Blending Ethnomedicine with Modern Technology-From Conventional to Tailored Products: Modulating Biopharmaceutical Properties of Berberis Extract by Solid Lipid Nanoparticles for Wound Healing.

Drug-delivery systems employing phytopharmaceuticals based on the leads in traditional knowledge offers not only an alternative but quicker and more economic strategy for drug development. Nanophytopharmaceuticals promise remarkable opportunities with the ability to overcome challenges associated with herbal medicines, such as low solubility and bioavailability, poor target specificity, and shelf life. Berberis extracts documented as Ropana (wound healer) in Sushruta Samhita are a popular traditional remedy that is amiss in the modern system of medicine as it exhibits very poor biopharmaceutical properties. Poor solubility and bioavailability necessitate the administration of high doses to achieve the desired therapeutic effects. Exploiting the diversified type of compounds with pleiotropic properties present in Berberis, the biopharmaceutical properties were engineered using an optimized freeze-dried extract and developed solid lipid nanoparticles (SLNs) as an effective drug-delivery system. An industrially viable and environment-friendly hot high-pressure homogenization technique led to a stable formulation with an average particle size of 178.4 nm, as well as a 7-fold increase in loading and a significant entrapment of 91 ± 1.25%. The pharmacodynamic studies of developed nanosystems in excision-wound models showed faster and complete healing of wounds with no scars.

Is Failure of Cocrystallization Actually a Failure? Eutectic Formation in Cocrystal Screening of Hesperetin.

Cocrystal screening of hesperetin with certain countermolecules generated highly soluble noncovalent derivatives in the form of eutectics, instead of expected cocrystals. As adhesive forces established by complimentary functional groups on hesperetin and coformers were unable to overcome the stress due to size shape mismatch of component molecules, thus, eutectics were formed. Hesperetin, a polyphenolic antioxidant with potent anticancer and cardioprotective effects, has an underdeveloped role in modern therapeutics on account of its critically low aqueous solubility resulting in stunted bioavailability. The liquid-assisted cogrinding of hesperetin and coformers generated binary-phase eutectics in fixed stoichiometry with theophylline (1:1.5), adenine (2:1), gallic acid (1.5:1), and theobromine (2:1). Primarily characterized by lower melting endotherm in differential scanning calorimetry, the eutectics showed complete melting in hot-stage microscopy. Apart from characteristic V-shaped binary-phase diagram, no discernible changes in the FTIR and powder X-ray diffraction spectra further confirm eutectic formation. The morphological differences were analyzed by SEM measurements. A 2 to 4 times enhanced dissolution profile of the eutectics measured in pH 7.4 aqueous buffer was coupled with the in vitro (1,1-diphenyl-2-picryl hydroxyl free radical antioxidant assay and RBC antihemolytic assay) studies to present a complete preliminary data on the improved bioavailability of hesperetin eutectics.

Plant parts substitution based approach as a viable conservation strategy for medicinal plants: A case study of Premna latifolia Roxb.

BACKGROUND: Rapid population growth and catastrophic harvesting methods of wild medicinal plants especially trees, result in the exploitation of natural sources and its management is the need of the hour. Dashamoolarishta is an amalgam of roots of ten plants of a popular Ayurvedic FDC formulation consisting of the root of Premna latifolia Roxb. as one of its ingredients. Presently, their populations like many other trees are under threat due to extensive use of the roots by the herbal drug industry. OBJECTIVE: With an aim to conserve the biodiversity, a systematic study based on a rational approach by substituting root/root bark with alternative and renewable parts was conducted. MATERIALS AND METHODS: The fingerprint profile together with anti-inflammatory and analgesic effect of different parts of the plant was established for comparison. RESULTS: The results based on chemical and biological study indicated close similarity between the roots and the leaves and suggest the possible use of latter over root/root bark. CONCLUSION: The study proposes that the substitution of the root with alternate renewable parts of the same plant shall form the best strategy towards conservation of the trees like P. latifolia.

Current Perspective in the International Trade of Medicinal Plants Material: An Update.

BACKGROUND: The recent years have seen an increased interest in medicinal plants together with the therapeutic use of phytochemicals. Medicinal plants are utilized by the industry for the production of extracts, phytopharmaceuticals, nutraceuticals and cosmeceuticals and their use is expected to grow faster than the conventional drugs. The enormous demand of medicinal plant material has resulted in huge trade both at domestic and international levels. METHODS: The trade data of medicinal plant material with commodity code HS 1211 (SITC.4, code 292.4) and their derived/related products which are traded under different commodity codes has been acquired from COMTRADE, Trade Map, country reports, technical documents etc for the period 2001 to 2014. The data was analyzed using statistical tools to draw conclusions. RESULTS: The significant features of the global trade; the leading source, consumer, import and export countries; and the striking trends are presented. The trade of the ten key countries and the selected important items is also discussed in detail. The conservative figure of trade of medicinal plants materials and their derived/related products including extracts, essential oils, phytopharmaceuticals, gums, spices used in medicine, tannins for pharmaceutical use, ingredients for cosmetics etc. as calculated from the global export data for the year 2014 is estimated at USD 33 billion. The average global export in medicinal plants under HS 1211 for the fourteen year period was USD 1.92 billion for 601,357 tons per annum and for the year 2014 it stood at 702,813 tons valued at USD 3.60 billion. CONCLUSION: For the studied period, an annual average growth rate (AAGR) of 2.4% in volumes and 9.2% in values of export was observed. Nearly 30% of the global trade is made up by top two countries of the import and export. China and India from Asia; Egypt and Morocco from Africa; Poland, Bulgaria and Albania from Europe; Chile and Peru from South America are important supply sources. The USA, Japan and Europe are the major consumers of the world.

Amelioration of testosterone induced benign prostatic hyperplasia by Prunus species.

ETHNOPHARMACOLOGICAL RELEVANCE: Benign prostatic hyperplasia (BPH) is a common urological disorder of men. The ethnomedicinal use of an African plant Prunus africana (Hook.f.) Kalkman (Pygeum) in treating men's problems made it a popular remedy all over the globe for the treatment of BPH and related disorders. However, rampant collections made from the wild in Africa have pushed the plant to Appendix II of CITES demanding conservation of the species. AIM OF THE STUDY: In the present study, the aim was to unearth the protective effect of bark of different species of Prunus against BPH. The five selected Indian plants of family Rosaceae viz. Prunus amygdalus Stokes, Prunus armeniaca L., Prunus cerasoides Buch.-Ham. ex D. Don, Prunus domestica L. and Prunus persica (L.) Batsch were evaluated against P. africana (Hook.f.) Kalkman for a suitable comparison of efficacy as antiBPH agents. MATERIALS AND METHODS: The antiBPH activity was evaluated in testosterone (2mg/kg/day, s.c, 21 days) induced BPH in Wistar rats. The parameters studied were body weights; histopathological examination, immunohistochemistry (PCNA) and biochemical estimations of the prostate; supported by prostatic index, testicular index, creatinine, testosterone levels; antioxidant and anti-inflammatory evaluation. The study also included chemical profiling using three markers (ß-sitosterol, docosyl ferulate and ursolic acid) and estimation of ß-sitosterol content through GC. RESULTS: The Prunus species showed the presence of all the three markers in their TLC fingerprint profile and maximum amount of ß-sitosterol by GC was observed in P. domestica. Interestingly, all the species exhibited significant amelioration in testosterone induced parameters with P. domestica showing the most encouraging effect as indicated from histopathological examination, immunohistochemistry and biochemical studies. The Prunus species further showed remarkable anti-inflammatory and antioxidant activity signifying their role in interfering with various possible factors involved in BPH. CONCLUSIONS: These findings are suggestive of a meaningful inhibitory effect of testosterone induced BPH by the bark of different species of Prunus in the order of P. domestica, P. persica, P. amygdalus, P. cerasoides and P. armeniaca with an efficacy of P. domestica comparable to P. africana and can be used as the potential backup of Pygeum for the management of BPH.

Attenuating effect of bioactive coumarins from Convolvulus pluricaulis on scopolamine-induced amnesia in mice.

Convolvulus pluricaulis Chois. (Convolvulaceae) has been used in Ayurveda as Medhya Rasyana (nervine tonic) to treat various mental disorders. This study was designed to isolate the bioactive compound(s) of this plant and to evaluate their effect against scopolamine-induced amnesia. Column chromatography of the chloroform and ethyl-acetate fractions led to the isolation of three coumarins identified as scopoletin, ayapanin and scopolin. All the three compounds at 2.5, 5, 10 and 15 mg/kg, p.o. were evaluated for memory-enhancing activity against scopolamine-induced amnesia using elevated plus maze and step down paradigms. Effect on acetylcholinesterase activity in mice brain was also evaluated. Scopoletin and scopolin, in both the paradigms, significantly and dose dependently attenuated the scopolamine-induced amnesic effect. Furthermore, these compounds at 10 and 15 mg/kg exhibited activity comparable to that of standard drug, donepezil. The compounds also exhibited significant acetylcholinesterase inhibitory activity.

Nootropic, anxiolytic and CNS-depressant studies on different plant sources of shankhpushpi.

CONTEXT: Shankhpushpi, a well-known drug in Ayurveda, is extensively used for different central nervous system (CNS) effects especially memory enhancement. Different plants are used under the name shankhpushpi in different regions of India, leading to an uncertainty regarding its true source. Plants commonly used under the name shankhpushpi are: Convolvulus pluricaulis Chois., Evolvulus alsinoides Linn., both from Convolvulaceae, and Clitoria ternatea Linn. (Leguminosae). OBJECTIVE: To find out the true source of shankhpushpi by evaluating and comparing memory-enhancing activity of the three above mentioned plants. Anxiolytic, antidepressant and CNS-depressant activities of these three plants were also compared and evaluated. MATERIALS AND METHODS: The nootropic activity of the aqueous methanol extract of each plant was tested using elevated plus-maze (EPM) and step-down models. Anxiolytic, antidepressant and CNS-depressant studies were evaluated using EPM, Porsolt?s swim despair and actophotometer models, respectively. RESULTS: C. pluricaulis extract (CPE) at a dose of 100 mg/kg, p.o. showed maximum nootropic and anxiolytic activity (p < 0.001). E. alsinoides extract (EAE) and C. ternatea extract (CTE) showed maximum memory-enhancing and anxiolytic activity (p < 0.001) at 200 and 100?mg/kg, respectively. Amongst the three plants, EAE and CTE showed significant (p < 0.05), while CPE did not exhibit any antidepressant activity. All the three plants showed CNS-depressant action at higher dose levels. DISCUSSION AND CONCLUSIONS: The above results showed all the three plants possess nootropic, anxiolytic and CNS-depressant activity. The results of memory-enhancing activity suggest C. pluricaulis to be used as true source of shankhpushpi.