moderate activity against adult S. mansoni and NTS (49% activity against adult S. mansoni at 10 µM and 41% activity against NTS at 1 µM). The results obtained in this investigation indicate that anemonin has the potential to be used as a template for designing novel antileishmanial and antischistosomal pharmacophores.     

Composition, antimicrobial and free-radical scavenging activities of the essential oil of Plectranthus marrubatus

Essential oil from the aerial part of Plectranthus marrubatus J. K. Morton (Lamiaceae), obtained by hydrodistillation was analyzed by gas chromatography/mass spectrometry (GC/MS) and evaluated for antimicrobial and free radical scavenging activities. Twenty-four compounds representing 99% of the total oil were identified. The major constituents were thymol, p-cymene and gamma-terpinene. The oil was tested against 21 bacterial and 4 fungal strains using the disc diffusion method and found to be active against a broad spectrum of pathogens including Gram-positive and Gram-negative bacteria as well as some fungal strains. The minimum inhibitory concentrations (MICs) of the oil against the bacterial strains tested ranged from 10 to 800 microg/mL, and from 400 to 800 microg/mL against the fungal strains employed. The in vitro antioxidant activity was assessed using 2,2-diphenyl-l-picrylhydrazil (DPPH) and showed a low EC50 value of 0.15 microl/mL. The study provides evidence for the broad-spectrum antimicrobial and antioxidant effect of Plectranthus marrubatus essential oil, and a possible explanation for its traditional use in the treatment of cold, fever, stomach disorder, diarrhea and as a skin cleaner.     

Free radical scavenging activity-guided isolation of a diterpenoid from Plectranthus punuctatus

Free radical scavenging activity-guided investigation of the acetone extract of Plectranthus punuctatus (L'Her) (Lamiaceae) resulted in the isolation of a novel diterpenoid 3,11,12,14,19-pentahydroxy-5,8,11,13-abietatraen-7-pyran[4,6]-16-dione whose structure was elucidated based on spectral evidence. The isolated compound showed a significant antioxidant activity in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and deoxyribose degradation assays with IC50 values of 9.65 microg/mL and 5.25 microg/mL, respectively.