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The amorphous form of poorly soluble drugs is physically unstable and prone to crystallization, resulting in decreased solubility and bioavailability. However, the conventional accelerated stability test for amorphous drugs is time-consuming and inaccurate. Therefore, there is an urgent need to develop rapid and accurate stability assessment technology. This study used the antitumor drug nilotinib free base as a model drug. The degree of disorder and physical stability in the amorphous form was assessed by applying the pair distribution function (PDF) and principal component analysis (PCA) methods based on powder X-ray diffraction (PXRD) data. Specifically, the assessment conditions, such as the PDF interatomic distance range, PXRD detector type, and PXRD diffraction angle range were also optimized. The results showed that more reliable PCA data could be obtained when the PDF interatomic distance range was 0–15 Å. When the PXRD detector was a semiconductor-type detector, the PDF data obtained were more accurate than other detectors. When the PXRD diffraction angle range was 5–40°, the intermolecular arrangement of the amorphous drugs could be accurately predicted. Finally, the accelerated stability test also showed that under the above-optimized conditions, this method could accurately and rapidly assess the degree of disorder and physical stability in the amorphous form of drugs, which has obvious advantages compared with the accelerated stability test. [ABSTRACT FROM AUTHOR]

Lignanoids are an active ingredient exerting powerful antioxidant and anti-inflammatory effects in the treatment of many diseases. In order to improve the efficiency of the resource utilization of traditional Chinese medicine waste, Magnolia officinalis Rehder & E.H.Wilson residue (MOR) waste biomass was used as raw material in this study, and a series of deep eutectic solvents (ChUre, ChAce, ChPro, ChCit, ChOxa, ChMal, ChLac, ChLev, ChGly and ChEG) were selected to evaluate the extraction efficiency of lignanoids from MORs. The results showed that the best conditions for lignanoid extraction were a liquid–solid ratio of 40.50 mL/g, an HBD-HBA ratio of 2.06, a water percentage of 29.3%, an extract temperature of 337.65 K, and a time of 107 min. Under these conditions, the maximum lignanoid amount was 39.18 mg/g. In addition, the kinetics of the extraction process were investigated by mathematic modeling. In our antioxidant activity study, high antioxidant activity of the lignanoid extract was shown in scavenging four different types of free radicals (DPPH, ·OH, ABTS, and superoxide anions). At a concentration of 3 mg/mL, the total antioxidant capacity of the lignanoid extract was 1.795 U/mL, which was equal to 0.12 mg/mL of Vc solution. Furthermore, the antibacterial activity study found that the lignanoid extract exhibited good antibacterial effects against six tested pathogens. Among them, Staphylococcus aureus exerted the strongest antibacterial activity. Eventually, the correlation of the lignanoid extract with the biological activity and physicochemical properties of DESs is described using a heatmap, along with the evaluation of the in vitro hypoglycemic, in vitro hypolipidemic, immunomodulatory, and anti-inflammatory activity of the lignanoid extract. These findings can provide a theoretical foundation for the extraction of high-value components from waste biomass by deep eutectic solvents, as well as highlighting its specific significance in natural product development and utilization. [ABSTRACT FROM AUTHOR]

To increase the effectiveness of using typical biomass waste as a resource, iridoids, chlorogenic acid, and flavonoids from the waste biomass of Eucommia ulmoides leaves (EULs) were extracted by deep eutectic solvents (DESs) in conjunction with macroporous resin. To optimize the extract conditions, the experiment of response surface was employed with the single-factor of DES composition molar ratio, liquid–solid ratio, water percentage, extraction temperature, and extraction time. The findings demonstrated that the theoretical simulated extraction yield of chlorogenic acid (CGA), geniposidic acid (GPA), aucubin (AU), geniposide (GP), rutin (RU), and isoquercetin (IQU) were 42.8, 137.2, 156.7, 5.4, 13.5, and 12.8 mg/g, respectively, under optimal conditions (hydrogen bond donor–hydrogen bond acceptor molar ratio of 1.96, liquid–solid ratio of 28.89 mL/g, water percentage of 38.44%, temperature of 317.36 K, and time of 55.59 min). Then, 12 resins were evaluated for their adsorption and desorption capabilities for the target components, and the HPD950 resin was found to operate at its optimum. Additionally, the HPD950 resin demonstrated significant sustainability and considerable potential in the recyclability test. Finally, the hypoglycemic in vitro, hypolipidemic in vitro, immunomodulatory, and anti-inflammatory effects of EUL extract were evaluated, and the correlation analysis of six active components with biological activity and physicochemical characteristics of DESs by heatmap were discussed. The findings of this study can offer a theoretical foundation for the extraction of valuable components by DESs from waste biomass, as well as specific utility benefits for the creation and development of natural products. [ABSTRACT FROM AUTHOR]

Breast cancer is the leading cause of cancer-related fatalities in female worldwide. Effective therapies with low side effects for breast cancer treatment and prevention are, accordingly, urgently required. Targeting anticancer materials, breast cancer vaccines and anticancer drugs have been studied for many years to decrease side effects, prevent breast cancer and suppress tumors, respectively. There are abundant evidences to demonstrate that peptide-based therapeutic strategies, coupling of good safety and adaptive functionalities are promising for breast cancer therapy. In recent years, peptide-based vectors have been paid attention in targeting breast cancer due to their specific binding to corresponding receptors overexpressed in cell. To overcome the low internalization, cell penetrating peptides (CPPs) could be selected to increase the penetration due to the electrostatic and hydrophobic interactions between CPPs and cell membranes. Peptide-based vaccines are at the forefront of medical development and presently, 13 types of main peptide vaccines for breast cancer are being studied on phase III, phase II, phase I/II and phase I clinical trials. In addition, peptide-based vaccines including delivery vectors and adjuvants have been implemented. Many peptides have recently been used in clinical treatments for breast cancer. These peptides show different anticancer mechanisms and some novel peptides could reverse the resistance of breast cancer to susceptibility. In this review, we will focus on current studies of peptide-based targeting vectors, CPPs, peptide-based vaccines and anticancer peptides for breast cancer therapy and prevention. [ABSTRACT FROM AUTHOR]

Development of efficient resource utilization and waste management strategies is highly required to meet ever increasing huge demand and consumption and to avoid reliance on fossil-based sources. Recently, the concept of circular economy has gained more attentions so as to achieve the core sustainable development goals. This study presented initial steps towards total valorisation of biomass with integrated biorefinery approach and the concept of circular economy. Industrial hemp residue (IHR) and spent mushroom substrate (SMS) were considered as a case study in the current research. Different pretreatment methods were employed to hydrolyse individual and/or various mix ratios of IHR and SMS. Finally, analysis of the raw materials, hydrolysates, and residual solids were undergone to gain some insights, identify key research gaps, and forward for future optimization of the process. The results showed that SMS was noticeably more degradable than IHR and cohydrolysis of mixture of these substrates have provided considerable advantages. [ABSTRACT FROM AUTHOR]

Succinic acid (SA) is one of the top candidate value-added chemicals that can be produced from biomass via microbial fermentation. A considerable number of cell factories have been proposed in the past two decades as native as well as non-native SA producers. Actinobacillus succinogenes is among the best and earliest known natural SA producers. However, its industrial application has not yet been realized due to various underlying challenges. Previous studies revealed that the optimization of environmental conditions alone could not entirely resolve these critical problems. On the other hand, microbial in silico metabolic modeling approaches have lately been the center of attention and have been applied for the efficient production of valuable commodities including SA. Then again, literature survey results indicated the absence of up-to-date reviews assessing this issue, specifically concerning SA production. Hence, this review was designed to discuss accomplishments and future perspectives of in silico studies on the metabolic capabilities of SA producers. Herein, research progress on SA and A. succinogenes, pathways involved in SA production, metabolic models of SA-producing microorganisms, and status, limitations and prospects on in silico studies of A. succinogenes were elaborated. All in all, this review is believed to provide insights to understand the current scenario and to develop efficient mathematical models for designing robust SA-producing microbial strains. [ABSTRACT FROM AUTHOR]

A rapid, green, and cost‐effective route for the preparation of graphene nanosheets (GRNs) from their layered bulks by the ultrasonic together with mechanical grinding was reported. The whole exfoliation process of synthesizing GRNs lasted just 2 hours without involvement of any acid solvent or other organic solvents; only one kind of waste biomass as adhesive could be used. The structure and morphology of GRNs were characterized and then was then introduced into polypropylene by melt blending, and the cone calorimetry test results indicated that the presence of GRNs could enhance the flame retardancy of PP composite. [ABSTRACT FROM AUTHOR]

Multidrug resistance (MDR) of tumor cells to chemotherapeutic agents is the main reason for the failure of cancer chemotherapy. Overexpression of ABCB1 transporter that actively pumps various drugs out of the cells has been considered a major contributing factor for MDR. Over the past decade, many antimicrobial peptides with antitumor activity have been identified or synthesized, and some antitumor peptides have entered the clinical practice. In this study, we report that peptide HX-12C has the effect of reversing ABCB1-mediated chemotherapy resistance. In ABCB1-overexpressing cells, nontoxic dose of peptide HX-12C inhibited drug resistance and increased the effective intracellular concentration of paclitaxel and other ABCB1 substrate drugs. The mechanism study showed that peptide HX-12C stimulated ABCB1 ATPase activity without changing the expression level and localization patterns of ABCB1. Molecular docking predicted the binding modes between peptide HX-12C and ABCB1. Overall, we found that peptide HX-12C reverses ABCB1-mediated MDR through interacting with ABCB1 and blocking its function without affecting the transporter's expression and cellular localization. Our findings suggest that this antimicrobial peptide may be used as a novel prospective cancer therapeutic strategy in combination with conventional anticancer agents. [ABSTRACT FROM AUTHOR]

Ceaseless growth in human population led to high demand in everything. Currently, the world largely depends on petroleum-based "all material synthesis" scheme. On the other hand, depletion of fossil-based resources and their huge impact on environmental pollution have forced us to search for sustainable and eco-friendly alternative resources. In this context, the notion to utilize waste biomass could possibly provide environmental and economic benefits. This study was carefully designed to critically review state of the art in the transformation of waste biomass into value-added products. Even though extensive reviews on biomass utilization have been published in the past few years, the current study basically focused on new trends and prospective in this area. Here, global biomass potential, research developments and practices, novel biomass transformation approaches, and future perspectives were broadly discussed. More importantly, in addition to revising published researches, already implemented and ongoing large-scale projects on valorization of waste biomass have been assessed. Therefore, this study is believed to give crucial information on the current status and future direction of waste biomass utilization so as to accomplish the quest towards green economy. Key Points • Huge biomass potential and dramatically increase in R&D trends on waste biomass. • Selection of appropriate waste biomass valorization techniques. • Development of efficient and feasible waste biomass transformation technology. • Coproduction of low-value, high-volume and high-value, low volume products. [ABSTRACT FROM AUTHOR]

Due to environmental issues and the depletion of fossil-based resources, ecofriendly sustainable biomass-based chemical production has been given more attention recently. Succinic acid (SA) is one of the top value added bio-based chemicals. It can be synthesized through microbial fermentation using various waste steam bioresources. Production of chemicals from waste streams has dual function as it alleviates environmental concerns; they could have caused because of their improper disposal and transform them into valuable products. To date, Actinobacillus succinogenes is termed as the best natural SA producer. However, few reviews regarding SA production by A. succinogenes were reported. Herewith, pathways and metabolic engineering strategies, biomass pretreatment and utilization, and process optimization related with SA fermentation by A. succinogenes were discussed in detail. In general, this review covered vital information including merits, achievements, progresses, challenges, and future perspectives in SA production using A. succinogenes. Therefore, it is believed that this review will provide platform to understand the potential of the strain and tackle existing hurdles so as to develop superior strain for industrial applications. It will also be used as a baseline for identification, isolation, and improvement of other SA-producing microbes. [ABSTRACT FROM AUTHOR]

In this study, a novel biorefinery concept of succinic acid (SA) production from fruit and vegetable wastes (FVWs) hydrolyzed by crude enzyme mixtures through solid state fermentation was designed. Enzyme complex solid mashes from various types of FVWs were on-site produced through solid-state fermentation by Aspergillus niger and Rhizopus oryzae . This solid was then added to FVW suspensions and undergo hydrolysis reaction to generate fermentable sugars and other essential nutrients for bacterial growth and product formation. The subsequent fungal hydrolysis produced 12.00 g/L glucose and 13.83 g/L fructose using 10% mass ratio (w/v) of FVW. Actinobacillus succinogenes used this FVW hydrolysate as the sole feedstock and produced 27.03 g/L of succinic acid with high yield and productivity of 1.18 g SA/g sugar and 1.28 gL −1 h −1 , respectively. This work demonstrated that FVWs can be biotransformed to value added products which have considerable potential economics and environmental meaning. [ABSTRACT FROM AUTHOR]

This study isolated fascinating novel fungal consortium from pomelo peel (PP) to discover its potential for on-site production of lignocellulose degrading enzymes through solid-state fermentation (SSF). SSF strategy was developed to use low and high recalcitrant substrates including PP and industrial hemp residue (IHR), respectively. The result revealed that SSF using a mixture of these substrates was significantly enhanced as compared with the corresponding individual substrate. IHR was pretreated with autohydrolysis, thermal hydrolysis, and thermochemical hydrolysis. A green and sustainable catalyst, oxalic acid, was employed to further optimize the thermochemical pretreatment of IHR. Pretreatment with 3% (w/v) oxalic acid resulted the highest sugar which is 8.3 and 3.24 folds compared to autohydrolysis and thermal hydrolysis, respectively. Finally, a novel approach dubbed one-pot pretreatment and saccharification was implemented using IHR treated with 2% oxalic acid and enzymes generated by SSF of mixed substrates. This strategy resulted the highest sugar production of 39.49 g/L. The current study can be considered as a proof-of-concept for sustainable and economic production of bio-based products from waste biomass resources. • Fungal consortium was isolated and identified from PP to produce enzymes via SSF. • Utilization of a mixture of low and high recalcitrant substrate enhanced SSF. • SSF and IHR pretreatment processes were optimized. • Oxalic acid was used as a green and sustainable catalyst to pretreat IHR. • One-pot pretreatment and saccharification of IHR resulted 39.49 g/L sugar. [ABSTRACT FROM AUTHOR]

This was early-stage, proof-of-concept research on the full utilization of biomass resources. The current study considered industrial hemp residue (IHR) and spent mushroom substrate (SMS) to demonstrate the initial upstream steps towards the total valorization of biomass. Accordingly, different pretreatment methods such as autohydrolysis, thermal hydrolysis, and thermochemical hydrolysis methods were employed against individual and various mix ratios of IHR and SMS. To this end, raw materials, hydrolysates, and residual solids were analyzed to gain some insights, identify gaps, and suggest future research directions in this area. Implementation of the full utilization of biomass resources is, in fact, not only a matter of transforming the resources into valuable products, but it is also a plausible waste management strategy in the quest towards the development of a circular bioeconomy and sustainable future. [ABSTRACT FROM AUTHOR]

Since the fluctuation of cellular selenocysteine (Sec) concentration plays an all-important role in the development of numerous human disorders, the real-time fluorescence detection of Sec in living systems has attracted plenty of interest during the past decade. In order to obtain a faster and more sensitive small organic molecule fluorescence sensor for the Sec detection, a new ratiometric fluorescence sensor Q7 was designed based on the fluorescence resonance energy transfer (FRET) strategy with coumarin fluorophore as energy donor and 4-hydroxy naphthalimide fluorophore (with 2,4-dinitrobenzene sulfonate as fluorescence signal quencher and Sec-selective recognition site) as an energy acceptor. The sensor Q7 exhibited only a blue fluorescence signal, and displayed two well distinguished emission bands (blue and green) in the presence of Sec with ∆λ of 68 nm. Moreover, concentrations ranging of quantitative detection of Sec of Q7 was from 0 to 45 μM (limit of detection = 6.9 nM), with rapid ratiometric response, high sensitivity and selectivity capability. Impressively, the results of the living cell imaging test demonstrated Q7 has the potentiality of being an ideal sensor for real-time Sec detection in biosystems. [ABSTRACT FROM AUTHOR]

• Tolerance level of A. succinogenes against HMF and furfural was scrutinized. • Inhibitory effect was investigated using single and mixed sugars. • A. succinogenes showed more tolerance against HMF than furfural. • Synergetic effect of inhibitors was severe relative to individual inhibitor. • A. succinogenes exhibited more preference to glucose than xylose. Pretreatment is crucial step to overcome the stiffness of lignocellulosic materials so as to make sugars available for subsequent enzymatic hydrolysis and microbial fermentation. Unfortunately, commonly used pretreatment methods cause formation of various toxic degradation products that have inhibitory effect on growth and fermentation. Hydroxymethylfurfural (HMF) and furfural are furan derivative inhibitors generated via degradation of hexoses and pentoses, respectively. In this study, inhibitory effects of HMF and furfural (0–10 g/L) on succinic acid producing Actinobacillus succinogenes were investigated using lignocellulosic model sugars of glucose and xylose. To this end, A. succinogenes attained explicable level of tolerance against these inhibitors but better performance with HMF than furfural. Nevertheless, synergetic effect of these inhibitors was severer compared with individual one. Overall, this study could provide vital notions to understand strain's tolerance level, and thereby helps to apply efficient pretreatment methods, utilize appropriate substrates, and develop robust biocatalysts. [ABSTRACT FROM AUTHOR]

Chitosan (CS) films were developed incorporating peptide HX-12C. The films were studied to determine their microstructures, physical properties, release properties of peptide HX-12C and functional properties. The results indicated that there may be hydrogen bonding interactions between CS and peptide HX-12C, thereby creating a homogeneous internal microstructure and lower crystallinity (10.8–12.8 %). Compared with CS film, CS-HX-12C films displayed lower light transmission, MC (20.8–19.9 %), WVP (8.82–8.59 × 10−11·g·m−1·s−1·Pa−1), OTR (0.015–0.037 cc/(m2.day)) and higher WS (15.7–32.4 %) values. Moreover, controlled-release experiments showed that pH, ionic strength and temperature could all significantly affect the release of peptide HX-12C from the films. Finally, the increase of pH value and TVC and lipid oxidation of fresh pork were delayed due to the treatment with CS-2%HX-12C film. However, incorporating peptide HX-12C into CS films did not improve the mechanical properties of the films and their effects against protein oxidation. Our results suggest that the CS-based antimicrobial packaging films integrated with peptide HX-12C exhibit the potential for fresh pork preservation. [ABSTRACT FROM AUTHOR]

• Timeline and R&D trends in peptide-based drug applications have been discussed. • Recent technological advancements in the therapeutic development of peptide drugs have been thoroughly assessed. • Challenges particularly drug formulation, peptide synthesis, and drug resistance related to peptide drugs have been presented. • Future outlooks in the development of efficient and sustainable peptide drugs have been proposed. Among other health related issues, the rising concerns on drug resistance led to look for alternative pharmaceutical drugs that are effective both against infectious and noninfectious diseases. Antimicrobial peptides (AMPs) emerged as potential therapeutic molecule with wide range of applications. With their limitations, AMPs have gained reputable attentions in research as well as in the pharmaceutical industry. This review highlighted the historical background, research trends, technological advancements, challenges, and future perspectives in the development and applications of peptide drugs. Some vital questions related with the need for pharmaceutical production, factors for the slow and steady journey, the importance of oral bioavailability, and the drug resistance possibilities of AMPs were raised and addressed accordingly. Therefore, the current study is believed to provide a profound understanding in the past and current scenarios and future directions on the therapeutic impacts of peptide drugs. [Display omitted] [ABSTRACT FROM AUTHOR]

In this study, glycine (GLY) was introduced into layers of kaolinite (Kaol-GLY) by intercalated and replaced to further enhance the flame retardancy and thermal stability properties of polypropylene (PP) containing intumescent flame-retardant (IFR) composite after deeply characterized and analyzed. The results indicated GLY successfully intercalated into the layers of Kaol. The presence of 1.5 wt% Kaol-GLY could increase the limit oxygen index and char residues of PP (75.0 wt%)/ IFR (23.5 wt%) composite, and decrease the value of peak heat/ smoke release rate. Structure and morphology analysis of char by SEM and FTIR demonstrated that Kaol-GLY could contribute to improve the char quality of PP composite. Furthermore, this work can also provide a way for preparing intercalated Kaol with hydrophilicity amino acids compared to similar prior literature, and the flame-retardant mechanism of PP/ IFR composite was deeply speculated and analyzed based on thermogravimetric-infrared analysis and real-time-FTIR results under the presence of Kaol-GLY. [Display omitted] • A novel intercalation compound was obtained by GLY intercalated Kaol (GLY-Kaol). • Kaol-GLY played an excellent effect on the flame retardancy of PP. • Flame-retardant mechanism of Kaol-GLY in PP/IFR composite was deeply analyzed. [ABSTRACT FROM AUTHOR]