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Carissa, a genus of the Apocynaceae family, consists of evergreen species, such as shrubs as well as small trees that are native to Asia, Africa, and Oceania’s subtropical and tropical regions. Most of the Carissa species are traditionally used to treat various diseases, such as chest pain, headaches, gonorrhoea, rheumatism, syphilis, oedema, rabies, stomach pain, hepatitis, cardiac diseases, and asthma. The pharmacological studies on Carissa species revealed its antioxidant, antimicrobial, anticancer, cardioprotective, antipyretic, analgesic, wound healing, anticonvulsant, antiarthritic, adaptogenic, anti-inflammatory, and antidiabetic activities, thus validating its use in indigenous medicine systems. The review article summarised the comprehensive literature available, including morphology, indigenous uses, bioactive composition, nutraceutical, and pharmacological activities of Carissa species. A total of 155 research papers were cited in this review article. The Carissa fruits are rich in dietary fibre, lipids, proteins, carbohydrates, vitamin C, and macro- and micro-elements. A total of 121 compounds (35 polyphenols (flavonoids and phenolic acids), 30 lignans, 41 terpenoids, 7 steroids, 2 coumarins, and 6 cardiac glycosides) have been extracted from C. spinarum, C. carandas, and C. macrocarpa. Among all chemical constituents, lupeol, carissol, naringin, carisssone, scopoletin, carissaeduloside A, D, J, carandinol, sarhamnoloside, carissanol, olivil, carinol, 3β-hydroxyolean-11-en-28,13β-oilde, ursolic acid, and carissone are the key bioactive constituents responsible for pharmacological activities of genus Carissa. The gathered ethnopharmacological information in the review will help to understand the therapeutic relevance of Carissa as well as paving a way for further exploration in the discovery of novel plant-based drugs.

Conifers have long been recognized for their therapeutic potential in different disorders. Alkaloids, terpenes and polyphenols are the most abundant naturally occurring phytochemicals in these plants. Here, we provide an overview of the phytochemistry and related commercial products obtained from conifers. The pharmacological actions of different phytochemicals present in conifers against bacterial and fungal infections, cancer, diabetes and cardiovascular diseases are also reviewed. Data obtained from experimental and clinical studies performed to date clearly underline that such compounds exert promising antioxidant effects, being able to inhibit cell damage, cancer growth, inflammation and the onset of neurodegenerative diseases. Therefore, an attempt has been made with the intent to highlight the importance of conifer-derived extracts for pharmacological purposes, with the support of relevant in vitro and in vivo experimental data. In short, this review comprehends the information published to date related to conifers’ phytochemicals and illustrates their potential role as drugs.

Thymoquinone (TQ), a potent bioactive of Nigella sativa plant, is highly hydrophobic molecule and thus associated with poor oral bioavailability. The present work proposes the phospholipid-nanoparticles (PLN) based delivery of TQ to enhance the low oral bioavailability and anti-inflammatory activity. TQ-loaded nanoparticles were prepared via micro-emulsification technique employing different phospholipid concentrations and extensively characterized for particle size, surface charge, surface morphology, entrapment efficiency, and drug release kinetics. Further, the nanoparticles were assessed for oral bioavailability, and anti-inflammatory activity employing rat paw edema model. The optimized nanoparticle composition (F1) was nanosized ( 70%), controlled drug release pattern, and negatively charged surface (zeta potential of −0.57 mV). After oral administration of a single dose of F1 formulation, showed approx. 226.6% relative bioavailability vis-a-vis plain TQ suspension. While, substantially higher reduction in the percent inhibition in paw edema in comparison to the pure drug suspension and diclofenac sodium, was observed in the inflammation model. The present work indicate that PLN could be an efficient nanodevices for the treatment of inflammatory disorders and promising carrier system to augment TQ oral bioavailability.

Background: The poor biopharmaceutical properties of thymoquinone (TQ) obstruct its development as a hepatoprotective agent. To surmount the delivery challenges of TQ, phospholipid nanoconstructs (PNCs) were constructed. Method: PNCs were constructed employing microemulsification technique and systematic optimization by three-factor three level Box-Behnken design. Result: Optimized PNC composition exhibited nano size (90%), controlled drug release pattern, and neutral surface charge (zeta potential of −0.65 mV). After oral administration of a single dose of PNC, it showed a relative bioavailability of 386.03% vis-à-vis plain TQ suspension. Further, TQ-loaded PNC demonstrated significant enhanced hepato-protective effect vis-à-vis pure TQ suspension and silymarin, as evidenced by reduction in the ALP, ALT, AST, bilirubin, and albumin level and ratified by histopathological analysis. Conclusion: TQ-loaded PNCs can be efficient nano-platforms for the management of hepatic disorders and promising drug delivery systems to enhance oral bioavailability of this hydrophobic molecule.

Ethnopharmacological relevance Rheum emodi Wall., is an important medicinal plant extensively used in Ayurvedic and Unani systems of traditional medicine. It is known to possess antioxidant, antibacterial, antifungal, anticancer, wound healing and immune enhancing activities. Aim of the study The aim of the current study was to investigate the antimicrobial activity and synergistic potential of different solvent fractions and phytocompounds of Rheum emodi rhizome against bacterial and fungal pathogens. Material and methods The antimicrobial and synergistic potential of the crude methanolic extract, different solvent fractions (n-hexane, chloroform, ethyl acetate, and residual aqueous) and isolated phytocompounds of the rhizome of Rheum emodi were assayed by broth microdilution method. The bioactive phytocompounds were isolated through silica TLC and quantified using HPTLC and HPLC. The bioactive phytocompounds were identified by LC-MS analysis. Results Phytochemical analysis of the sub-fractions showed that the TPC (417.94 ± 1.2 mg g-1 GAE) and TFC (187.40 ± 0.5 mg g-1 RE) were highest in residual aqueous extracts. The chloroform sub-fraction possessed the highest antimicrobial activity against bacterial (Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae) and fungal strains (Candida albicans MTCC 277 and ATCC 90028). The MIC of chloroform sub-fraction against S. aureus, K. pneumoniae, E. coli, C. albicans was 1.95, 3.91, 15.62 and 62.5 μg ml-1, respectively. TLC and LC-MS analysis of chloroform sub-fraction identified phytocompounds namely emodin D4 (m/z 274.262), rhein13c6 (m/z 290.176), chrysophanol dimethyl ether (m/z 282.291), and resveratrol (m/z 340.456). Quantification of emodin content showed that the chloroform sub-fraction (101.4543 μg mg-1, 194.8037 μg mg-1 measured through HPTLC and HPLC, respectively), and its TLC fraction (II) (75.18 μg mg-1, 232.384 μg mg-1 measured through HPTLC and HPLC, respectively) are rich in emodin. Furthermore, chloroform sub-fraction, its TLC fractions and emodin showed profound synergistic activity in combination with antibacterial and antifungal antibiotics and lowered the dosage of antibiotics by 4–257 folds. Conclusions The bioassay guided fractionation of R. emodi rhizome methanolic extract identified phytocompounds (emodin, rhein13c6, chrysophanol dimethyl ether and resveratrol) that act as bioavailability enhancers of antibacterial and antifungal antibiotics, hence revealing their potential in treating multidrug resistance.

Glibenclamide, sulfonylurea receptor inhibitor, is reported to be neuroprotective in ischemic stroke by reducing cytotoxic edema, which is the primary cause of morbidity. As neurological worsening in stroke occurs from 3 to 10 days post-injury, there is a need to develop a system that would provide the release of glibenclamide for 10–15 days in a sustained manner in order to y improve the neurological functions effectively. In situ forming microparticles (ISFM) of glibenclamide was developed using PLGA 50:50 as a biodegradable polymer and by applying RSM I-Optimal design. In vitro evaluation studies were carried out for optimized formulation. In vivo pharmacological assessments and pharmacokinetics studies were performed in the Bilateral common carotid artery occlusion model (BCCAO) in Wistar rats. In vitro drug release studies showed a minimum burst release at 12 h and maximum release on 15th day. In vivo results showed a significant improvement in neurological functions, reduction in the infarct area, and hemispheric swelling in glibenclamide ISFM treated animals as compared to diseased animals. From in vitro and in vivo animal studies, it was concluded that long-acting ISFM of glibenclamide was successfully developed, which showed drug release pattern in a sustained manner for up to 15 days for preventing the neurological worsening in stroke.

Objective: To observe gender specific seasonal variation of two phenolic glycosides (PG’s) (populin and salicin) in Populus ciliata male and female trees.Methods: Plant material (bark) was collected from male and female trees throughout the year. The content of salicin and populin was measured using HPLC. Because of the lack of populin in the market, the standard compound was synthesized in the laboratory from salicin following standard procedure. Confirmation and characterization of synthesized populin were done using 1H NMR and 13C NMR. TLC and LC-MS of methanolic extract were performed to observe the presence of populin and salicin in the plant bark.Results: TLC showed the presence of populin and salicin in crude plant extract at Rf value 0.84 and 0.52, respectively. The results of monthly variation showed a consistent pattern of two PG’s for both the sexes. However, salicin content was observed highest compared to populin content. Whereas female trees were observed with low content of PG’s compared to male trees. The maximum content of salicin and populin was observed in the flowering season. LC-MS of bark methanolic extract confirmed the presence of a significantly larger peak, which was identified as a cinnamoyl-salicin peak at 463.Conclusion: The study confirms the highest content of PG’s in the flowering season. Additionally, LC-MS study concluded a new compound cinnamoyl-salicin (M+at 463) which is reported first time to the best of author’s knowledge. It seems that it could be the denaturation product of 2'-O-cinnamoyl salicortin and can be further explored for biological applications.