Development of phytosterol-loaded silver nanoparticles for ameliorating haemorrhoidal complications via the AMPK pathway-a mechanistic approach.

The aim of the current study was to synthesize silver nanoparticles (PLSNPs) using green technology by means of phytosterol-enriched fractions fromBlumea laceraextracts (EAF) and evaluate their toxicological and anti-haemorrhoidal potential. The average size of the synthesized particles was found to be 85.64 nm by scanning electron microscopy and transmission electron microscopy. Energy dispersive spectroscopy showed the elemental composition of PLSNPs to be 12.59% carbon and 87.41% silver, indicating the capping of phytochemicals on the PLSNPs. The PLSNPs were also standardized for total phytosterol content using chemical methods and high-perfromance liquid chromatography. The PLSNPs were found to be safe up to 1000 mg kg-1as no toxicity was observed in the acute and sub-acute toxicity studies performed as per OECD guidelines. After the induction of haemorrhoids, experimental animals were treated with different doses of EAF, PLSNPs and a standard drug (Pilex) for 7 d, and on the eighth day the ameliorative potential was assessed by evaluating the haemorrhoidal (inflammatory severity index, recto-anal coefficient) and biochemical (tumour necrosis factor-alpha and interleukin-6) parameters and histology of the recto-anal tissue. The results showed that treatment with PLSNPs and Pilex significantly (p< 0.05) reduced haemorrhoidal and biochemical parameters. This was further supported by restoration of altered antioxidant status. Further, a marked reduction in the inflammatory zones along with minimal dilated blood vessels was observed in the histopathological study. The results of molecular docking studies also confirmed the amelioration of haemorrhoids via AMP-activated protein kinase (AMPK)-mediated reduction of inflammation and endothelin B receptor modification by PLSNPs. In conclusion, PLSNPs could be a good alternative for the management of haemorrhoids.

Evaluation of anticancer activity of Gmelina asiatica leaves, in-vitro and in-silico studies.

Cervical cancer poses a major threat to women's health worldwide, constituting the fourth most prevalent cancer among the female population. High-risk variants of human papillomavirus (HPV) with its oncogenic proteins are a necessary cause of cervical cancer. Due to the resistance of cancer cells to the current treatment, there is a need for new medicines with new strategies to treat cervical cancer. Gmelina asiatica Linn. is a medicinal plant with various traditional uses and biological activities. Its anticancer potential against breast cancer and lymphoma has been demonstrated in the literature. In view of this, our study aims to investigate the anticancer activity of Gmelina asiatica leaves against cervical cancer. Various extracts of Gmelina asiatica leaves were prepared by soxhletation and maceration methods. The cytotoxic activity of the extracts was evaluated through in-vitro studies against SiHa cell line using MTT assay and fluorescence imaging. The most potent extract (GAME) phytochemical profile was analysed by UHPLC-HRMS. Further, in-silico studies were performed on its phytoconstituents against E6 oncoprotein, and the DFT studies were conducted on the active component to assess the physicochemical properties. In-vitro studies revealed that methanolic extract (GAME) showed the highest inhibition on the SiHa cell line compared to the other extracts and the control (p < 0.0001). In-silico studies indicated high affinity with stable interaction of the compound 5 (JC5ABDR) at E6 binding sites. This study revealed the importance of Gmelina asiatica plant as a potential source of anticancer molecules with a specific mode of action against cervical cancer.Communicated by Ramaswamy H. Sarma.

Icacinaceae Plant Family: A Recapitulation of the Ethnobotanical, Phytochemical, Pharmacological, and Biotechnological Aspects.

Icacinaceae, an Angiospermic family comprising 35 genera and 212 accepted species, including trees, shrubs, and lianas with pantropical distribution, is one of the most outshining yet least explored plant families, which despite its vital role as a source of pharmaceuticals and nutraceuticals has received a meagre amount of attraction from the scientific community. Interestingly, Icacinaceae is considered a potential alternative resource for camptothecin and its derivatives, which are used in treating ovarian and metastatic colorectal cancer. However, the concept of this family has been revised many times, but further recognition is still needed. The prime objective of this review is to compile the available information on this family in order to popularize it in the scientific community and the general population and promote extensive exploration of these taxa. The phytochemical preparations or isolated compounds from the Icacinaceae family have been centrally amalgamated to draw diverse future prospects from this inclusive plant species. The ethnopharmacological activities and the associated endophytes and cell culture techniques are also depicted. Nevertheless, the methodical evaluation of the Icacinaceae family is the only means to preserve and corroborate the folkloristic remedial effects and provide scientific recognition of its potencies before they are lost under the blanket of modernization.

Wound healing activity of the ethanol root extract and polyphenolic rich fraction from Potentilla fulgens.

CONTEXT: Potentilla fulgens Wall. ex Hook (Rosaceae) is a potent medicinal plant of the Western Himalayas, where its roots are traditionally used by the local people of Uttaranchal (India) to treat wounds and tiger bites. OBJECTIVE: The present study scientifically evaluates the wound healing activity of P. fulgens ethanol root extract (EPF) and its ethyl acetate fraction (PFEA) on experimental rats. MATERIALS AND METHODS: Wounds were inflicted on animals by using both excision and incision models. The wounded animals were treated for 16 days with EPF (oral: 200-400 mg/kg and topical: 5-10% w/w) and PFEA (oral: 75 mg/kg; topical: 1.75% w/w). Various physical (wound contraction, epithelialization rate, tensile strength) and biochemical parameters (hydroxyproline, hexosamine, proteins, DNA) were examined during the study. Oxidant product (lipidperoxidase), antioxidant enzymes (catalase, superoxide-dismutase) and reduced glutathione were determined. Morphological and histopathological studies of the skin tissues were monitored. RESULTS: A significant (p < 0.05) wound healing property was observed when the animals were treated topically with EPF (10% w/w) and PFEA (1.75% w/w). A significantly (p < 0.05) increased in the levels of hydroxyproline, hexosamine, protein and DNA up to 59.22, 70.42, 61.01 and 60.00% was observed, respectively. This effect was further demonstrated by the morphological and histopathological representation, thus showing significant (p < 0.05) re-epethelialization on the healing area. EPF and PFEA also showed significant (p < 0.05) antioxidant activity. CONCLUSIONS: The present study provided the scientific evidence, where P. fulgens rich in polyphenolic components possess remarkable wound healing activities, thereby supporting the traditional claims.

Phytochemical standardization, antioxidant, and antibacterial evaluations of Leea macrophylla: A wild edible plant.

In Ayurveda, Leea macrophylla Roxb. ex Hornem. (Leeaceae) is indicated in worm infestation, dermatopathies, wounds, inflammation, and in symptoms of diabetes. The present study aims to determine the antioxidant and antibacterial potential of ethanolic extract and its different fractions of Leea macrophylla root tubers using phytochemical profiling which is still unexplored. Quantitative estimations of different phytoconstituents along with characterization of ethanol extract using high performance liquid chromatography (HPLC) were performed using chlorogenic acid as a marker compound for the first time. The extract and its successive fractions were also evaluated for in vitro antioxidant activity using different models. The extract was further tested against a few Gram-positive and Gram-negative bacteria for its antibacterial activity. Phytochemical screening and quantitative estimations revealed the extract to be rich in alkaloid, flavonoid, phenols, and tannins, whereas chlorogenic acid quantified by HPLC in ethanol extract was 9.01% w/w. The results also indicated potential antioxidant and antibacterial activity, which was more prominent in the extract followed by its butanol fraction.

Cryptocoryne spiralis, a substitute of Aconitum heterophyllum in the treatment of diarrhoea.

OBJECTIVE: To scientifically validate the traditional substitution of roots of highly expensive Aconitum heterophyllum (AH) with rhizomes of Cryptocoryne spiralis (CS) in the treatment of diarrhoea. METHODS: Different fractions from root/rhizome extract of both the plant were subjected to faecal excretion rate and castor oil-induced diarrhoea models. Further, bioactive fractions from both plants, i.e. chloroform (CAH) from AH at 50 mg/kg p.o. and ethyl acetate (EACS) from CS at 100 mg/kg p.o., were examined for small intestinal transit, intestinal fluid accumulation and PGE2 -induced enteropooling models in rats. Biochemical estimations and Na(+) and K(+) concentration in intestinal fluid were also determined along with antibacterial studies. Phytochemical standardisation of AH and CS was performed by quantifying aconitine for the former and stigmasterol for the latter using HPLC. KEY FINDINGS: CAH and EACS illustrated a significant reduction in faecal output rate and demonstrated a protection of 63.068% at CAH 50 and 59.090% at EACS 100 mg/kg p.o. in castor oil-induced diarrhoea model. The fractions also persuaded promising effects in all the other models, restored alterations in biochemical parameters and showed potential antibacterial activity. CONCLUSION: The antidiarrhoeal potential of AH and CS may be attributed to an antimotility and antisecretory type of effect.

Antisecretory and antimotility activity of Aconitum heterophyllum and its significance in treatment of diarrhea.

AIM: The roots of the plant Aconitum heterophyllum (EAH) are traditionally used for curing hysteria, throat infection, dyspepsia, abdominal pain, diabetes, and diarrhea. Therefore, the present study was undertaken to determine the mechanism involved in the anti-diarrheal activity of roots of A. heterophyllum. MATERIALS AND METHODS: Ant-diarrheal activity of ethanol extract at 50, 100, and 200 mg/kg p.o. was evaluated using fecal excretion and castor oil-induced diarrhea models, while optimized dose, that is, 100 mg/kg p.o. was further subjected to small intestinal transit, intestinal fluids accumulation, PGE2-induced enteropooling and gastric emptying test. To elucidate the probable mechanism, various biochemical parameters and Na(+), K(+) concentration in intestinal fluids were also determined. Further, antibacterial activity of extract along with its standardization using aconitine as a marker with the help of HPLC was carried out. RESULTS: The results depicted a significant (P < 0.05) reduction in normal fecal output at 100 and 200 mg/kg p.o. of extract after 5th and 7th h of treatment. Castor oil-induced diarrhea model demonstrated a ceiling effect at 100 mg/kg p.o. with a protection of 60.185% from diarrhea. EAH at 100 mg/kg p.o. also showed significant activity in small intestinal transit, fluid accumulation, and PGE2-induced enteropooling models, which also restored the altered biochemical parameters and prevented Na(+) and K(+) loss. The extract with 0.0833% w/w of aconitine depicted a potential antibacterial activity of extract against microbes implicated in diarrhea. CONCLUSION: The study concluded antisecretory and antimotility effect of A. heterophyllum, which mediates through nitric oxide path way.

Antidiarrhoeal evaluation of root extract, its bioactive fraction, and lupinifolin isolated from Eriosema chinense.

The roots of the plant Eriosema chinense are traditionally used by the tribal people of North East India for treatment of diarrhoea. Therefore, the present investigation was undertaken to scientifically validate the traditional claim that these roots have an antidiarrhoeal effect. Ethanol extract along with three fractions, ethyl acetate, chloroform, and hexane, as well as isolated lupinifolin from the chloroform fraction, were screened for the normal faecal excretion rate and castor oil-induced diarrhoea model. The results demonstrated a significant (p < 0.05) reduction in normal faecal output at ethanol extract 400, chloroform fraction 100, chloroform fraction 200, and lupinifolin 10 mg/kg p. o. after the 3rd, 5th, and 7th hours of treatment. Also, the same dose level of ethanol extract, chloroform fraction, and lupinifolin depicted maximum protection from diarrhoea in the castor oil-induced diarrhoea model showing a ceiling effect at chloroform fraction 100 mg/kg p. o. Ethanol extract at 400, its bioactive fraction chloroform fraction at 100, and lupinifolin at 10 mg/kg p. o. significantly inhibited peristaltic index, intestinal fluid volume, and PGE2-induced enteropooling. They also restored alterations in biochemical parameters such as nitric oxide, total carbohydrates, protein, DNA, superoxide dismutase, catalase, and lipid peroxidation. The ethanol extract, chloroform fraction, and lupinifolin demonstrated a significant recovery from Na+ and K+ loss and a pronounced antibacterial activity against bacterial strains mainly implicated in diarrhoea. Phytochemical analysis revealed the ethanol extract and chloroform fraction to be highly rich in flavonoids, phenols, alkaloids, and tannin contents, whereas lupinifolin (a prenylated flavanone), isolated and quantified by HPTLC for the first time, was found to comprise 6.480 % and 6.718 % (w/w) of the ethanol extract and chloroform fraction, respectively. The antidiarrhoeal activity of the chloroform fraction was found to be the highest, followed by those of the ethanol extract and lupinifolin, which may be due to the presence of lupinifolin along with other phytoconstituents. Thus, the study scientifically validated the antidiarrhoeal potential of the roots from E. chinense, which may be attributed to antimotility- and antisecretory-type effects with a potential antibacterial activity.

Wound-healing potential of the root extract of Albizzia lebbeck.

The present investigation is an attempt to scientifically validate the traditional use of the roots of the plant Albizzia lebbeck in Ayurvedic system of medicine for curing wounds. The study included phytochemical standardization of the ethanol root extract of A. lebbeck, which was further subjected to oral acute toxicity study. Wound-healing activity of the ethanol root extract was evaluated using incision and excision wound models. Biochemical parameters such as hydroxyproline, hexuronic acid, hexosamine, and antioxidant enzymes like superoxide dismutase, reduced glutathione and free radical parameters including lipid peroxidation and nitric oxide were evaluated on the 10th post-wounding day following dead space method. For confirmation of activity, histopathology of the wounds and granulation tissues from excision and dead space wound model were performed. The study also included assessment of antibacterial activity of ethanol root extract against strains implicated in wound infection. The ethanol root extract was found to be highly rich in flavonoids, saponins, phenols, and tannins, while the amount of rutin was found to be 4.66 % w/w. It significantly increased the wound breaking strength showing a ceiling effect at 500 mg/kg p. o. The ethanol root extract at 500 mg/kg p. o. depicted an optimum wound contraction on the 18th day, while complete wound contraction was observed at the 22nd post wound day. It also demonstrated a significant increase in dry tissue weight, total protein, hydroxyproline, hexosamine, hexuronic acid, superoxide dismutase, and reduced glutathione levels, whereas a decrease in the levels of lipid peroxidation and nitric oxide was also observed with a potential antibacterial activity. Histopathological studies revealed a normal epithelization and fibrosis which was evidenced through an increase in collagen density. Thus, the study scientifically validated the wound-healing activity of the ethanol root extract along with a potential antibacterial property which may be attributed to the enhanced collagen synthesis and a potential antioxidant activity.

Gastroprotective activity of ethanolic root extract of Potentilla fulgens Wall. ex Hook.

ETHNOPHARMACOLOGICAL RELEVANCE: Potentilla fulgens (Wall.) ex Hook. (Rosaceae) is a potent medicinal plant of the Western Himalayas, known under the name "Himalayan Cinquefoil or Bajradanti", and has been used traditionally to treat ailments including peptic ulcers, mouth ulcers, diarrhea, diabetes and cancer. OBJECTIVE: The aim of the present study was to scientifically evaluate the gastric-ulcer protective effect of P. fulgens ethanolic root extract (EPF) on experimental rats. MATERIAL AND METHODS: The gastroprotective activity of EPF was evaluated on four gastric-ulcer models such as pyloric ligation (PL), ethanol (EtOH), cold restrain stress (CRS) and aspirin (ASP)-induced gastric ulcers. The gastric acid obtained from 4h PL-induced gastric ulcer rats was determined for total volume content, pH and total acid-pepsin output. Total carbohydrates and protein ratio, expressed as index of mucin activity, and DNA content were estimated in the gastric juice and gastric mucosal tissue. The microvascular permeability, H(+)K(+)-ATPase activity, gastric mucus and histamine content were also determined. The levels of antioxidant enzymes (superoxide dismutase, catalase, and glutathione) and malondialdehyde in the stomach tissue (mucosal scrapings) were quantified. A histopathological study of the stomach was evaluated using eosin-haematoxylin stain. RESULTS: EPF (200-400mg/kg, p.o.) showed significant protection against acute gastric-ulcer induced by EtOH, PL and CRS (400mg/kg, p.o.), but was found to be ineffective against ASP-induced ulcerogens. The effect of EPF on gastric juice studies in 4h PL rats significantly produced an increased level in gastric pH, whereas the effect on gastric volume and acid-pepsin output was observed to decrease significantly. However, EPF was found to have no significant effect on the defensive factors, thus revealing its antisecretory property by inhibiting the aggressive factors. EPF, significantly decreased the histamine level, inhibited the H(+)K(+)-ATPase activity and prevented the microvascular injury caused by ethanol in the rat stomach. Moreover, it was also observed to have antioxidant effects by producing a significant increase in the levels of SOD, CAT, and GSH and decreased the LPO activity. Histopathological studies showed that EPF significantly prevented gastric lesions caused by ethanol. CONCLUSIONS: The present study showed that EPF has potent gastroprotective and antisecretory effects, thus justifying the traditional usage of this herb to treat gastric ulcers.

Antidiabetic activity of alcoholic leaves extract of Alangium lamarckii Thwaites on streptozotocin-nicotinamide induced type 2 diabetic rats.

OBJECTIVE: To investigate antidiabetic potential of alcoholic leaves extract of Alangium lamarckii (A. lamarckii) on streptozotocin-nicotinamide induced type 2 diabetic rats. METHODS: Oral glucose tolerance test was done by inducing hyperglycemic state via administration of glucose in water (2g/kg). Single dose of alcoholic leaves extract of A. lamarckii (250 and 500 mg/kg, p.o.) were administered to normoglycemic, hyperglycemic rats. Type 2 diabetes was induced by single intraperitoneal injection of nicotinamide (110 mg/kg) followed by streptozotocin (65mg/kg). The study also included estimations of blood plasma glucose, lipid profile, liver glycogen, body weight and antioxidant status in normal and diabetic rats. RESULTS: Admistration of alcoholic extract of A. lamarckii at two dosage 250 and 500 mg/kg, p.o. did not showed any significant change in blood glucose level of normoglycemic rats (P>0.05), whereas, oral glucose tolerance test depicted reduction in blood glucose level (P<0.05). The streptozotocin-nicotinamide induced diabetic rats, significantly decreased the blood plasma glucose level (P<0.001) comparable to glibenclamide (10 mg/kg), restored the lipid profile and showed improvement in liver glycogen, body weight and antioxidant status in diabetic rats. CONCLUSIONS: Present finding demonstrated the significant antidiabetic activity of alcoholic leaves extract of A. lamarckii.

Inhibitory effect of two Indian medicinal plants on aldose reductase of rat lens in vitro.

OBJECTIVE: To assesse the inhibitory effect of alcoholic extract of two Indian medicinal plants namely Ceasalpinia digyna Rottler and, Alangium lamarckii Thwaits on aldose reductase (AR) of rat lens. METHODS: Rats lens were enucleated through posterior approach and their homogenate was prepared and centrifuged to obtain a clear supernatant for the determination of AR activity and protein content. RESULTS: The alcoholic extract of Ceasalpinia digyna and Alangium lamarckii had a potent inhibitory effect on the lens AR enzyme. The IC(50) values of alcoholic extract of the selected plants were calculated and were (46.29±11.17) and (106.00±5.11) µg/mL, respectively. Quercetin was used as a positive control and its IC(50) value was (2.95±1.53) µg/mL. CONCLUSIONS: Thus, it is concluded that alcoholic extracts of the selected plant exhibit significant inhibitory effects on AR in the rat lens in vitro.

Pedalium murex Linn.: an overview of its phytopharmacological aspects.

Pedalium murex Linn (family: Pedaliaceae) (P. murex) commonly known as Large Caltrops and Gokhru (India) is a shrub found in the Southern part, Deccan region of India and in some parts of Ceylon. Different parts of the plant are used to treat various ailments like, cough, cold and as an antiseptic. Interestingly, P. murex is reported traditionally to have an excellent cure in patients with reproductive disorders which are mainly impotency in men, nocturnal emissions, gonorrhoea as well as leucorrhoea in women. The plant has also benifited in complications like urinary track disorder as well as gastro intestinal tract disorders. Phytochemically the plant is popular for the presence of a considerable amount of diosgenin and vanillin which are regarded as an important source and useful starting materials for synthesizing steroidal contraceptive drugs and isatin alkaloids. Other phytochemicals reported in the plant includes quercetin, ursolic acid, caffeic acid, amino acids (glycine, histidine, tyrosine, threonine, aspartic acid and glutamic acid) and various classes of fatty acids (triacontanoic acid, nonacosane, tritriacontane, tetratriacontanyl and heptatriacontan-4-one). Pharmacologically, the plant have been investigated for antiulcerogenic, nephroprotective, hypolipidemic, aphrodisiac, antioxidant, antimicrobial and insecticidal activities. From all these reports it can be concluded that the plant were found to have a better profile with potential natural source for the treatment of various range of either acute or chronic disease. The overall database of our review article was collected from the scientific sources in regards with all the information of the research article for P. murex published so far.

Evaluation of phytochemical and antioxidant activities of the different fractions of Hybanthus enneaspermus (Linn.) F. Muell. (Violaceae).

OBJECTIVE: To investigate the naturally occurring antioxidant for the first time from the different solvent fractions of Hybanthus enneaspermus (H. enneaspermus) Linn F. Muell. family (Violaceae). METHODS: Different fractions of H. enneaspermus were tested for total phenolic content, and in vitro antioxidant activity was measured by total antioxidant assay, DPPH assay, reducing power, nitric oxide (NO), hydrogen peroxide (H(2)O(2)) scavenging assays. RESULTS: The ethyl acetate (EA) fraction was found to have high levels of phenolic content [(212.15±0.79) mg GAE/g]. The EA fraction exhibited higher total antioxidant capacity, higher percentage of DPPH radical scavenging activity [(127.07±2.29) µg/mL], nitric oxide [(245.16±1.44) µg/mL], hydrogen peroxide [(227.38±7.18) µg/mL], deoxyribose [(270.61±8.72) µg/mL] and higher reducing power. There was a significant correlation between total phenolic content and total antioxidant activity (r(2)=0.972). CONCLUSIONS: These results reveal that EA fraction of H. enneaspermus has strong antioxidant potential compared with other fractions. Our further study has been extended to the isolation of the possible compound that is responsible for having antioxidant property.

Ethnomedicinal plants used for diarrhea by tribals of Meghalaya, Northeast India.

Environmental status and diarrhea is regarded as a complex and multidimensional topic. Diarrhea is one of the main water-borne diseases considered to be endemic in many regions of the world and brings the major health threats to the world populations, both in tropical and subtropical poor countries. The state Meghalaya situated in the North-Eastern India is an upland landmass bound by seven districts surrounded within by different tribes. The population is predominantly rural, with 81.41% of the population belongs merely to the scheduled tribes. The state offers a wide range of disease environments, dominated by communicable diseases (35.68%), and diarrhea is one of the water-borne diseases that alter the society of the state. Various factors like poor environmental sanitation, unavailability of safe drinking water, seasonal rainfall, infected foods, infection through fomites, flies, cockroaches, etc. are the main culprit that led to the cause of diarrhea in the state. The local people are very much closely associated with nature, and with their ethnobiological knowledge about the plants available around them, they can easily avert and cure themselves from several disease complications. In this review, the information regarding the traditional method of utilization of 58 plant species that are used to treat and cure diarrhea and dysentery are enlisted briefly.

Antinociceptive activity of steroid alkaloids isolated from Solanum trilobatum Linn.

Solasodine (1) was isolated for the first time from the roots of Solanum trilobatum Linn., a member of the Solanaceae, and assessed for its presumed antinociceptive activity using several experimental murine models, viz. the writhing, formalin, and hot plate tests. When used at doses of 2, 4, and 8 mg/kg, this steroidal alkaloid caused a significant and dose-dependent decrease in the nociception induced by an intraperitoneal injection of acetic acid (p < 0.001). It also led to a significant reduction of the painful sensation caused by formalin in both phases of the formalin test (p < 0.001). Furthermore, the alkaloid produced a significant increase in the reaction time in the hot plate test (p < 0.001). These results suggest that solasodine elicited antinociceptive activity through both central and peripheral mechanisms.