Isolation of the antidiarrhoeal tiliroside and its derivative from Waltheria indica leaf extract

The antidiarrhoeal effect of Waltheria indica methanol extract and fractions have been reported earlier but, the present work examined the intestinal relaxant effects of two flavonoid-phenyl propanoids isolated from the methanol extract. The active aqueous fraction was subjected to vacuum liquid chromatography using dichloromethane with increasing concentration of ethyl acetate, and that of methanol and water successively. The ten (10) fractions obtained were combined to give seven (7). The fraction 2 (C, D) was subjected to preparative thin layer chromatography on silica gel GF254 (10-40μm) using CHCl3-CH3OH (8:2) to obtain compound coded F2. Fraction 4 (F) was subjected to column chromatography using silica gel (60-120μm mesh) and eluted with dichloromethane with increasing concentrations of methanol. Fractions 9-28 were combined and subjected to column chromatography using chloroform with increasing concentration of methanol. The fractions 1-16 of these were purified on Sephadex LH-20 to obtain compound BAA. The identities of the two compounds were established using spectroscopic methods. The antidiarrheal effect of compound F2 was evaluated on mice using charcoal transit (100,200, 400mg/kg), castor oil (40, 60 mg/kg) while the two compounds were examined for their inhibitory effects on Ach-induced ileum contraction. The effects of the compounds were compared with loperamide (3mg/kg) and atropine (80μg). Compounds F2 and BAA were identified as tiliroside and 3’’’, 5’’’-dimethoxy tiliroside respectively. Tiliroside inhibited the charcoal transition in the animals in a dose dependent pattern with 400mg/ mL eliciting 63.41% inhibition compared to 59.23% produced by loperamide. The compound also elicited significantly (P<0.05) prolonged onset of stooling and reduced the number and weight of stools produced lower than the control. The two compounds drastically inhibited the Ach-induced contractions of the ileum. The compound, tiliroside at 10mg, completely abolished the contraction by Ach unlike 3’’’, 5’’’-dimethoxy tiliroside which reduced the contraction to 1.92% at 20mg. The identified compounds seem to be responsible for the ethnomedicinal use of the plant in treating diarrhea.

Antibacterial activity of Urena lobata against uropathogens

Urinary tract infections (UTI) are one of the most common form of bacterial infections but the treatment becomes cumbersome as the etiological bacteria are developing resistance against antibiotics. This present study evaluated the efficacy of antimicrobial activity of Urena lobata against uropathogens. Six urine samples from UTI patients were collected from Pathological Laboratory, G.B. Vaghani Multispecialty Hospital, Surat. Bacteria were isolated from these samples using Nutrient agar, Mac Conkey agar plate, Blood agar, Mannitol salt agar, Eosin Methylene Blue agar and King’s agar. The bacterial isolates were identified using cultural characteristics, microscopic features and biochemical characteristics. Leaf extract of Urena lobata was prepared using Soxhlet Extraction Method whereby methanol and distilled water were the extractants used. Herbal extract disc was prepared at concentrations of 50,75, and100 mg/ml and tested against all the isolates. DMSO and antibiotics (Nitrofurantion, Amikacin, Levofloxacin, Norofloxacin, Ofloxacin and Cephalosporins) were used as negative and positive controls respectively.Staphylococcus aureus, Escherichia coli, Bacillus cereus, Streptococcus pneumoniae, Klebsiella spp. and Brevibacillus panacihumi were isolated from the urine samples. All concentrations of aqueous and methanolic extracts of U. lobata leaf displayed highest zone of inhibition against B. cereus. No inhibitory effect was observed against the growth of Klebsiella except at the highest concentrations. Further study is encouraged on the in-vivo study of efficacy of U. lobata on etiological agent of UTI.

In vitro antioxidant activity and phytochemical analyses of Acalypha godseffiana (Euphobiaceae) leaf extracts

The presence of various bioactive components makes it necessary to analyse plants for their potential to act as a source of useful treatments and cures for many inflammatory, infectious and pathogenic diseases. This study was carried out to determine phytochemicals and in-vitro antioxidant activities of the leaf extracts of Acalypha godseffiana. The leaves of A. godseffiana were collected, dried, pulverized and extracted separately with methanol and water using maceration method. The extract was concentrated in vacuo with rotary evaporator at 40oC. The extracts were subjected to quantitative phytochemical analysis and different anti-oxidant analytical procedures like FRAP, DPPH etc to determine the radical scavenging capabilities. The results of phytochemical analysis estimated the quantities and revealed the presence of alkaloids, flavonoids, tannins, saponins and terpenoids which varied in both extracts. The methanol and aqueous extracts exhibited antioxidant activities with relatively high IC50 (IC50 = 3.67 ìg/ml and 4.42ìg/ml respectively) which accounted for a low free radical-scavenging activity when compared with the reference antioxidant, vitamin C (IC50 = 1.51ìg/ml). The results of the study indicates that A. godseffiana leaf extracts contain secondary metabolites and possesses antioxidant properties.

Investigation on the antimalarial properties of Plumeria alba Linn (apocynaceae) cultivated in Nigeria

Many of the African antimalarial ethno medicinal plants are good sources of promising antimalarial compounds. The stem bark of Plumeria alba Linn, was evaluated for in vivo chemosuppressive antimalarial activities in order to identify the most active solvent fraction from which antimalarial constituents can be isolated. The stem-bark of Plumeria alba Linn, family Apocynaceae was collected, air-dried, powdered, macerated in methanol and the extract concentrated in vacuo. The acute toxicity study was performed on the extract using Lorke’s method. The extract was thereafter tested for chemosuppressive antiplasmodial activities against Plasmodium berghei berghei NK65- infected mice using Peter’s four-day test at doses 100-800 mg /kg with normal saline (0.2 ml) and chloroquine (10 mg/kg) as negative and positive control drugs respectively. The average percentage parasitaemia, percentage chemosuppression and effective doses (ED50 and ED90), the survival times and percentage survivors elicited in all the mice were determined as indices of antimalarial activity. The active extract was subsequently partitioned successively into n-hexane, dichloromethane, ethyl acetate and butanol. The respective partitioned fractions with the aqueous phase were also tested as above at doses 0-80 mg/kg. All results were subjected to statistical analysis using ANOVA with Student Newman Keul’s post hoc test. Crude extracts of P. alba gave considerable reduction of percentage parasitaemia up to 200 mg/kg. The percentage chemosuppression at all doses, were significantly higher (p<0.05) than the negative but lower than the positive control with 200 mg/kg dose showing the highest activity of 65.88 %. The effective doses, ED50 and ED90 were 305.82±9.99 and 389.74± 9.60, respectively. The most active n-hexane partitioned fraction elicited a percentage chemosuppression of 67.75 and a significantly lower (p<0.05) ED50 and ED90 of 31.27±0.85 and 54.80±1.75 mg/kg. The butanol and ethyl acetate partitioned fractions gave significantly higher (p<0.05) survival time value than those of the crude extract, other partition fractions and the positive control, while the n-hexane, dichloromethane and the aqueous, just like chloroquine, gave high percentage survivors. The study concluded that Plumeria alba stem-bark extract was active as an antimalarial drug with its antiplasmodial and the survival time–enhancing activity concentrated in the n-hexane and ethyl acetate with butanol partitioned fractions respectively, thus confirming and justifying its ethnomedical application in malaria.

Correlation between tumor markers in pre and post treatment of pancreatic cancer patients

One of the main causes of death in India is pancreas cancer. Various blood tumour indicators such as 19-9 carbohydrate antigen (CA19-9), antigen125 carbohydrate (CA125), antigen carcinoembryogenic (CEA) and alphaetoprotein (AFP) imbalance are observed in therapy for cancer. In disease predictions, thorough monitoring of the change in serum tumour markers was highly essential. The present investigation was thus conducted to examine serum marker tumour profiles before and after therapy of individuals with pancreatic cancer. The study comprised 400 individuals from both sexes suffering from pancreatic carcinogenic malignancy. In the pre and post-treatment of patients we detected serum tumour markers. In post-treatment groups, serum tumour marker levels were lower than before the individuals were treated. However, using pairs of samples t-testing at pfleg.0.05 these changes were statistically significant. Marker alterations in the serum tumour have shown risk for individuals. These alterations therefore enable the cancer individuals to predict and monitor properly.

Chemical composition and anticancer effects of Hyptis Suaveolens L. Poit (lamiaceae) volatile oil

The leaf of Hyptis suaveolens have found application in ethnomedicine in the treatment of various ailments including those that are related to tumor and cancer. This study was therefore undertaken to evaluate the cytotoxic effects of its volatile oil. Volatile oil distilled from freshly collected leaves using a Clavenger-type apparatus was screened using tadpoles of Raniceps ranninus (10-40 µg/mL) and brine shrimp of Artemia salina (10-1000 µg/mL) with bench-top assay procedures for cytotoxicity while growth inhibitory activity was assessed using radicles of Sorghum bicolor seeds (1-30 mg/mL). The essential oils were further tested on breast cancer (AU 565) and cervical cancer (HeLa) at 50 µg /mL using 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay and afterwards subjected to Gas Chromatography Mass Spectrometric (GCMS) analysis for its constituents. An LC50 of 188.67 and 8 µg/mL were obtained in the brine shrimp mortality and tadpole lethality assays respectively. The oil showed inhibitions of 86.74 and 21.8 % against AU 565 and HeLa cells respectively. GCMS analysis revealed the major constituents as sabinene (10.64 %) and (-)-4-terpineol (7.27 %). These results support its use in treating tumor-related ailments and should be considered for further studies.

Chemical composition and anticancer effects of Zingiber officinale volatile oil

Zingiber officinale rhizome is used in ethnomedicine in treating tumor-related ailments. This study was undertaken to evaluate the cytotoxic effects of this plant. The oil was extracted using a Clavenger apparatus by hydro-distillation method. Preliminary screening was carried out with brine shrimp cytotoxicity test at 10-1000 µg/mL. The volatile oil was further tested on breast cancer (AU 565) and cervical cancer (HeLa) at 50 µg /mL using MTT assay and later subjected to GCMS analysis. LC50 of 157.75 µg/mL was obtained in the brine shrimp mortality assay. Z. officinale oil showed high anticancer activities with 50 and 43 % inhibitions against HeLa and AU 565 cells respectively. GCMS analysis revealed the major constituents of Z. officinale oil as a-citral (11.68 %) and a-citral (10.18 %). These results suggest the medicinal potency of this plant oil.

A focus on biometal systems of some phyto-antibiotic drug complexes

Biometal coordination bearing active donor atoms of medicinal plant extracts or herbal isolates (phytochemicals) in the recent approach of biomedical sciences is a new and advanced chemotherapeutics for combating antibiotics resistance. Stereochemistry of central metal ions around active plant molecules can give rise to robust solid state 3D metal complexes of antibiotics aiding better biological performance/affinity without any side effect compared with the parent biomolecules (organic ligands). This review therefore focuses on the applications of medicinal plant extracts as antibiotics. Structural systems of metal complexes of flavonoids, curcumins, alkaloids, carotenoids and coumarins from aloe vera, acalypha and henna leaf (AAH) are also described with a view to achieving the rationale for functional bioactive antibiotic drugs

Plausible causes of low incidence of COVID 19 in Tropical Africa: A review

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Bioassay-guided isolation of cytotoxic constituents of Aframomum melegueta K.Schum. seeds

The seeds of Aframomum melegueta are used extensively in the Nigerian ethnomedicine for the management of cancer. This study therefore aimed at isolating and characterizing its cytotoxic constituents. Methanol extract of the seed was obtained through cold maceration, and it was further partitioned into n – hexane, dichloromethane and ethylacetate. The most active fraction was purified on repeated chromatographic techniques, using vacuum liquid chromatography (VLC), column (CC), and high-performance liquid chromatography (HPLC). The extract, purified fractions and isolated compounds were tested for their cytotoxic activities against the human Rhabdomyosarcoma (RD) and breast (MCF-7) cancer cell lines, using MTT assay. The crude extract and n-hexane fraction were found to be selectively cytotoxic to the cancer cell lines. Bioassay-guided fractionation of the n-hexane fraction led to the isolation of three compounds, which were identified as 6-shogaoal, 6-paradol, and 1-dehydro-6-gingerdione. 6-shogaoal demonstrated the highest cytotoxicity with CC50 values of 0.11 ± 0.02 and 0.25 ± 0.05ìg/mL against RD and MCF-7 cell lines respectively, and these were higher in activity when compared with cyclophosphamide (CC50 = 1.98 ± 0.15 and 0.71 ± 0.7ìg/mL). The presented data validates the ethnomedicinal use of A. melegueta in the treatment of cancer and is also indicative of the potential of 6-shogaol as an anticancer agent.