The research presented in this study combines natural product chemistry with organic / Thesis (M.Sc.)-University of KwaZulu-Natal, Pietermaritzburg, 2010.

All over Africa, traditional healers use medicinal plants to prepare medicines to treat a wide range of illnesses. One of these illnesses is sickle cell anaemia or drepanocytosis or sicklemia. This disease is particularly common among sub-Saharan Africans with a clear predominance in equatorial Africa. However, it also exists in North Africa, Greece, Turkey, Saudi Arabia and India. An estimated 50 million people are affected worldwide. A literature review on sickle cell anaemia revealed that a number of plants have anti-drepanocytosic activity. The availability and frequency of ethnobotanic use of plants were taken into account when selecting the plants investigated in this study. Cajanus cajan, Callistemon viminalis, Melaleuca bracteata var. Revolution Gold and Syzygium guineense (from DRC and South Africa) were selected for study. The selected plants were subjected to modern phytochemical analysis. A total of 8 compounds were isolated from the plants’ extracts and their structures determined by modern spectroscopic techniques (1D and 2D NMR, FT-IR and MS). S. guineense from DRC (Democratic Republic of Congo) yielded flavanonoid glycoside (A) as its major chemical constituent. The South African S. guineense afforded 4 compounds namely betulinic acid (B), sitosterol (C), friedelan-3-one (D) and a betulinic acid derivative (E). Cajanus cajan showed the presence of fatty acids, one of them was characterized as an unsaturated fatty acid (I). Callistemon viminalis afforded one compound, betulic acid (F) and Melaleuca bracteata afforded two compounds which were characterized as betulinic acid acetate (G) and ursolic acid acetate (H). CH3-(CH2)n-CH2-CH=CH-CH2-CH=CH-(CH2)n-CH2-CH2-COOH The investigation of the anti-drepanocytosis activities of the extractives and their crude extracts showed in vitro antisickling activity. Ethyl acetate crude extracts of Callistemon viminalis and Melaleuca bracteata; hexane, dichloromethane and ethyl acetate crude extracts of Syzygium guineense of DRC, betulinic acid, betulinic acid acetate and maslinic acid showed a high antisickling activity, more than 70% of normalization. The compound BF4, a fatty acid, from Melaleuca bracteata was found to have a medium activity, between 50 and 70% of normalization and oleanolic acid showed the weakest activity, between 10 and 50 % of normalization. Maslinic acid and oleanolic acid which were used for anti-sickling bioassay were isolated and characterized from Syzygium cordatum by my supervisor, Professor Shode. Others crude extracts and pure isolated compounds were found to be non-active antisickling agents. These included crude hexane and methanol extracts of Cajanus cajan; crude dichloromethane extract of Callistemon viminalis; crude dichloromethane, methanol and 80% aqueous methanol extracts of Melaleuca bracteata; crude hexane, dichloromethane, ethyl acetate, and methanol extracts of Syzygium guineense (South Africa); ursolic acid from Melaleuca bracteata and flavanone glycoside from Syzygium guineense of DRC. This is the first report of the in vitro anti-sickling activity of betunilic acid, betulinic acid acetate, oleanolic acid, and maslinic acid. / Thesis (M.Sc.)-University of KwaZulu-Natal, Westville, 2010.

Šio darbo tikslas buvo įvertinti medicininės dėlės (Hirudo verbana) jauniklių elgesį sudarant sankaupas, nustatyti sankaupų pokyčius laiko bėgyje bei veikiant terminiam ir šviesos dirgikliui. Vykdant uždavinį, ištirti jauniklių elgesį nuo jų išsiritimo iš kokonų momento iki pirmojo maitinimosi, buvo stebima, kad tik išsiritus jaunikliams iš kokonų, dar neperkėlus į vandenį, būdingos ryškios sankaupos 100% grupių. Perkėlus jauniklius į vandenį, labai trumpam dėl mechaninio poveikio, sankaupos iširsta, tačiau jau po 31,25±0.752 min. Išaiškinta, kad tiek mažo, tiek didelio tankio grupėms būdinga tendencija pirmąją savaitę sudaryti labai ryškias sankaupas, o su laiku jos pradeda irti. Lyginant šias grupes nustatyta, kad po 1 paros nuo išsiritimo negautas patikimas skirtumas tarp šių grupių, tačiau jau po 3 parų gautas patikimas skirtumas. Taip pat stebėti grupių sankaupų ryškumo skirtumai prieš maitinimąsi ir po. Gauta, kad statistiniai skirtumai yra labai patikimi nesvarbu kokio tankumo grupėse. Tyrimai parodė, kad sankaupų ryškumas grupėse, susidedančiose iš viename kokone buvusių jauniklių, nuo grupių, sudarytų iš įvairių kokonų jauniklių statistiškai nepatikimas. 640-670 lx apšvietimas stipriai paveikė dėles ir jos sudarė labai ryškias sankaupas. Rezultatai tarp eksperimentinių ir kontrolinių grupių yra labai patikimi. Tai dar kartą patvirtina neigiamą poveikį dėlėms, kurios pademonstravo ryškią apsauginę reakciją. Tiriant terminį poveikį jaunikliams, nustatyta vidutinė... [toliau žr. visą tekstą] / The aim of the study is to evaluate behaviour of medicinal juvenile leeches (Hirudo verbana) by composing aggregation, establishing changes in aggregation during effect of time also applying thermic and light stimulus. During investigation of juvenile leeches behaviour from leaving the cocoon to first feeding, first aim was to observe juvenile leeches which has just left the cocoon bearing in mind that leeches cannot be moved into water. Characteristics of this observation were 100% groups’ aggregation. Moving juvenile into the water for a short period of time due to mechanical effect, aggregations separate fast after 31,25±0.752 min. Observation concludes, that both large and small density groups have a tendency to show intense aggregations and with time aggregations starts to separate. Comparing these groups it was determined that after 1 day since hatching, significant effect was not achieved between these groups, but after 3 days significant effect have been achieved. In addition, group aggregation difference was observed before and after feeding. Achievement was that statistical difference was accurate disputing density groups. Experiments showed that aggregation intensity in groups were composed out of juvenile leeches that were in the cocoon and groups that were composed out of different cocoons were statistically unreliable. 640-670lx illumination strongly affected leeches and they composed intense aggregations. Results showed that results between experimental and... [to full text]

UA Open Access Publishing Fund / Background: Ethnobotanical knowledge continues to be important for treating illness in many rural communities, despite access to health care clinics and pharmaceuticals. However, access to health care clinics and other modern services can have an impact on the distribution of medical ethnobotanical knowledge. Many factors have been shown to be associated with distributions in this type of knowledge. The goal of the sub-analyses reported in this paper was to better understand the relationship between herbal remedy knowledge, and two such factors, age and social network position, among the Yucatec Maya in Tabi, Yucatan. Methods: The sample consisted of 116 Yucatec Maya adults. Cultural consensus analysis was used to measure variation in herbal remedy knowledge using competence scores, which is a measure of participant agreement within a domain. Social network analysis was used to measure individual position within a network using in-degree scores, based on the number of people who asked an individual about herbal remedies. Surveys were used to capture relevant personal attributes, including age. Results: Analysis revealed a significant positive correlation between age and the herbal medicine competence score for individuals 45 and under, and no relationship for individuals over 45. There was an insignificant relationship between in-degree and competence scores for individuals 50 and under and a significant positive correlation for those over 50. Conclusions: There are two possible mechanisms that could account for the differences between cohorts: 1) knowledge accumulation over time; and/or 2) the stunting of knowledge acquisition through delayed acquisition, competing treatment options, and changes in values. Primary ethnographic evidence suggests that both mechanisms may be at play in Tabi. Future studies using longitudinal or cross-site comparisons are necessary to determine the whether and how the second mechanism is influencing the different cohorts.

Flow chemistry can be characterized as a continuous chemical reaction system performed in solution in connecting tubing and flow reactors which is efficient. Photochemistry is the chemical reaction initiated by light, and is the result of the absorption of photon by a reagent or starting material. Poly (ADP-ribose) polymerase is a big family of proteins related to cellular repair and death. Phenanthridinones have been shown to exhibit PARP inhibitory potency as competitive inhibitors. Instead of using conventional costly and low-efficiency coupling reactions, we have managed to develop a method to synthesize phenanthridinone-type compounds by photo-cyclization under flow conditions for the purposes of generating novel PARP inhibitors. In total, we have generated a series of phenanthridinones in yields ranging from 13 % to 99%, 18 examples. Additionally, we have also developed a flow photocyclization method for the synthesis of complex heterocycles, naphthyridinones (5 examples, yields ranging from 24-52%) and thieno-quinolinones (18 examples, yields ranging from 23-90%), molecules that would be much more difficult to construct using conventional batch methods. Overall, we have demonstrated that a flow photocyclization pathway is a robust synthesis route for producing phenanthridinone-type compounds for the purposes of developing novel PARP inhibitors. / October 2016

In vitro cultures of medicinal plants - XI. Elicitation is one of the few strategies that can be used in enhancement of secondary metabolites production from explant cultures. The effect of abiotic elicitor (silver nitrate) on flavonolignan and flavonoid taxifolin production in suspension culture of Silybum marianum L. (Gaertn.) and on isoflavones production in suspension culture of Genista tinctoria L. was tested. Silver nitrate in various concentrations (5.887.10-3 mol/l; 5.887.10-4 mol/l; 5.887.10-5 mol/l) was used as elicitor. Content of secondary metabolites in suspension cultures was determinated by high performance liquid chromatography (HPLC). The samples were taken after 6, 12, 24, 48, 72 and 168 hours after elicitor treatment. The highest content of taxifolin production (0.02 %) in suspension culture of Silybum marianum L. (Gaertn.) after silver nitrate (5.887.10-4 mol/l) treatment and 72 h sampling was detected. The highest content of genistin (0.05 %) in suspension culture of Genista tinctoria L. was found after silver nitrate (5.887.10-4 mol/l) treatment and 48 h sampling. The highest content of daidzein (0.09 %) was detected after elicitor (5.887.10-4 mol/l) treatment and 168 h sampling.

Martina Janoutová In vitro cultures of medicinal plants - XII. Abstract The effect of ultrasound (US) as abiotic elicitor on the flavonolignans production in Silybum marianum L suspension culture was investigated. The culture was cultivated in Murashige and Skoog nutritive medium with ( - NAO) (g/l) as growth regulator at 25o C and luminous period 16 h of light and 8 h of darkness. The elicitor - ultrasound by frequency 35kHz and intensity 0,1Wcm-3 for a period 1, 2, 3, 4 and 5 min has been used. The samples were taken in 0, 6, 12, 24, 48, 72 and 168 h after US exposition. The control samples were taken in 0 and 48 h. The quantity of flavonolignans was determined by High performance liquid chromatography (HPLC). The highest increase of taxifolin content was apparent after 5 min of US elicitation and 48 h sampling (0,04%) - 400%, other increase was apparent after 5 min of elicitation and 72 h sampling. The higher content of silychristin was found after 1 min of US elicitation and 72 h sampling, the same level was observed after 2 min of elicitation and 24 h sampling. The higher level of silydianin was detected after 2 min of US elicitation and 6 h sampling and the silybin B after 2 min of elicitation and 12 h sampling after exposition. Taxifolin and flavonolignans release to the nutrient medium was...

Jan Kubeš Genista tinctoria in vitro - abiotická elicitace Cultures of medicinal plants in vitro - XIII. The plants cultures in vitro contain lesser amounts of secondary metabolites in compare with intact plants. The elicitors can affect these metabolites production. The effect of electric current (50mA) of different voltage (5, 7, 8, 10, 15, 20 and 24 V) and different time exposition (10, 30, and 60 minutes) on content of isoflavones was studied on (Genista tinctoria) suspension culture. The highest concentration of genistin (0.17 %) was measured in suspension culture after 30 min of elicitation by 10 V after 6 hours of cultivation. The highest concentration of daidzein (0.35 %) was found in suspension culture after 60 min of elicitation by 5 V after 24 hours of cultivation. The highest concentration of genistin (1.6 mg/100ml) was measured in medium after 30 min of elicitation by 5 V after 24 hours of cultivation. The highest concentration of daidzein (1.77 mg/100ml) was found in medium after 10 min of elicitation by 24 V after 6 hours of cultivation.

Introducción: Se cree que la uva Borgoña (Vitis vinifera Pinot Noir) presenta beneficios para la salud debido a la presencia de polifenoles concentrados en la cáscara. Estos fitoquímicos podrían tener un impacto importante en el tratamiento de la hiperlipemia. Objetivos: El objetivo del presente estudio fue determinar si la cáscara pulverizada de uva presenta efecto hipolipidémico en ratas con hiperlipemia inducida. Diseño: Estudio analítico, experimental y transversal. Material biologico: Ratas de cepa Holtzmann, Vitis vinifera variedad Pinot Noir Intervenciones: Las ratas se distribuyeron en 4 grupos de 6 individuos: Un control negativo (sin la enfermedad), un control positivo (8 mg/g de glutamato monosódico) y dos grupos experimentales (8 mg/g de glutamato monosódico más cáscara pulverizada de uva a las dosis de 50 mg/kg peso and 200 mg/kg peso). Luego de 30 días de tratamiento se procedió a medir la concentración de colesterol total, triglicéridos, HDL y LDL. Resultados: Se encontró disminución significativa de colesterol total y de LDL (p<0,05), pero no se observó diferencia significativa en la concentración de triglicéridos y HDL (p>0,05). Conclusiones. El pulverizado de cáscara de uva presenta efecto hipolipidémico bajo condiciones experimentales.

Introducción: Ansiedad enfermedad del milenio, el cual requiere tratamiento para evitar trastorno mayores. Objetivo: Determinar efecto sedante de Melissa officinalis “Toronjil” más Matricaria chamomilla “Manzanilla” sobre ansiedad inducida en ratones albinos. Diseño: Experimental. Lugar: Facultad de Medicina y Facultad de Farmacia y Bioquímica, Universidad Nacional Mayor de San Marcos. Material Biológico: ratones, ratas albinos. Intervenciones: Treintaises ratones fueron inducidos a hiperactividad y/o cambios conductuales por NMDA, considerándose grupos 1) SSF 10 mL/kg; 2) NMDA 75 mg/kg; 3, 4, 5) NMDA + Extracto 1, 2, 4 g/Kg correspondientemente, y 6) NMDA + DAP-7 antagónico del NMDA 0.33 nmol/kg; observándose hiperactividad, cambios conductuales, periodo latencia en minutos y porcentaje de protección. Se comparó el efecto sedante con diazepam en 30 ratones: 1) SSF 10 mL/kg; 2) diazepam 50 mg/kg; 3, 4, y 5) Extracto 1, 2, 4 g/kg respectivamente, midiéndose tiempo de dormir (minutos). Se realizó el estudio de estudio de toxicidad crónica a 60 días en 20 ratas divididos en 4 grupos: 1, 2 blanco control 3, 4, (extracto alcohólico) a dosis de 4 g/Kg. por vía oral, se evaluó los niveles tóxicos determinando a nivel, Bioquímicos: urea, colesterol, transaminasas, lipoproteína HDL e histología. Resultados: Los compuestos fenólicos y terpenoídes estuvieron en mayor cantidad en el extracto alcohólico; el 100% (p<0.05) de ratones mostró efecto sedante; los hallazgos hematológicos, bioquímicos se encontraron dentro de los límites aceptados; e histopatológicamente no hubo evidencia de cambios morfológicos. Conclusiones: El extracto alcohólico de hojas y flores de Melissa officinalis “Toronjil” más Matricaria chamomilla “Manzanilla” es sedante en ratones, y sin toxicidad en ratas. Palabras clave: Extracto alcohólico, sedación, plantas medicinales, NMDA, diazepam, DAP-7 / --- Introduction: Anxiety millennium ilness requires treatment to prevent further disorder. Objective: To determine the sedative effect of Melissa officinalis "Toronjil" Matricaria chamomilla more "Manzanilla" on anxiety induced in albino mice. Design: Experimental. Location: Faculty of Medicine and Faculty of Pharmacy and Biochemistry of the Mayor national university, San Marcos. Biological Material: Mice, albino rats. Interventions: 36 mice were induced hyperactivity and / or behavioral changes by NMDA, considering groups 1) SSF 10 mL / kg; 2) NMDA 75 mg / kg; 3, 4, 5) NMDA + Extract 1, 2, 4 g / Kg correspondingly, and 6) NMDA antagonist + DAP NMDA-7 0.33 nmol / kg; observed hyperactivity, behavioral changes, latency period in minutes and percentage of protection. Was compared the sedative diazepam in 30 mice: 1) SSF 10 mL / kg; 2) diazepam 50 mg / kg; 3, 4, and 5) Extract 1, 2, 4 g / kg, respectively, measured sleep time (minutes). Chronic toxicity study it has been made 60 days in 20 rats divided into 4 groups: 1, 2 white handle 3, 4, (alcoholic extract) at a dose of 4 g / kg., urea, cholesterol, transaminases, lipoprotein HDL and the histology: toxic levels by orraly determining a level Biochemicals evaluated. Results: The phenolic and terpenoid compounds were more abundant at the alcoholic extract; 100% (p <0.05) in mice showed sedative effect; hematological findings, biochemical were within accepted limits; and histopathologically there was evidence of morphological changes. Conclusions: The alcoholic extract of leaves and flowers of Melissa officinalis "Toronjil" Matricaria chamomilla more "Manzanilla" is sedative in mice without toxicity in rats. Keywords: Alcoholic extract, sedation, medicinal plants, NMDA, diazepam, DAP-7